Product Description: H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations[1].
Applications: Neuroscience-Neuromodulation
Formula: C31H34N4O2
References: [1]Puyang X, et al. Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer. Cancer Discov. 2018 Sep;8(9):1176-1193.
CAS Number: 2052128-15-9
Molecular Weight: 494.63
Compound Purity: 99.73
Research Area: Cancer
Solubility: DMSO : 83.33 mg/mL (ultrasonic)
Target: Estrogen Receptor/ERR