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CAS No. : 2052128-15-9
MCE 国际站:H3B-5942
产品活性: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,Ki 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 ERαWT 或者突变型 ERα 的肿瘤细胞和动物具有抗肿瘤活性。
研究领域:Vitamin D Related/Nuclear Receptor
作用靶点:Estrogen Receptor/ERR
In Vitro: 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-ERαWT, various MCF7-ERαMUT lines, and the PDX-ERαY537S/WT line.
H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERαWT, and MCF7-LTED-ERαY537C 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 ERαWT or clinically frequent ERα mutations.
In Vivo: 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 ERαY537S/WT ST941 model in athymic female nude mice.
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货号: HY-112611
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