H3B-5942 |
Catalog No.GC33262 |
H3B-5942는 선택적이고 비가역적이며 경구 활성인 에스트로겐 수용체 공유 길항제이며, 각각 1nM 및 0.41nM의 Kis로 Cys530을 표적화하여 야생형 및 돌연변이 ERα를 모두 비활성화합니다. H3B-5942는 ERα 표적 유전자 GREB1을 감소시키고 다중 세포주 또는 ERαWT 또는 ERα 돌연변이가 있는 동물 모두에서 강력한 항종양 활성을 나타냅니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2052128-15-9
Sample solution is provided at 25 µL, 10mM.
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].
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[1].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[1]. 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[1].
H3B-5942 (1, 3, 10, or 30 mg/kg, p.o, q.d.) 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[1].
[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.
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