Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : H3B-5942
CAS No.: 2052128-15-9
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $148 | In stock | |
| 10 mg | $228 | In stock | |
| 25 mg | $388 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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).
| M.Wt | 494.639 | |
| Formula | C31H34N4O2 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| 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.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
