H3B-5942 是一种选择性、不可逆、可口服的 estrogen receptor 共价拮抗剂，能够靶作用于 Cys530，使野生型和突变型 ERα 失活，K_i 值分别为 1 nM 和 0.41 nM。H3B-5942 能够减少 ERα 的目标基因 GREB1 的表达。H3B-5942 具有抗癌作用，对含有 ERα^WT 或者突变型 ERα 的肿瘤细胞和动物具有抗肿瘤活性。

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with K i s 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 ERα or ERα mutations.

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ERα 0.41 nM (Ki) ERα 1 nM (Ki)

H3B-5942 is a selective and irreversible 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 elevates ERα protein level distinct from SERMs/SERD, blocks ERα-dependent transcription in breast cancer cells. H3B-5942 (0.01-10 μM) reduces ERα target gene GREB1 in MCF7-ERα, various MCF7-ERαMUT lines, and the PDX-ERα/WT line.
H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERα, and MCF7-LTED-ERα lines with GI50s of 0.5, 2, and 30 nM, respectively. H3B-5942 (10-25 nM) in combination with CDK4/6 inhibitors (≥25 pM) has synergic inhibitory effect on multiple cell lines bearing ERα or clinically frequent ERα mutations. has not independently confirmed the accuracy of these

H3B-5942 (1, 3, 10, or 30 mg/kg, p.o, q.d. for 17 days) dose-dependently inhibits tumor growth in MCF7 xenograft model in athymic female nude mice.
H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERα ST941 model in athymic female nude mice. has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.

In Vitro: DMSO : 83.33 mg/mL (168.47 mM; Need ultrasonic)配制储备液