H3B-5942 ( H3B5942 )

Catalog No. M13184 CAS No. 2052128-15-9

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Product Name

H3B-5942
Note

Research use only, not for human use.
Brief Description

H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo.
Description

H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo; covalently inactivates both wild-type and mutant ERα by targeting Cys530 and enforcing a unique antagonist conformation; demonstrated significant single-agent antitumor activity in xenograft models representing ERαWT and ERα Y537S breast cancer that was superior to fulvestrant.
Synonyms

H3B5942
Pathway

Endocrinology/Hormones
Target

Estrogen Receptor/ERR
Recptor

Estrogen Receptor/ERR
Research Area

——
Indication

——

CAS Number

2052128-15-9
Formula Weight

494.64
Molecular Formula

C31H34N4O2
Purity

>98% (HPLC)
Solubility

——
SMILES

CCC(=C(C1=CC=C(C=C1)OCCNCC=CC(=O)N(C)C)C2=CC3=C(C=C2)NN=C3)C4=CC=CC=C4
Chemical Name

(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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