Chemical Structure : H3B-5942
CAS No.: 2052128-15-9
货号: PC-35365Not For Human Use, Lab Use Only.
H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA) with Ki 1 nM and 0.41 nM for wild-type and mutant ERα Y537S respectively, covalently targeting Cys530.
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5 mg | ¥1480 | In stock | |
10 mg | ¥2280 | In stock | |
25 mg | ¥3880 | In stock | |
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100 mg | Get quote |
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H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA) with Ki 1 nM and 0.41 nM for wild-type and mutant ERα Y537S respectively, covalently targeting Cys530.
H3B-5942 demonstrates potent ERα antagonist activity in vitro and in vivo.
H3B-5942 covalently inactivates both wild-type and mutant ERα by targeting Cys530 and enforcing a unique antagonist conformation.
H3B-5942 demonstrates significant single-agent antitumor activity in xenograft models representing ERαWT and ERα Y537S breast cancer, which is superior to fulvestrant (Cat# PC-21622).
分子量 | 494.639 | |
分子式 | C31H34N4O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(E)-4-((2-(4-((E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)phenoxy)ethyl)amino)-N,N-dimethylbut-2-enamide |
1. Puyang X, et al. Cancer Discov. 2018 Jul 10. pii: CD-17-1229.
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