H3B-5942 |
رقم الكتالوجGC33262 |
H3B-5942 هو مضاد تساهمي لمستقبلات هرمون الاستروجين انتقائي ، لا رجعة فيه ونشط عن طريق الفم ، يعمل على تعطيل كل من ERα من النوع البري والمتحور من خلال استهداف Cys530 ، مع Kis من 1 نانومتر و 0.41 نانومتر ، على التوالييقلل H3B-5942 من جين ERα المستهدف GREB1 ، ويظهر نشاطًا قويًا مضادًا للورم في كل من خطوط الخلايا المتعددة أو الحيوانات التي تحمل طفرات ERαWT أو ERα
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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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