THIQ 40 | ERα inhibitor | Probechem Biochemicals

Chemical Structure : THIQ 40

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THIQ 40 (THIQ40)

货号: PC-35861Not For Human Use, Lab Use Only.

THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation).

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100 mg		Get quote

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生物&药学活性

THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation).
THIQ 40 potently inhibits insulin driven proliferation in MCF-7 cells with IC50 of 2.1 nM, downregulate ERα protein levels and inhibit MCF-7 proliferation in an estradiol-independent manner.
THIQ 40 demonstrated SERD activity at tolerated and efficacious exposures in vivo.

物理化学性质&存储条件

分子量	427.544
分子式	C28H29NO3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-3-(4-(6-Hydroxy-2-(4-isopropylphenyl)-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)phenyl)acrylic Acid

参考文献

1. Burks HE, et al. J Med Chem. 2017 Apr 13;60(7):2790-2818.

THIQ 40 (THIQ40)

生物&药学活性

物理化学性质&存储条件

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THIQ 40 (THIQ40)

生物&药学活性

物理化学性质&存储条件

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