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Irinotecan Hydrochloride Trihydrate Topoisomerase I Inhibitor

Name: Irinotecan Hydrochloride Trihydrate
Brand: Selleck Chemicals
SKU: S2217
Rating: 5 (90 reviews)

Kat.-Nr.S2217

Irinotecan HCl Trihydrate ist ein Hydrochlorid-Trihydrat von Irinotecan (Camptosar, Campto, CPT-11), einem Topoisomerase I-Inhibitor mit einer IC50 von 15,8 bzw. 5,17 μM für LoVo-Zellen und HT-29-Zellen.

Irinotecan Hydrochloride Trihydrate Topoisomerase Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 677.18

Springe zu

Qualitätskontrolle

Charge: Reinheit: 99.97%

99.97

Verwandte Ziele	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Weitere Topoisomerase Inhibitoren	Camptothecin (CPT) Betulinic acid Beta-Lapachone (S)-10-Hydroxycamptothecin Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Cu(II)-Elesclomol Hydroxy Camptothecine Rubitecan

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Aktivitätsbeschreibung	PMID
RPMI8402	Cytotoxicity assay		4 days	Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment. IC50=0.57 μM	12747798
Hep3B	Antiproliferative assay		72 hrs	Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 μM.	19796956
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay, GI50 = 5.94 μM.	19796956
NCI60	Growth inhibition assay			Growth inhibition of human NCI60 cells by SBR assay, GI50 = 14.1254 μM.	21035334
Hep3B	Growth inhibition assay		72 hrs	Growth inhibition of human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 μM.	22079254
HepG2	Growth inhibition assay		72 hrs	Growth inhibition of human HepG2 cells after 72 hrs by XTT assay, GI50 = 5.94 μM.	22079254
MDA-MB-231	Growth inhibition assay		72 hrs	Growth inhibition of human MDA-MB-231 cells after 72 hrs by XTT assay, GI50 = 9.17 μM.	22079254
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay, GI50 = 5 μM.	22867019
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTT assay, GI50 = 7.1 μM.	22867019
MDA-MB-435	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay, GI50 = 12.2 μM.	22867019
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs, GI50 = 1.9 μM.	25420175
A549	Antitumor assay		4 hrs	Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50 = 6.528 μM.	18207748
LOVO	Antitumor assay		4 hrs	Antitumor activity against human LOVO cells after 4 hrs by MTT assay, IC50 = 9.015 μM.	18207748
MCF7	Antitumor assay		4 hrs	Antitumor activity against human MCF7 cells after 4 hrs by MTT assay, IC50 = 17.403 μM.	18207748
LS174T	Cytotoxicity assay		96 hrs	Cytotoxicity against human LS174T cells after 96 hrs by MTT assay, IC50 = 1.16 μM.	18513976
KB3-1	Cytotoxicity assay			Cytotoxicity against human KB3-1 cells by MTT method, IC50 = 0.68 μM.	18771930
KBH5.0	Cytotoxicity assay			Cytotoxicity against human KBH5.0 cells by MTT method, IC50 = 7.4 μM.	18771930
KBV1	Cytotoxicity assay			Cytotoxicity against human KBV1 cells by MTT method, IC50 = 40 μM.	18771930
MDA-MB-435	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50 = 1.14 μM.	20371183
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 4.61 μM.	20371183
LoVo	Cytotoxicity assay		72 hrs	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50 = 4.99 μM.	20371183
A549	Cytotoxicity assay		3 days	Cytotoxicity against human A549 cells after 3 days by MTT assay, IC50 = 6.4 μM.	20942490
LoVo	Cytotoxicity assay		3 days	Cytotoxicity against human LoVo cells after 3 days by MTT assay, IC50 = 8.8 μM.	20942490
MDA-MB-435	Cytotoxicity assay		3 days	Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay, IC50 = 17 μM.	20942490
A375	Cytotoxicity assay		72 hrs	Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50 = 0.004 μM.	21341674
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay, IC50 = 0.004 μM.	21341674
LNCAP	Cytotoxicity assay		72 hrs	Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50 = 0.009 μM.	21341674
MESSA	Cytotoxicity assay		72 hrs	Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay, IC50 = 0.01 μM.	21341674
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay, IC50 = 0.015 μM.	21341674
H69	Cytotoxicity assay		72 hrs	Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay, IC50 = 0.022 μM.	21341674
MES-SA/Dx5	Cytotoxicity assay		72 hrs	Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50 = 0.022 μM.	21341674
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA, IC50 = 0.027 μM.	21341674
IGROV1	Cytotoxicity assay		72 hrs	Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay, IC50 = 0.03 μM.	21341674
SK-MEL-2	Cytotoxicity assay		72 hrs	Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay, IC50 = 0.1 μM.	21341674
MALME-3M	Cytotoxicity assay		72 hrs	Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay, IC50 = 0.2 μM.	21341674
DU145	Cytotoxicity assay		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay, IC50 = 0.2 μM.	21341674
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay, IC50 = 0.22 μM.	21341674
H69AR	Cytotoxicity assay		72 hrs	Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50 = 0.25 μM.	21341674
DU145	Cytotoxicity assay			Cytotoxicity against human DU145 cells by SRB assay, IC50 = 9.3 μM.	23102893
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells by SRB assay, IC50 = 9.48 μM.	23102893
KB	Cytotoxicity assay			Cytotoxicity against human KB cells by SRB assay, IC50 = 9.83 μM.	23102893
HEK293	Inhibition of human		1.5 mins	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis, IC50 = 2.1 μM.	23241029
HEK293	Inhibition of human		3 mins	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 2.7 μM.	23241029
MDCK2	Inhibition of human		5 mins	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50 = 4.3 μM.	23241029
HEK293	Inhibition of human	up to 500 uM	1.5 mins	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay, IC50 = 7.9 μM.	23241029
HEK293	Inhibition of human		1.5 mins	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50 = 7.9 μM.	23241029
HEK293	Inhibition of human		3 mins	Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 20.8 μM.	23241029
H3347	Cytotoxicity assay		72 hrs	Cytotoxicity against human H3347 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay, IC50 = 7.53 μM.	24583355
DLD1	Cytotoxicity assay		72 hrs	Cytotoxicity against human DLD1 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay, IC50 = 25.1 μM.	24583355
DU145	Cytotoxicity assay		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by SRB assay, IC50 = 9.3 μM.	25003995
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 9.5 μM.	25003995
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 9.8 μM.	25003995
MDA-MB-435	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50 = 6.3 μM.	26226379
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 18.6 μM.	26226379
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 20.1 μM.	26226379
HCT116	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by SRB assay, IC50 = 2 μM.	26595875
RKO	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human RKO cells after 24 to 72 hrs by SRB assay, IC50 = 6.2 μM.	26595875
HCT15	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human HCT15 cells after 24 to 72 hrs by SRB assay, IC50 = 8.5 μM.	26595875
SW480	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human SW480 cells after 24 to 72 hrs by SRB assay, IC50 = 12.3 μM.	26595875
PC3	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC3 cells assessed as cellular DNA content after 72 hrs by CyQUANT NF fluorescence assay, IC50 = 0.8 μM.	26731300
MCF7	Antiproliferative assay		96 hrs	Antiproliferative activity against human MCF7 cells assessed as cellular DNA content after 96 hrs by CyQUANT NF fluorescence assay, IC50 = 0.9 μM.	26731300
T84	Antiproliferative assay		96 hrs	Antiproliferative activity against human T84 cells assessed as cellular DNA content after 96 hrs by CyQUANT NF fluorescence assay, IC50 = 1.2 μM.	26731300
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells assessed as cellular DNA content after 72 hrs by CyQUANT NF fluorescence assay, IC50 = 1.9 μM.	26731300
MCF7	Cytotoxicity assay		24 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.5 μM.	26841168
A549	Cytotoxicity assay		24 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.8 μM.	26841168
HepG2	Cytotoxicity assay		24 hrs	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.9 μM.	26841168
SW480	Cytotoxicity assay		24 hrs	Cytotoxicity against human SW480 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 1.4 μM.	26841168
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B colorimetric assay, IC50 = 9.48 μM.	26994847
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B colorimetric assay, IC50 = 9.828 μM.	26994847
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay, IC50 = 7.99 μM.	28285912
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay, IC50 = 8.3 μM.	28285912
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay, IC50 = 11.3 μM.	28285912
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay, IC50 = 15.6 μM.	28285912
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.3 μM.	28351590
ZR-7530	Antiproliferative assay		72 hrs	Antiproliferative activity against human ZR-7530 cells after 72 hrs by MTT assay, IC50 = 18 μM.	28351590
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 20 μM.	28351590
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 7.99 μM.	28789891
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 8.31 μM.	28789891
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 11.32 μM.	28789891
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50 = 15.56 μM.	28789891
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 7.99 μM.	28927790
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 8.3 μM.	28927790
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 11.3 μM.	28927790
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50 = 15.6 μM.	28927790
Maver2	Antiproliferative assay		72 hrs	Antiproliferative activity against human Maver2 cells after 72 hrs by MTT assay, IC50 = 0.74 μM.	29150335
NB4	Antiproliferative assay		72 hrs	Antiproliferative activity against human NB4 cells after 72 hrs by MTT assay, IC50 = 1 μM.	29150335
Capan1	Antiproliferative assay		72 hrs	Antiproliferative activity against human Capan1 cells after 72 hrs by SRB assay, IC50 = 1.5 μM.	29150335
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay, IC50 = 2.4 μM.	29150335
DU145	Antiproliferative assay		72 hrs	Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay, IC50 = 2.8 μM.	29150335
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay, IC50 = 3.8 μM.	29150335
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay, IC50 = 4 μM.	29150335
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells after 72 hrs by SRB assay, IC50 = 4.1 μM.	29150335
U2932	Antiproliferative assay		72 hrs	Antiproliferative activity against human U2932 cells after 72 hrs by MTT assay, IC50 = 4.4 μM.	29150335
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay, IC50 = 4.8 μM.	29150335
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay, IC50 = 5.8 μM.	29150335
MM487	Antiproliferative assay	10 uM	72 hrs	Antiproliferative activity against human MM487 cells at 10 uM after 72 hrs by MTT assay relative to control, IC50 = 9.4 μM.	29150335
MM432	Antiproliferative assay	10 uM	72 hrs	Antiproliferative activity against human MM432 cells at 10 uM after 72 hrs by MTT assay relative to control, IC50 = 10 μM.	29150335
A2780/DX	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780/DX cells after 72 hrs by SRB assay, IC50 = 20.1 μM.	29150335
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 1.63347 μM.	30115492
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay, IC50 = 1.88093 μM.	30115492
colon cancer cells	Cytotoxicity assay			Compound was tested in vitro for cytotoxicity against HCT116, human colon cancer cells (taxol-resistant) at a drug concentration producing 50% inhibition of colony formation, ID50 = 0.54 μM.	11965362
SW620	Antitumor assay	12.5 mg/kg		Antitumor activity against human SW620 cells xenografted in nude SCID mouse assessed as delay in tumor growth at 12.5 mg/kg, ip	22111927
HT-29	Antitumor assay	60 mg/kg	2 days	Antitumor activity against human HT-29 cells xenografted in nude mouse assessed as tumor growth inhibition at 60 mg/kg, iv tid administered 2 days measured on day 20	23360284
BT-483	Function assay	1 uM	24 hrs	Induction of DNA damage in human BT-483 cells assessed as gamma H2AX phosphorylation at Ser139 at 1 uM after 24 hrs by Western blot analysis	23419737
HCT116	Antitumor assay	30 mg/kg	6 days	Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as survival at 30 mg/kg,iv qd administered for 6 days	24583355
H3347	Antitumor assay	30 mg/kg	6 days	Antitumor activity against human H3347 cells xenografted in nude mouse assessed as survival at 30 mg/kg,iv qd administered for 6 days	24583355
HCT116	Antitumor assay	100 mg/kg		Antitumor activity against human HCT116 cells xenografted in nu/nu mouse assessed as tumor regression at 100 mg/kg, iv dosed once every week	25003995
NCI-H526	Antitumor assay	30 mg/kg		Antitumor activity against human NCI-H526 cells xenografted in athymic nude mouse at 30 mg/kg, iv qd administered 5 times for every 2 days	28064078
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 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
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) 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
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht	677.18	Formel	C₃₃H₃₈N₄O₆.HCl.3H₂O	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	136572-09-3	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	CPT-11 HCl Trihydrate			Smiles	CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl

Löslichkeit

In vitro
Charge:

DMSO : 100 mg/mL (147.67 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (147.67 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

DMSO : 187.5 mg/mL (276.88 mM) Mit 50°C Wasserbad erwärmt; Ultraschallbehandelt;
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (147.67 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 12 mg/mL

Water : 1 mg/mL

DMSO : 100 mg/mL (147.67 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
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	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	5.000mg/ml (7.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	2%DMSO 1 98%Corn oil Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	0.200mg/ml (0.30mM)	Taking the 1 mL working solution as an example, add 20 μL of 10 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. 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-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Merkmale	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets/IC₅₀/Ki	Topo I
In vitro	Irinotecan wird durch Carboxylesterasen zu SN-38 aktiviert, um mit seinem Target, Topoisomerase I, interagieren zu können. Irinotecan induziert ähnliche Mengen an spaltbaren Komplexen bei seiner IC50 in LoVo-Zellen und HT-29-Zelllinien. SN-38 induziert eine konzentrationsabhängige Bildung von spaltbaren Komplexen, die sich in LoVo-Zellen und HT-29-Zelllinien nicht signifikant unterscheidet. Die Zellakkumulation von Irinotecan ist deutlich unterschiedlich und erreicht in HT-29-Zellen durchweg höhere Werte als in LoVo-Zellen. Der Lacton-E-Ring von Irinotecan und SN-38 hydrolysiert reversibel in wässrigen Lösungen, und die Umwandlung zwischen den Lacton- und Carboxylatformen ist pH- und temperaturabhängig. Die Leber ist hauptsächlich für die Aktivierung von Irinotecan zu SN-38 verantwortlich. Bei gleichen Konzentrationen von Irinotecan und SN-38-Glucuronid ist die Rate der Beta-Glucuronidase-vermittelten SN-38-Produktion sowohl in Tumor- als auch in Normalgewebe höher als die aus Irinotecan gebildete. Irinotecan wird auch in Darm, Plasma und Tumorgewebe zu SN-38 umgewandelt. Irinotecan ist in SCLC-Zelllinien signifikant aktiver als in NSCLC-Zelllinien, während mit SN-38 kein signifikanter Unterschied zwischen histologischen Typen beobachtet wird.
In vivo	In COLO 320-Xenografts induziert Irinotecan eine maximale Wachstumshemmung von 92 %. Eine Einzeldosis von Irinotecan erhöht signifikant die Mengen an Topoisomerase I, die kovalent an DNA in Magen, Zwölffingerdarm, Dickdarm und Leber gebunden sind. Gleichzeitig zeigt die mit Irinotecan behandelte Gruppe signifikant höhere Mengen an DNA-Strangbrüchen in Dickdarmmukosazellen im Vergleich zur Kontrollgruppe.
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/11914913/ [2] https://pubmed.ncbi.nlm.nih.gov/16842384/ [3] https://pubmed.ncbi.nlm.nih.gov/15182436/ [4] https://pubmed.ncbi.nlm.nih.gov/9649129/ [5] https://pubmed.ncbi.nlm.nih.gov/9033637/ [6] https://pubmed.ncbi.nlm.nih.gov/21046105/ [7] https://pubmed.ncbi.nlm.nih.gov/16317751/

Anwendungen

Methoden	Biomarker	PMID
Western blot	TopI / pAKT / pMEK / pERK / p-p38 MAPK / pJNK2 NFκB p65 / phospho-NFκB p65 / NFκB p50 / IκBα / p27Kip1 AMPK / p-AMPK / mTOR / p-mTOR / p70S6K / p-p70S6K	29237470
Immunofluorescence	NFκB	22206574
Growth inhibition assay	Cell viability	25973791

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
NCT05854498	Recruiting	Metastatic Colorectal Cancer	University of Wisconsin Madison\|Ipsen	October 13 2023	Phase 2
NCT05732129	Not yet recruiting	Homologous Recombination Deficiency Alterations Metastatic Colorectal Cancer	Fudan University	March 1 2023	Phase 2
NCT05731518	Recruiting	Small Cell Lung Cancer	Biocity Biopharmaceutics Co. Ltd.	February 23 2023	Phase 1\|Phase 2
NCT06003998	Recruiting	Colorectal Cancer\|Peritoneal Metastases	Catharina Ziekenhuis Eindhoven	December 27 2022	Phase 2
NCT05277766	Recruiting	Peritoneal Carcinomatosis\|Peritoneal Metastases\|Colorectal Cancer\|Small Bowel Cancer\|Appendix Cancer\|Gastric Cancer\|Pancreatic Cancer\|Bile Duct Cancer	University Hospital Ghent\|Kom Op Tegen Kanker\|University Ghent	November 21 2022	Phase 1
NCT05379790	Recruiting	Gastric Cancer\|Peritoneal Metastases	Erasmus Medical Center	May 25 2022	Phase 1

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