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4-Hydroxytamoxifen (Afimoxifene) Estrogen Receptor Modulator

Name: 4-Hydroxytamoxifen (Afimoxifene)
Brand: Selleck Chemicals
SKU: S7827
Rating: 5 (31 reviews)

Kat.-Nr.S7827

4-Hydroxytamoxifen (Afimoxifene) ist der aktive Metabolit von Tamoxifen und ein selektiver estrogen receptor (ER) Modulator, der in der therapeutischen und chemopräventiven Behandlung von Brustkrebs weit verbreitet ist. Es aktiviert die On-Target-Modifikationsfrequenz für Intein-Cas9-Varianten.

4-Hydroxytamoxifen (Afimoxifene) Estrogen/progestogen Receptor Modulator Chemical Structure

Chemische Struktur

Molekulargewicht: 387.51

Springe zu

Qualitätskontrolle

Charge: Reinheit: 99.89%

99.89

Verwandte Ziele	Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Weitere Estrogen/progestogen Receptor Inhibitoren	Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Kaempferol Cholesterol G15 Endoxifen HCl Licochalcone A Chrysin Pregnenolone

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Aktivitätsbeschreibung	PMID
MCF7 cells	Proliferation assay			Inhibition of estrogen-stimulated MCF-7 cell proliferation, IC50=0.5 nM	9548817
MCF7	Function assay			Effective dose for [3H]- estradiol against proliferation of MCF-7 cells, EC50 = 0.00003 μM.	2769681
MCF7	Function assay		4 hrs	Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal dextran-treated FBS incubated for 4 hrs by SP1 and anti-ER rabbit monocolnal antibody based in-cell Western assay, Activity = 0.0001 μM.	30086626
MCF7	Function assay			Effective concentration against MCF-7 breast tumor cells using MCF-7 assay, EC50 = 0.00012 μM.	12825935
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells, IC50 = 0.0005 μM.	22405286
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells, IC50 = 0.000537 μM.	26407012
MCF	Function assay			Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response, IC50 = 0.0007943 μM.	26407012
Ishikawa endometrial cells	Function assay			Agonist activity as alkaline phosphatase induction in Ishikawa endometrial cells compared to E2, EC50 = 0.0008 μM.	15380208
MCF7	Function assay			Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells, IC50 = 0.00117 μM.	9154963
MCF7	Function assay		24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay, IC50 = 0.003 μM.	28296398
Rosetta 2 DE3	Function assay		1 hr	Displacement of [3H]-estradiol from recombinant human N-terminal His-tagged ERalpha LBD harboring C381S/C417S/C530S mutant expressed in Rosetta 2 DE3 competent cells after 1 hr by SPA binding assay, IC50 = 0.004 μM.	28296398
insect cells	Function assay			Inhibition of fluormone ES2 green binding to recombinant full length human ERalpha expressed in insect cells by fluorescence polarization assay, IC50 = 0.00629 μM.	28735214
MCF-7-2a	Function assay			Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells, IC50 = 0.007 μM.	12672249
MCF7	Antiproliferative assay		24 hrs	Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay, IC50 = 0.0085 μM.	18272256
MCF7	Function assay			Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay, IC50 = 0.0085 μM.	12825935
Ishikawa cells	Function assay		72 hrs	Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assay, IC50 = 0.01 μM.	28426931
insect cells	Function assay			Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.02 μM.	18835176
MCF7	Cytotoxicity assay		5 days	Cytotoxicity against human MCF7 cells after 5 days, IC50 = 0.0291 μM.	23864928
GT1-7	Function assay		20 to 24 hrs	Antagonist activity at estrogen receptor in mouse GT1-7 cells harboring beta-galactosidase reporter gene assessed as reduction in 17beta-estradiol induced response measured after 20 to 24 hrs by luciferase reporter gene assay, IC50 = 0.0332 μM.	28400239
insect cells	Function assay			Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.04 μM.	18835176
HEK293	Function assay		30 mins	Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis, IC50 = 0.044 μM.	19136975
HEK293	Function assay		1 hr	Antagonist activity at recombinant human ERalpha expressed in HEK293 cells assessed as inhibition of estradiol-induced YFP-fused SRC1 coactivator recruitment measured after 1 hr in presence of Coelenterazine H by BRET assay, IC50 = 0.07 μM.	30078609
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.107 μM.	18835176
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue assay, GI50 = 0.107 μM.	23735829
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against ER-dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.11 μM.	28426931
T47D	Cytotoxicity assay		5 days	Cytotoxicity against human T47D cells after 5 days, IC50 = 0.21 μM.	23864928
Ishikawa endometrial cells	Function assay			Antagonist activity as inhibition of 1 nM 17-beta-estradiol stimulated alkaline phosphatase induction in Ishikawa endometrial cells, IC50 = 0.51 μM.	15380208
CV1	Function assay		45 hrs	Inverse agonist activity at GAL4-DNA binding domain-fused mouse ERRgamma ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay, IC50 = 0.6 μM.	28189393
CV1	Function assay		45 hrs	Inverse agonist activity at GAL4-DNA binding domain-fused human ERRbeta ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay, IC50 = 0.65 μM.	28189393
HEK293	Function assay			Agonist activity at human estrogen related receptor gamma expressed in HEK293 cells by luciferase reporter gene assay, IC50 = 1.35 μM.	25305688
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50 = 1.41254 μM.	21513275
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 1.90546 μM.	21513275
HeLa	Function assay		4.5 hrs	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 1.96 μM.	29624387
MDA-MB-231	Cytotoxicity assay		4 days	Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 2.5 μM.	30078609
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells assessed as incorporation of [methyl-3H]thymidine into cellular DNA in serum free medium in in absence of 6.2 ug/mL RNase 1, IC50 = 2.7 μM.	22611478
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.79 μM.	26896706
MCF12A	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 3.23594 μM.	21513275
MCF7	Cytotoxicity assay		4 days	Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 3.3 μM.	30078609
MCF12A	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50 = 3.31131 μM.	21513275
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 3.46737 μM.	21513275
MDA-MB-231	Cytotoxicity assay		4 days	Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 3.5 μM.	30078609
MCF12A	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 3.89045 μM.	21513275
MCF7	Cytotoxicity assay		4 days	Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 3.9 μM.	30078609
MCF7	Function assay			Inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]- estradiol (E2), IC30 = 4 μM.	2769681
MCF10A	Cytotoxicity assay		4 days	Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 4 μM.	30078609
MCF10A	Cytotoxicity assay		4 days	Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 4 μM.	30078609
yeast cells	Antiestrogenic assay			Antiestrogenic activity at estrogen receptor alpha expressed in yeast cells assessed as inhibition of 17-beta-estradiol-induced beta-galactosidase activity by two hybrid assay, IC50 = 4.4 μM.	16441086
NCI-ADR-RES	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50 = 4.46684 μM.	21513275
BT-20	Function assay	10 μM		Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration, IC30 = 4.8 μM.	2769681
Calu-1	Function assay		30 mins	Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis, IC50 = 4.8 μM.	19136975
MCF7	Function assay			Antagonist activity at ERalpha receptor in human MCF7 cells, IC50 = 4.89779 μM.	26407012
MDA-MB-231	Anticancer assay		48 hrs	Anticancer against human ER-positive MDA-MB-231 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 5.4 μM.	24946145
MCF-7	Cytotoxicity assay			Cytotoxicity against MCF-7 cells in the absence of 1 uM E2 (estradiol), Cytotoxicity = 6 μM.	9089332
NCI-ADR-RES	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 6.16595 μM.	21513275
AU565	Anticancer assay		48 hrs	Anticancer against human ER-negative AU565 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.2 μM.	24946145
MCF7L	Anticancer assay		48 hrs	Anticancer against human ER-positive MCF7L cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.3 μM.	24946145
SKOV3-MDR1-M6/6	Anticancer assay		48 hrs	Anticancer against human SKOV3-MDR1-M6/6 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.49 μM.	24946145
MCF7	Antiproliferative assay		24 hrs	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 7.2 μM.	24189055
SKOV3	Anticancer assay		48 hrs	Anticancer against human SKOV3 cells overexpressing P-gp assessed as cell viability after 48 hrs by SRB assay, IC50 = 7.46 μM.	24946145
PC3	Antiproliferative assay		48 hrs	Antiproliferative activity against androgen receptor-deficient human PC3 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50 = 7.58578 μM.	21513275
NCI-ADR-RES	Antiproliferative assay		48 hrs	Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 7.76247 μM.	21513275
MCF-7	Cytotoxicity assay			Cytostaticity against MCF-7 cells in the presence of 1 uMolar E2 (estradiol), IC50 = 8 μM.	9089332
LNCAP	Antiproliferative assay		48 hrs	Antiproliferative activity against human LNCAP cells expressing androgen receptor incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50 = 8.31764 μM.	21513275
MCF7	Antiproliferative assay		5 days	Antiproliferative activity against human MCF7 cells after 5 days by WST-8 assay, IC50 = 8.9 μM.	25614118
MCF7	Anticancer assay		48 hrs	Anticancer against human ER-positive MCF7 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 9.2 μM.	24946145
MCF-7	Cytotoxicity assay			Cytotoxicity against MCF-7 cells in presence of 1 uM E2 (estradiol), Cytotoxicity = 9.4 μM.	9089332
MDA-MB-231	Antiproliferative assay		24 hrs	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 10.4 μM.	24189055
MDA-MB-453	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by MTT assay, IC50 = 10.4 μM.	28506582
DU145	Antiproliferative assay		48 hrs	Antiproliferative activity against androgen receptor-deficient human DU145 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50 = 10.7152 μM.	21513275
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 13.6 μM.	25618595
Vero	Antiproliferative assay		72 hrs	Antiproliferative activity against african green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.1 μM.	25993269
DU145	Antiproliferative assay		72 hrs	Antiproliferative activity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.3 μM.	25993269
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 15.6 μM.	28506582
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.6 μM.	25993269
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 20.1 μM.	28506582
MCF7	Antiproliferative assay	0.625 nM	24 hrs	Antiproliferative activity against human MCF7 cells at 0.625 nM after 24 hrs by MTS assay	18272256
MCF7	Antiproliferative assay	0.625 to 10 nM	24 hrs	Antiproliferative activity against human MCF7 cells at >0.625 to 10 nM after 24 hrs by MTS assay	18272256
MCF7:WS8	Function assay			Activation of human ER in human MCF7:WS8 cells expressing estrogen responsive element by luciferase reporter gene assay	20334368
MCF7:WS8	Antiestrogenic assay	1 uM	7 days	Antiestrogenic activity in human ERalpha expressing MCF7:WS8 cells assessed as inhibition of estradiol-induced proliferation at 1 uM after 7 days	20334368
MCF7	Antiestrogenic assay			Antiestrogenic activity in human MCF7 cells assessed as inhibition of estradiol-stimulated prolactin gene expression	20334368
MCF7	Antiestrogenic assay			Antiestrogenic activity in human MCF7 cells assessed as inhibition of estradiol-stimulated proliferation	20334368
T47D:C:4:2	Function assay			Estrogenic activity at wild type ER alpha expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay	20334368
MDA-MB-231	Cytotoxicity assay		3 days	Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay	20598555
T47D:C:4:2	Function assay			Estrogenic activity at wild type ER alpha D351G mutant expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay	20334368
MCF7	Function assay	1 μM	6 days	Drug uptake in human MCF7 cells at 10'-6 M after 6 days by HPLC-MS/MS analysis	23864928
MCF7	Function assay	10 uM	6 hrs	Upregulation of ERalpha protein levels in human MCF7 cells at 10 uM after 6 hrs by Western blot method	24332630
MCF7:WS8	Function assay	1 μM	48 hrs	Agonist activity at ER in human MCF7:WS8 cells assessed as pS2 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis	24805199
MCF7:WS8	Function assay	1 μM	48 hrs	Agonist activity at ER in human MCF7:WS8 cells assessed as GREB1 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis	24805199
GH3	Function assay	1 μM	48 hrs	Antagonist activity at ER in rat GH3 cells assessed as inhibition of estradiol-induced prolactin gene expression at 10'-6 M after 48 hrs by RT-PCR analysis	24805199
GH3	Function assay	0.1 nM to 1 μM	48 hrs	Antagonist activity at ER in rat GH3 cells assessed as inhibition of estradiol-induced prolactin gene expression at 10'-10 to 10'-6 M after 48 hrs by RT-PCR analysis	24805199
MCF7	Anticancer assay	250 to 500 nM	5 days	Anticancer against human ER-positive MCF7 cells assessed as inhibition of estradiol-induced cell proliferation at 250 to 500 nM after 5 days	24946145
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYC mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of TFF1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of GREB1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYBL2 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CCND1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CDC6 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of E2F1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
MCF7	Function assay	5 uM	24 hrs	Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MKI67 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis	30078609
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht	387.51	Formel	C₂₆H₂₉NO₂	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	68392-35-8	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	Afimoxifene			Smiles	CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3

Löslichkeit

In vitro
Charge:

DMSO : 77 mg/mL (198.7 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 390 mg/mL (1006.42 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 78 mg/mL (201.28 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL (51.61 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 77 mg/mL (198.7 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.
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.	7.500mg/ml (19.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 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 clarify; 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.
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.	4.000mg/ml (10.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 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 clarify; 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.
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 Corn oil Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	8.000mg/ml (20.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 160 mg/ml clear DMSO stock solution to 950 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.

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

In vitro	4-OHT ist ein potenter Aktivator von ER und hat eine höhere Affinität zu Estrogenrezeptoren gezeigt. Es hat signifikante dosis- und zeitabhängige direkte Effekte, um die kontraktile Funktion isolierter adulter Rattenkardiomyozyten zu verändern. 4-HT aktiviert die On-Target-Modifikationsfrequenz für Intein-Cas9-Varianten .
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/24205315/ [2] https://pubmed.ncbi.nlm.nih.gov/10190564/ [3] https://pubmed.ncbi.nlm.nih.gov/25848930/

Anwendungen

Methoden	Biomarker	Bilder	PMID
Western blot	p-ERK / ERK / p-MEK / MEK1 / MEK2 / p21 / Cyclin D1		26163823
Growth inhibition assay	Cell viability		26014809

Klinische Studieninformationen

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

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
NCT05133674	Unknown status	Breast Cancer\|Breast Carcinoma\|Breast Tumors\|Cancer of Breast\|Malignant Neoplasm of Breast	Karolinska University Hospital	April 4 2022	Phase 2

Technischer Support

Handhabungshinweise

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

Wenn Sie weitere Fragen haben, hinterlassen Sie bitte eine Nachricht.

Häufig gestellte Fragen

Frage 1:
It has two configurations, E and Z. Which one does selleck provide?

Antwort:
According to the literature, its configuration does not affect biological activity. S7827 is a mixture of E and Z configurations, of which the Z form accounts for more than 70%.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):