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Dasatinib (BMS-354825) Tyrosinekinase-remmer

Name: Dasatinib (BMS-354825)
Brand: Selleck Chemicals
SKU: S1021
Rating: 5 (619 reviews)

Cat.Nr.S1021

Dasatinib is een nieuwe, krachtige en multi-gerichte remmer die zich richt op Abl, Src en c-Kit, met IC50 van respectievelijk <1 nM, 0,8 nM en 79 nM in celvrije assays. Dasatinib induceert autophagy en apoptosis met anti-tumoractiviteit.

Dasatinib (BMS-354825) Src remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 488.01

Ga naar

Kwaliteitscontrole

Batch: Zuiverheid: 99.99%

99.99

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Gerelateerde doelwitten	EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl
Overige Src Inhibitoren	WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 1-Naphthyl PP1(1-NA-PP1) RK 24466

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	PMID
M07ep210	Growth Inhibition Assay		72 h	DMSO	IC50=0.00007 μM	17956080
K562	Growth Inhibition Assay		72 h	DMSO	IC50=0.001 μM	17956080
M07e	Growth Inhibition Assay		72 h	DMSO	IC50=0.0012 μM	17956080
ALL3	Cytotoxic Assay	0.1μM	72 h	DMSO	IC50=0.0004 μM	19889540
CML	Growth Inhibition Assay		20 min	DMSO	IC50=0.001 μM	19219016
BA/F3	Growth Inhibition Assay		72 h	DMSO	IC50=6.589 μM	23088644
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant with IC50 of 0.00083μM	23088644
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl with IC50 of 0.0045μM	23088644
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant with IC50 of 1.714μM	23088644
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth Inhibition with IC50 of 0.0009μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth Inhibition with IC50 of 0.0032μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth Inhibition with IC50 of 0.0051μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth Inhibition with IC50 of 0.008μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth Inhibition with IC50 of 0.0013μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth Inhibition with IC50 of 0.0019μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth Inhibition with IC50 of 0.0023μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth Inhibition with IC50 of 3.6μM	23301703
BA/F3	Growth Inhibition Assay		72 h	DMSO	Induces cytotoxicity against mouse BA/F3 cells assessed as growth Inhibition with IC50 of 2.5μM	23301703
T cell	Growth Inhibition Assay		72 h	DMSO	Inhibits anti CD3- and anti CD28-induced T cell proliferation with IC50 of 0.003μM	17154512
WiDr	Growth Inhibition Assay		72 h	DMSO	IC50=0.052 μM	15615512
PC3	Growth Inhibition Assay		72 h	DMSO	IC50=0.0094 μM	15615512
MDA-MB-231	Growth Inhibition Assay		72 h	DMSO	IC50=0.012 μM	15615512
Hs578T	Cytotoxic Assay		72 h	DMSO	GI50=0.03 μM	24015327
HMEC	Cytotoxic Assay		72 h	DMSO	GI50=1.8 μM	24015327
DU145	Cytotoxic Assay		72 h	DMSO	GI50=0.16 μM	24015327
U251	Cytotoxic Assay		72 h	DMSO	GI50=2.81 μM	24015327
NCI60	Cytotoxic Assay		72 h	DMSO	GI50=5.7 μM	24015327
MALME-3M	Cytotoxic Assay		72 h	DMSO	GI50=6.61 μM	24015327
KM12	Cytotoxic Assay		72 h	DMSO	GI50=7.44 μM	24015327
SW620	Cytotoxic Assay		72 h	DMSO	GI50=8.43 μM	24015327
RXF 393NL	Cytotoxic Assay		4 days	DMSO	IC50=0.0217 μM	23253074
LXFA 983L	Cytotoxic Assay		4 days	DMSO	IC50=0.0565 μM	23253074
PRXF DU145	Cytotoxic Assay		4 days	DMSO	IC50=0.0623 μM	23253074
PAXF 1657L	Cytotoxic Assay		4 days	DMSO	IC50=0.121 μM	23253074
CXF 1103L	Cytotoxic Assay		4 days	DMSO	IC50=4.36 μM	23253074
GXF251L	Cytotoxic Assay		4 days	DMSO	IC50=2.25 μM	23253074
NCI-H23	Growth Inhibition Assay		72 h	DMSO	IC50=2.27 μM	23521020
HCT116	Growth Inhibition Assay		72 h	DMSO	IC50=2.3 μM	23521020
MCF7	Growth Inhibition Assay		72 h	DMSO	IC50=2.57 μM	23521020
NCI-H460	Growth Inhibition Assay		72 h	DMSO	IC50=8.99 μM	23521020
DLD1	Growth Inhibition Assay		72 h	DMSO	IC50=4.6 μM	23567960
NCI-H661	Growth Inhibition Assay		72 h	DMSO	IC50=7.8 μM	23567960
A549	Growth Inhibition Assay		72 h	DMSO	IC50=8.2 μM	23567960
U937	Growth Inhibition Assay		72 h	DMSO	IC50=12.2 μM	23567960
HEK293	Function Assay	10 μM		DMSO	Induces binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells with IC50 of 0.063μM	22770610
HUVEC	Growth Inhibition Assay	0.15 μM	72 h	DMSO	Induces antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as Inhibition of cell growth at 0.15 uM	22853993
HUVEC	Function Assay	15 μM	72 h	DMSO	Induces antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as Inhibition of network formation at 1.8 to 15 uM	22853993
Plasmodium falciparum	Function Assay	10 μM	15 min	DMSO	Inhibits Plasmodium falciparum proliferation by inhibiting the Function of PfCDPK1 protein with IC50 of 1.17μM	24550330
PC3	Function Assay	0.1 μM	5 h	DMSO	Inhibits human PC3 cell adhesion at 100 nM	19462975
DU145	Function Assay	0.1 μM	5 h	DMSO	Inhibits human DU145 cell adhesion at 100 nM	19462975
PC3	Kinase Assay	0.1 μM	5 h	DMSO	Inhibits cSrc in human PC3 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM	19462975
DU145	Kinase Assay	0.1 μM	5 h	DMSO	Inhibits cSrc in human DU145 cells assessed as reduction of phosphorylated Src Y416 level at 100 nM	19462975
PC3	Kinase Assay	0.1 μM	5 h	DMSO	Inhibits cSrc in human PC3 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM	19462975
DU145	Kinase Assay	0.1 μM	5 h	DMSO	Inhibits cSrc in human DU145 cells assessed as reduction of phosphorylated FAK Y576/Y577 level at 100 nM	19462975
Huh7	Antiviral Assay	2.5 μM	4 days	DMSO	Inhibits viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM	17360676
C6/36	Antiviral Assay	2.5 μM	4 days	DMSO	Inhibits viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM	17360676
U937	Function Assay	1 μM	1 h	DMSO	Reduces basal TNFalpha release in human U937 cells	17684099
U937	Function Assay	1 μM	1 h	DMSO	Reduces LPS-induced TNFalpha release in human U937 cells	17684099
murine mast cell	Function Assay	1 μM	24 h	DMSO	Inhibits antigen-induced IL6 secretion in IgE primed mouse mast cells at 1 uM	17684099
FDC-P1	Function assay		48 hrs		IC50 = 0.0074 μM	20156689
K562	Cytotoxicity assay		72 hrs		IC50 = 12.83 μM	22217877
U937	Cytotoxicity assay		72 hrs		IC50 = 13.63 μM	22217877
Sf21	Function assay		5 mins		IC50 = 10 μM	22961681
Ba/F3	Function assay		1 hr		Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis	23600806
Ba/F3	Function assay		1 hr		Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis	23600806
Ba/F3	Function assay		1 hr		Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis	23600806
Sf9	Function assay		15 to 20 mins		IC50 = 13.1 μM	23956101
Sf9	Function assay		20 mins		IC50 = 27.3 μM	23956101
HMC-1.2	Antiproliferative assay				IC50 = 0.82 μM	25004409
RXF 393NL	Antiproliferative assay		4 days		GI50 = 0.0217 μM	25076195
LXFA 983L	Antiproliferative assay		4 days		GI50 = 0.0565 μM	25076195
PRXF DU145	Antiproliferative assay		4 days		GI50 = 0.0623 μM	25076195
PAXF 1657L	Antiproliferative assay		4 days		GI50 = 0.121 μM	25076195
GXF251L	Antiproliferative assay		4 days		GI50 = 2.25 μM	25076195
CXF 1103L	Antiproliferative assay		4 days		GI50 = 4.36 μM	25076195
SH-SY5Y	Apoptosis assay	0.1 uM	24 hrs		Induction of apoptosis in human SH-SY5Y cells assessed as accumulation of hypodiploid cells at 0.1 uM after 24 hrs by propidium iodide staining-based cytofluorimetry	25469771
ECRF24	Cytotoxicity assay		72 hrs		IC50 = 5.7 μM	25815152
A2780	Cytotoxicity assay		72 hrs		IC50 = 8.7 μM	25815152
HEK293	Cytotoxicity assay		72 hrs		IC50 = 14.3 μM	25815152
MDA-MB-231	Cytotoxicity assay		72 hrs		IC50 = 0.178 μM	25835317
MDA-MB-231	Antiinvasive assay	0.1 uM	24 hrs		Antiinvasive activity against human MDA-MB-231 cells at 0.1 uM after 24 hrs by transwell assay	25835317
MDA-MB-231	Cell cycle assay	0.3 uM	24 to 48 hrs		Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 0.3 uM after 24 to 48 hrs by flow cytometric analysis	25835317
MDA-MB-231	Function assay	>0.03 uM	20 hrs		Inhibition of Src in human MDA-MB-231 cells assessed as reduction of FAK phosphorylation at >0.03 uM after 20 hrs by Western blot analysis	25835317
MDA-MB-231	Antimigratory assay	0.03 to 0.3 uM	20 hrs		Antimigratory activity against human MDA-MB-231 cells at 0.03 to 0.3 uM after 20 hrs by wound healing assay	25835317
MDA-MB-231	Function assay	0.001 to 1 uM	20 hrs		Inhibition of Src phosphorylation in human MDA-MB-231 cells at 0.001 to 1 uM after 20 hrs by Western blot analysis	25835317
MDA-MB-231	Antiproliferative assay	>0.01 uM	12 days		Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of colony formation at >0.01 uM after 12 days by crystal violet staining-based assay	25835317
MDA-MB-231	Antitumor assay	40 mg/kg/day	18 days		Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 40 mg/kg/day administered for 18 days measured every 3 days during compound dosing	25835317
MDA-MB-231	Cytotoxicity assay		48 hrs		IC50 = 1.12 μM	25899332
MCF7	Cytotoxicity assay		48 hrs		IC50 = 8.05 μM	25899332
HCC366	Antiproliferative assay		72 hrs		IC50 = 0.029 μM	26191369
NCI-H2286	Antiproliferative assay		72 hrs		IC50 = 0.032 μM	26191369
K562	Antiproliferative assay		72 hrs		IC50 = 0.001 μM	26195136
K562	Cytotoxicity assay				IC50 = 0.08 μM	26264503
IR-K562	Cytotoxicity assay				IC50 = 1.9 μM	26264503
THP1	Cytotoxicity assay				IC50 = 6 μM	26264503
HEK293	Cytotoxicity assay				CC50 = 16 μM	26264503
K562	Cytotoxicity assay		48 hrs		IC50 = 0.45 μM	26451772
K562	Antiproliferative assay		72 hrs		GI50 = 0.0003 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.0003 μM	26789553
KU812	Antiproliferative assay		72 hrs		GI50 = 0.0003 μM	26789553
MEG01	Antiproliferative assay		72 hrs		GI50 = 0.0003 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.001 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.001 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.001 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.003 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.004 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.004 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.005 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.008 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.008 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.01 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.014 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.014 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.017 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 0.039 μM	26789553
CHL	Antiproliferative assay		72 hrs		GI50 = 0.27 μM	26789553
MOLM14	Antiproliferative assay		72 hrs		GI50 = 2.3 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 3 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 3 μM	26789553
MV4-11	Antiproliferative assay		72 hrs		GI50 = 3.6 μM	26789553
HEL	Antiproliferative assay		72 hrs		GI50 = 5.3 μM	26789553
BA/F3	Function assay		72 hrs		GI50 = 9.94 μM	26789553
KU812	Function assay	0.1 uM	1 hr		Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
KU812	Function assay	0.1 uM	1 hr		Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
MEG01	Function assay	0.1 uM	1 hr		Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
MEG01	Function assay	0.1 uM	1 hr		Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
K562	Function assay	0.1 uM	1 hr		Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
K562	Function assay	0.1 uM	1 hr		Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 0.1 uM after 1 hr by immunoblotting method	26789553
K562	Cytotoxicity assay		72 hrs		IC50 = 0.00025 μM	26814890
BA/F3	Cytotoxicity assay		72 hrs		IC50 = 0.09 μM	26814890
BAF3	Function assay		72 hrs		EC50 = 0.00004 μM	27010810
BAF3	Function assay		72 hrs		EC50 = 0.00004 μM	27010810
BxPC3	Antiproliferative assay		72 hrs		EC50 = 0.033 μM	27010810
MDA-MB-231	Antiproliferative assay		72 hrs		EC50 = 0.044 μM	27010810
Caki2	Antiproliferative assay		72 hrs		EC50 = 0.055 μM	27010810
NCI-H1975	Antiproliferative assay		72 hrs		EC50 = 0.173 μM	27010810
PC3	Antiproliferative assay		72 hrs		EC50 = 0.232 μM	27010810
insect	Function assay		20 mins		IC50 = 0.0005 μM	27115835
MDA-MB-231	Antiproliferative assay		5 days		Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 days by PrestoBlue assay	27115835
MDA-MB-231	Function assay	3 to 100 nM	1.5 hrs		Inhibition of SRC phosphorylation at tyrosine 416 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis	27115835
MDA-MB-231	Function assay	3 to 100 nM	1.5 hrs		Inhibition of FAK phosphorylation at tyrosine 861 in human MDA-MB-231 cells at 3 to 100 nM preincubated for 1.5 hrs followed by serum stimulation for 1 hr by Western blot analysis	27115835
MDA-MB-231	Antimigratory assay	10 nM	6 hrs		Antimigratory activity in human MDA-MB-231 cells assessed as reduction in cell motility at 10 nM at 6 hrs by microscopy based scratch-wound cell migration assay	27115835
MCF7	Antiproliferative assay	0.03 to 300 uM	5 days		Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability at 0.03 to 300 uM after 5 days by PrestoBlue assay	27115835
HCT116	Cytotoxicity assay		96 hrs		IC50 = 5.23 μM	27155464
A549	Cytotoxicity assay		96 hrs		IC50 = 8.37 μM	27155464
U937	Cytotoxicity assay		96 hrs		IC50 = 10.23 μM	27155464
K562	Cytotoxicity assay		96 hrs		IC50 = 11.95 μM	27155464
K562	Cytotoxicity assay				CC50 = 0.25 μM	27474918
K562	Antiproliferative assay				GI50 = 0.001 μM	28435526
K562	Function assay				IC50 = 0.000069 μM	29395973
HL60	Function assay				IC50 = 0.00011 μM	29395973
KG1a	Function assay				IC50 = 8.98 μM	29395973
B16-BL6	Function assay	8.13 uM	24 to 48 hrs		Inhibition of cell migration of mouse B16-BL6 cells at 8.13 uM incubated for 24 to 48 hrs by cell wound scratch assay	29395973
MCF7	Function assay	7.5 uM	10 days		Inhibition of colony formation in human MCF7 cells at 7.5 uM incubated for 10 days by crystal violet staining based plate cloning test	29395973
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
HEK293	Function assay		1 hr		Ki = 0.0005 μM	29941193
HEK293	Function assay		1 hr		IC50 = 0.006 μM	29941193
Ba/F3	Function assay		48 hrs		GI50 = 0.00021 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.00025 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.00029 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.0003 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.00033 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.00042 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.00077 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.00098 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 0.00144 μM	30137981
Ba/F3	Function assay		48 hrs		GI50 = 2.562 μM	30137981
Vero	qHTS assay				Vero cells viability qHTS for Zika virus inhibitors	33229545
HepG2	qHTS assay				HepG2 cells viability qHTS for Zika virus inhibitors	33229545
BV-173	Growth Inhibition Assay				IC50=0.000000109 μM	SANGER
K-562	Growth Inhibition Assay				IC50=0.000000266 μM	SANGER
BL-70	Growth Inhibition Assay				IC50=0.000000822 μM	SANGER
EM-2	Growth Inhibition Assay				IC50=0.00000108 μM	SANGER
LAMA-84	Growth Inhibition Assay				IC50=0.00000321 μM	SANGER
MEG-01	Growth Inhibition Assay				IC50=0.0000098 μM	SANGER
EoL-1-cell	Growth Inhibition Assay				IC50=0.0000131 μM	SANGER
CTV-1	Growth Inhibition Assay				IC50=0.0000404 μM	SANGER
TE-15	Growth Inhibition Assay				IC50=0.00589 μM	SANGER
NOS-1	Growth Inhibition Assay				IC50=0.00613 μM	SANGER
D-336MG	Growth Inhibition Assay				IC50=0.0063 μM	SANGER
LB1047-RCC	Growth Inhibition Assay				IC50=0.00989 μM	SANGER
LB996-RCC	Growth Inhibition Assay				IC50=0.00991 μM	SANGER
SW982	Growth Inhibition Assay				IC50=0.01115 μM	SANGER
TK10	Growth Inhibition Assay				IC50=0.01174 μM	SANGER
A704	Growth Inhibition Assay				IC50=0.01491 μM	SANGER
TE-8	Growth Inhibition Assay				IC50=0.01576 μM	SANGER
DOHH-2	Growth Inhibition Assay				IC50=0.01719 μM	SANGER
HOP-62	Growth Inhibition Assay				IC50=0.01834 μM	SANGER
TE-12	Growth Inhibition Assay				IC50=0.01861 μM	SANGER
KGN	Growth Inhibition Assay				IC50=0.01942 μM	SANGER
NCI-H1648	Growth Inhibition Assay				IC50=0.02011 μM	SANGER
OS-RC-2	Growth Inhibition Assay				IC50=0.0203 μM	SANGER
GB-1	Growth Inhibition Assay				IC50=0.02157 μM	SANGER
RXF393	Growth Inhibition Assay				IC50=0.02357 μM	SANGER
LC-2-ad	Growth Inhibition Assay				IC50=0.02586 μM	SANGER
KS-1	Growth Inhibition Assay				IC50=0.0273 μM	SANGER
ETK-1	Growth Inhibition Assay				IC50=0.02832 μM	SANGER
SW954	Growth Inhibition Assay				IC50=0.02927 μM	SANGER
Becker	Growth Inhibition Assay				IC50=0.03003 μM	SANGER
MZ1-PC	Growth Inhibition Assay				IC50=0.03119 μM	SANGER
ES6	Growth Inhibition Assay				IC50=0.03193 μM	SANGER
KURAMOCHI	Growth Inhibition Assay				IC50=0.03487 μM	SANGER
CGTH-W-1	Growth Inhibition Assay				IC50=0.03548 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay				IC50=0.03902 μM	SANGER
LXF-289	Growth Inhibition Assay				IC50=0.03956 μM	SANGER
MPP-89	Growth Inhibition Assay				IC50=0.04049 μM	SANGER
SW872	Growth Inhibition Assay				IC50=0.04161 μM	SANGER
SNB75	Growth Inhibition Assay				IC50=0.04435 μM	SANGER
PSN1	Growth Inhibition Assay				IC50=0.04474 μM	SANGER
LB831-BLC	Growth Inhibition Assay				IC50=0.04609 μM	SANGER
MFH-ino	Growth Inhibition Assay				IC50=0.04724 μM	SANGER
TGBC24TKB	Growth Inhibition Assay				IC50=0.04761 μM	SANGER
A388	Growth Inhibition Assay				IC50=0.05095 μM	SANGER
BB30-HNC	Growth Inhibition Assay				IC50=0.05437 μM	SANGER
GI-ME-N	Growth Inhibition Assay				IC50=0.06118 μM	SANGER
TGBC1TKB	Growth Inhibition Assay				IC50=0.06164 μM	SANGER
TE-10	Growth Inhibition Assay				IC50=0.06357 μM	SANGER
A498	Growth Inhibition Assay				IC50=0.07284 μM	SANGER
TE-11	Growth Inhibition Assay				IC50=0.07858 μM	SANGER
BB65-RCC	Growth Inhibition Assay				IC50=0.08227 μM	SANGER
C2BBe1	Growth Inhibition Assay				IC50=0.08308 μM	SANGER
NCI-H747	Growth Inhibition Assay				IC50=0.08362 μM	SANGER
IST-MES1	Growth Inhibition Assay				IC50=0.08552 μM	SANGER
KALS-1	Growth Inhibition Assay				IC50=0.0949 μM	SANGER
GCIY	Growth Inhibition Assay				IC50=0.09656 μM	SANGER
RL95-2	Growth Inhibition Assay				IC50=0.1038 μM	SANGER
TE-1	Growth Inhibition Assay				IC50=0.1054 μM	SANGER
NCI-H1355	Growth Inhibition Assay				IC50=0.11028 μM	SANGER
SW962	Growth Inhibition Assay				IC50=0.11292 μM	SANGER
KLE	Growth Inhibition Assay				IC50=0.11317 μM	SANGER
MC116	Growth Inhibition Assay				IC50=0.1141 μM	SANGER
NMC-G1	Growth Inhibition Assay				IC50=0.11606 μM	SANGER
KU812	Growth Inhibition Assay				IC50=0.11883 μM	SANGER
COLO-829	Growth Inhibition Assay				IC50=0.12213 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay				IC50=0.12283 μM	SANGER
IST-MEL1	Growth Inhibition Assay				IC50=0.1345 μM	SANGER
MLMA	Growth Inhibition Assay				IC50=0.14032 μM	SANGER
LS-123	Growth Inhibition Assay				IC50=0.14064 μM	SANGER
LB2518-MEL	Growth Inhibition Assay				IC50=0.14162 μM	SANGER
NB69	Growth Inhibition Assay				IC50=0.14436 μM	SANGER
8-MG-BA	Growth Inhibition Assay				IC50=0.15458 μM	SANGER
K5	Growth Inhibition Assay				IC50=0.16489 μM	SANGER
KINGS-1	Growth Inhibition Assay				IC50=0.16666 μM	SANGER
SF268	Growth Inhibition Assay				IC50=0.17404 μM	SANGER
PF-382	Growth Inhibition Assay				IC50=0.17678 μM	SANGER
SH-4	Growth Inhibition Assay				IC50=0.18413 μM	SANGER
NALM-6	Growth Inhibition Assay				IC50=0.19295 μM	SANGER
CP66-MEL	Growth Inhibition Assay				IC50=0.19531 μM	SANGER
697	Growth Inhibition Assay				IC50=0.19987 μM	SANGER
CP67-MEL	Growth Inhibition Assay				IC50=0.20488 μM	SANGER
DSH1	Growth Inhibition Assay				IC50=0.24001 μM	SANGER
HCE-4	Growth Inhibition Assay				IC50=0.26439 μM	SANGER
MZ2-MEL	Growth Inhibition Assay				IC50=0.28537 μM	SANGER
BL-41	Growth Inhibition Assay				IC50=0.29123 μM	SANGER
HUTU-80	Growth Inhibition Assay				IC50=0.3142 μM	SANGER
LOXIMVI	Growth Inhibition Assay				IC50=0.31503 μM	SANGER
no-10	Growth Inhibition Assay				IC50=0.31931 μM	SANGER
KARPAS-422	Growth Inhibition Assay				IC50=0.33997 μM	SANGER
SW684	Growth Inhibition Assay				IC50=0.3498 μM	SANGER
SF126	Growth Inhibition Assay				IC50=0.3541 μM	SANGER
D-263MG	Growth Inhibition Assay				IC50=0.36224 μM	SANGER
OVCAR-4	Growth Inhibition Assay				IC50=0.37433 μM	SANGER
BB49-HNC	Growth Inhibition Assay				IC50=0.38599 μM	SANGER
ONS-76	Growth Inhibition Assay				IC50=0.42951 μM	SANGER
MZ7-mel	Growth Inhibition Assay				IC50=0.47911 μM	SANGER
RCC10RGB	Growth Inhibition Assay				IC50=0.4911 μM	SANGER
BOKU	Growth Inhibition Assay				IC50=0.49133 μM	SANGER
no-11	Growth Inhibition Assay				IC50=0.50228 μM	SANGER
IST-SL2	Growth Inhibition Assay				IC50=0.50302 μM	SANGER
RKO	Growth Inhibition Assay				IC50=0.52966 μM	SANGER
HT-144	Growth Inhibition Assay				IC50=0.53609 μM	SANGER
NCI-H446	Growth Inhibition Assay				IC50=0.6276 μM	SANGER
QIMR-WIL	Growth Inhibition Assay				IC50=0.70629 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay				IC50=0.74469 μM	SANGER
EW-16	Growth Inhibition Assay				IC50=0.76178 μM	SANGER
EW-24	Growth Inhibition Assay				IC50=0.78165 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay				IC50=0.82508 μM	SANGER
TE-9	Growth Inhibition Assay				IC50=0.87532 μM	SANGER
A3-KAW	Growth Inhibition Assay				IC50=0.98452 μM	SANGER
A101D	Growth Inhibition Assay				IC50=1.03043 μM	SANGER
OCUB-M	Growth Inhibition Assay				IC50=1.04412 μM	SANGER
ES4	Growth Inhibition Assay				IC50=1.05145 μM	SANGER
TE-6	Growth Inhibition Assay				IC50=1.21226 μM	SANGER
D-502MG	Growth Inhibition Assay				IC50=1.23376 μM	SANGER
KNS-42	Growth Inhibition Assay				IC50=1.24412 μM	SANGER
SNU-C2B	Growth Inhibition Assay				IC50=1.30589 μM	SANGER
NCI-H1838	Growth Inhibition Assay				IC50=1.30733 μM	SANGER
NKM-1	Growth Inhibition Assay				IC50=1.30859 μM	SANGER
GI-1	Growth Inhibition Assay				IC50=1.3622 μM	SANGER
NB5	Growth Inhibition Assay				IC50=1.39827 μM	SANGER
CAS-1	Growth Inhibition Assay				IC50=1.40992 μM	SANGER
HCE-T	Growth Inhibition Assay				IC50=1.56714 μM	SANGER
SBC-1	Growth Inhibition Assay				IC50=1.57984 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay				IC50=1.73466 μM	SANGER
TE-5	Growth Inhibition Assay				IC50=1.79139 μM	SANGER
CAN	Growth Inhibition Assay				IC50=1.82252 μM	SANGER
SK-UT-1	Growth Inhibition Assay				IC50=2.16693 μM	SANGER
JVM-2	Growth Inhibition Assay				IC50=2.36284 μM	SANGER
LB771-HNC	Growth Inhibition Assay				IC50=2.57551 μM	SANGER
NCCIT	Growth Inhibition Assay				IC50=2.86616 μM	SANGER
NCI-H2126	Growth Inhibition Assay				IC50=2.87552 μM	SANGER
Calu-6	Growth Inhibition Assay				IC50=3.05741 μM	SANGER
SK-LMS-1	Growth Inhibition Assay				IC50=3.11886 μM	SANGER
ARH-77	Growth Inhibition Assay				IC50=3.46915 μM	SANGER
NB17	Growth Inhibition Assay				IC50=3.63847 μM	SANGER
A253	Growth Inhibition Assay				IC50=3.73246 μM	SANGER
OPM-2	Growth Inhibition Assay				IC50=4.27685 μM	SANGER
MV-4-11	Growth Inhibition Assay				IC50=4.36454 μM	SANGER
SR	Growth Inhibition Assay				IC50=4.49954 μM	SANGER
KG-1	Growth Inhibition Assay				IC50=4.60845 μM	SANGER
OCI-AML2	Growth Inhibition Assay				IC50=5.86154 μM	SANGER
D-247MG	Growth Inhibition Assay				IC50=6.12519 μM	SANGER
DJM-1	Growth Inhibition Assay				IC50=6.48558 μM	SANGER
RPMI-6666	Growth Inhibition Assay				IC50=7.27067 μM	SANGER
KARPAS-45	Growth Inhibition Assay				IC50=7.51671 μM	SANGER
LP-1	Growth Inhibition Assay				IC50=7.54782 μM	SANGER
RS4-11	Growth Inhibition Assay				IC50=7.65787 μM	SANGER
DU-4475	Growth Inhibition Assay				IC50=8.21652 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay				IC50=8.27066 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay				IC50=8.56128 μM	SANGER
SJSA-1	Growth Inhibition Assay				IC50=8.72805 μM	SANGER
MMAC-SF	Growth Inhibition Assay				IC50=8.79307 μM	SANGER
SK-NEP-1	Growth Inhibition Assay				IC50=8.89155 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay				IC50=8.96529 μM	SANGER
SKM-1	Growth Inhibition Assay				IC50=9.01734 μM	SANGER
LB2241-RCC	Growth Inhibition Assay				IC50=9.02012 μM	SANGER
SIG-M5	Growth Inhibition Assay				IC50=9.02493 μM	SANGER
EVSA-T	Growth Inhibition Assay				IC50=9.27793 μM	SANGER
GT3TKB	Growth Inhibition Assay				IC50=9.35546 μM	SANGER
NB6	Growth Inhibition Assay				IC50=9.92259 μM	SANGER
EHEB	Growth Inhibition Assay				IC50=10.0656 μM	SANGER
HEL	Growth Inhibition Assay				IC50=10.4776 μM	SANGER
ALL-PO	Growth Inhibition Assay				IC50=10.7938 μM	SANGER
TGW	Growth Inhibition Assay				IC50=11.2828 μM	SANGER
BC-3	Growth Inhibition Assay				IC50=12.1138 μM	SANGER
IA-LM	Growth Inhibition Assay				IC50=12.4445 μM	SANGER
UACC-257	Growth Inhibition Assay				IC50=12.9198 μM	SANGER
KP-N-YS	Growth Inhibition Assay				IC50=12.9283 μM	SANGER
Raji	Growth Inhibition Assay				IC50=13.7497 μM	SANGER
SF539	Growth Inhibition Assay				IC50=13.8557 μM	SANGER
DMS-153	Growth Inhibition Assay				IC50=14.0028 μM	SANGER
L-540	Growth Inhibition Assay				IC50=15.0672 μM	SANGER
MN-60	Growth Inhibition Assay				IC50=15.1979 μM	SANGER
RPMI-8866	Growth Inhibition Assay				IC50=17.4454 μM	SANGER
NCI-H510A	Growth Inhibition Assay				IC50=19.3973 μM	SANGER
NB13	Growth Inhibition Assay				IC50=19.4877 μM	SANGER
HAL-01	Growth Inhibition Assay				IC50=19.7543 μM	SANGER
NCI-H720	Growth Inhibition Assay				IC50=20.2733 μM	SANGER
REH	Growth Inhibition Assay				IC50=20.6357 μM	SANGER
KNS-81-FD	Growth Inhibition Assay				IC50=23.146 μM	SANGER
HC-1	Growth Inhibition Assay				IC50=24.5551 μM	SANGER
NCI-H2141	Growth Inhibition Assay				IC50=24.7754 μM	SANGER
MOLT-4	Growth Inhibition Assay				IC50=26.6753 μM	SANGER
OMC-1	Growth Inhibition Assay				IC50=27.1422 μM	SANGER
LC-1F	Growth Inhibition Assay				IC50=27.3245 μM	SANGER
NCI-H1304	Growth Inhibition Assay				IC50=28.1628 μM	SANGER
BC-1	Growth Inhibition Assay				IC50=28.651 μM	SANGER
NCI-H64	Growth Inhibition Assay				IC50=29.6253 μM	SANGER
MOLT-16	Growth Inhibition Assay				IC50=29.6292 μM	SANGER
U-87-MG	Growth Inhibition Assay				IC50=30.766 μM	SANGER
GAK	Growth Inhibition Assay				IC50=31.2686 μM	SANGER
ES8	Growth Inhibition Assay				IC50=32.1252 μM	SANGER
HCC1599	Growth Inhibition Assay				IC50=32.3325 μM	SANGER
EB-3	Growth Inhibition Assay				IC50=34.3117 μM	SANGER
HCC1187	Growth Inhibition Assay				IC50=35.8052 μM	SANGER
SK-PN-DW	Growth Inhibition Assay				IC50=36.1943 μM	SANGER
JVM-3	Growth Inhibition Assay				IC50=37.2338 μM	SANGER
HCC2157	Growth Inhibition Assay				IC50=37.9946 μM	SANGER
A4-Fuk	Growth Inhibition Assay				IC50=38.1009 μM	SANGER
COR-L279	Growth Inhibition Assay				IC50=40.2851 μM	SANGER
DEL	Growth Inhibition Assay				IC50=41.9086 μM	SANGER
NCI-H1395	Growth Inhibition Assay				IC50=42.0163 μM	SANGER
MHH-NB-11	Growth Inhibition Assay				IC50=43.0818 μM	SANGER
NCI-H2107	Growth Inhibition Assay				IC50=43.4846 μM	SANGER
NEC8	Growth Inhibition Assay				IC50=44.336 μM	SANGER
COLO-684	Growth Inhibition Assay				IC50=46.2258 μM	SANGER
LS-411N	Growth Inhibition Assay				IC50=48.4748 μM	SANGER
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	488.01	Formule	C₂₂H₂₆ClN₇O₂S	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	302962-49-8	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	BMS-354825			Smiles	CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO

Oplosbaarheid

In vitro
Batch:

DMSO : 98 mg/mL (200.81 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 5%Tween80 3 61%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	5.000mg/ml (10.25mM)	Taking the 1 mL working solution as an example, add 40 μL of 125 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 610 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	LCK Abl (Cell-free assay) 0.6 nM Src (Cell-free assay) 0.8 nM c-Kit (D816V) (Cell-free assay) 37 nM c-Kit (wt) (Cell-free assay) 79 nM
In vitro	Dasatinib is effectiever in het remmen van de proliferatie van Ba/F3-cellen die wild-type Bcr-Abl en Bcr-Abl-mutanten tot expressie brengen, met uitzondering van T315I. Deze verbinding heeft een twee-log (∼325-voudig) verhoogde potentie. Het remt krachtig wild-type Abl-kinase en alle mutanten behalve T315I over een smal bereik. Dit middel richt zich direct op wild-type en mutante Abl-kinase-domeinen en remt autofosforylering en substraatfosforylering op een concentratieafhankelijke manier. Het vertoont een 325-voudig grotere potentie tegen cellen die wild-type Bcr-Abl tot expressie brengen. Het percentage kolonies van TgE-beenmergcellen is gedaald van 100% in onbehandelde putjes tot 4,12% in met deze verbinding behandelde putjes. In aanwezigheid van deze chemische stof is het verschil in het percentage kolonies gevormd door WT- en TgE-beenmergcellen statistisch significant. Expressie van LMP2A is in staat om de overleving en proliferatie van B-lymfocyten te bevorderen, wat kan worden geremd door Lyn en/of c-Abl-kinases te targeten via dit middel. De behandeling remt Src-signalering, vermindert de groei en induceert celcyclusarrest en apoptose in een subgroep van schildklierkankercellen. Behandeling met toenemende doses van deze verbinding (0,019 μM tot 1,25 μM) gedurende 3 dagen remt de groei van de C643-, TPC1-, BCPAP- en SW1736-cellijnen met ongeveer 50% bij lage nanomolaire concentraties, terwijl hogere concentraties nodig zijn om de groei van de K1-cellijn te remmen. Behandeling met 10 nM of 50 nM van deze chemische stof resulteert in een toename van 9-22% van de cellen in de G1-populatie onder BCPAP-, SW1736- en K1-cellen, en een overeenkomstige afname van 7-18% in het percentage cellen in de S-fase.
Kinase Assay	Kinase-autofosforyleringsassays
Kinase Assay	Kinase-assays met wild-type en mutante glutathion-S-transferase (GST)-Abl-fusie-eiwitten (c-Abl-aminozuren 220-498) worden uitgevoerd. GST-Abl-fusie-eiwitten worden voor gebruik vrijgemaakt van glutathion-Sepharose-kralen; de ATP-concentratie is 5 μM. Onmiddellijk voor gebruik in kinase-autofosforylerings- en in vitro peptide-substraatfosforyleringsassays worden GST-Abl-kinase-domein-fusie-eiwitten behandeld met LAR-tyrosinefosfatase. Na 1 uur incubatie bij 30 °C wordt LAR-fosfatase geïnactiveerd door toevoeging van natriumvanadaat (1 mM). Immunoblot-analyse die onbehandeld GST-Abl-kinase vergelijkt met gedephosphoryleerd GST-Abl-kinase wordt routinematig uitgevoerd met behulp van fosfotyrosine-specifieke antilichaam 4G10 om volledige (>95%) defosforylering van tyrosineresiduen te bevestigen en c-Abl-antilichaam CST 2862 om gelijke belading van GST-Abl-kinase te bevestigen. Het Dasatinib-concentratiebereik wordt uitgebreid tot 1.000 nM voor mutant T315I. Dezelfde remmerconcentraties worden gebruikt voor de in vitro peptide-substraatfosforyleringsassays. De drie remmers worden getest over dezelfde concentratiebereiken tegen GST-Src-kinase en GST-Lyn-kinase.
In vivo	Dasatinib keert splenomegalie om bij LMP2A/MYC dubbel-transgene muizen. Deze verbinding voorkomt specifiek kolonieformatie door LMP2A-expresserende beenmerg-B-cellen en vermindert de miltgrootte bij de TgE-muizen. De miltmassa is significant verminderd bij met deze verbinding behandelde Tg6/λ-MYC-muizen in vergelijking met de controlegroep. Het remt lymfadenopathie bij LMP2A/MYC dubbel-transgene muizen. Deze chemische stof keert splenomegalie om bij Rag1KO-muizen die zijn geënt met tumorcellen van LMP2A/MYC dubbel-transgene muizen. De therapie remt Lyn-fosforylering in B-lymfocyt-tumoren die LMP2A tot expressie brengen.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/15930265/ [2] https://pubmed.ncbi.nlm.nih.gov/16434489/ [3] https://pubmed.ncbi.nlm.nih.gov/22609829/ [4] https://pubmed.ncbi.nlm.nih.gov/22586301/

Toepassingen

Methoden	Biomarkers	PMID
Western blot	phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 p-FAK / p-STAT3 cleaved caspase 3	23049975
Growth inhibition assay	IC50	23721490
Immunofluorescence	SRC / Met F-actin / Actinin-4 / Paxillin α-tubulin	26517812
ELISA	TNF-α E-selectin VCAM-1	17684099

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT05527418	Recruiting	Recent HIV-1 Infection	Eva Bonfill\|Institut d''Investigacions Biomèdiques August Pi i Sunyer	January 26 2024	Phase 2
NCT05993949	Recruiting	Lymphoblastic Leukemia	Stanford University\|Kite Pharma	October 2 2023	Phase 1
NCT05780073	Recruiting	HIV Infection Primary	Fundació Institut Germans Trias i Pujol\|Fundación FLS de Lucha Contra el Sida Enfermedades Infecciosas y Promoción de la Salud y Ciencia\|Spanish Clinical Research Network - SCReN\|IrsiCaixa\|University of Turin Italy\|Instituto de Salud Carlos III\|Germans Trias i Pujol Hospital	October 16 2023	Phase 2
NCT05198843	Terminated	Anatomic Stage IV Breast Cancer AJCC v8\|Metastatic Triple-Negative Breast Inflammatory Carcinoma	National Cancer Institute (NCI)	November 8 2022	Phase 1\|Phase 2
NCT04925648	Recruiting	Metastatic Prostate Cancer	St Vincent''s Hospital Sydney	October 18 2021	Phase 2

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

Als u nog andere vragen heeft, kunt u een bericht achterlaten.

Veelgestelde vragen

Vraag 1:
What’s the difference between S1021 and S7782? Which one is better for in vivo studies?

Antwoord:
Usually, hydrate will be more stable and dissolve better than free base. But it (S1021) dissolves better in DMSO than hydrate one (S7782).

Vraag 2:
Can I give it to mice by oral gavage? If so, how to dissolve this compound?

Antwoord:
Our S1021 in 1% DMSO+30% PEG 300+1% Tween 80 at 30 mg/ml is a suspension which you can administrate to mice via oral gavage. If you want a clear solution, it can be dissolved in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5 mg/ml clearly.

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