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H3B-5942

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.

Product Specifications

CAS Number

2052128-15-9

Product Name Alternative

H3B5942

Purity

>98% (HPLC)

Solubility

In Vitro: DMSO : 83.33 mg/mL (168.47 mM)

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

Molecular Formula

C31H34N4O2

Molecular Weight

494.639

Storage Conditions

Storage temperature: -20°C. Stability: ≥ 2 years

Notes

For research use only.

Other Product Names

(E) -4- ((2- (4- ((E) -1- (1H-indazol-5-yl) -2-phenylbut-1-en-1-yl) phenoxy) ethyl) amino) -N, N-dimethylbut-2-enamide

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