化合物 T11530L T11530L
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
50 mg | 2052130-80-8 | ¥14,900.00 | 询底价 |
25 mg | 2052130-80-8 | ¥11,400.00 | 询底价 |
100 mg | 2052130-80-8 | ¥23,500.00 | 询底价 |
5 mg | 2052130-80-8 | ¥2,890.00 | 询底价 |
2 mg | 2052130-80-8 | ¥2,570.00 | 询底价 |
1 mL | 2052130-80-8 | ¥3,950.00 | 询底价 |
Product Introduction
Bioactivity
英文名: H3B-6545
描述: H3B-6545 is an oral and selective antagonist of estrogen receptor covalent (SERCA).
体外活性: H3B-6545 inhibits ERαWT activity and growth of ERαWT -positive breast cancer lines and it also effectively inhibits ERαWT activity and suppresses proliferation of ERαWT -positive breast cancer lines (GI50s: 0.3-0.4, 1.0, 0.5, 5.2, and 0.2 nM for MCF7, HCC1428, BT483, T47D, and CAMA-1 cell lines). H3B-6545 is a first-in-class selective ER covalent antagonist (SERCA). H3B-6545 is a highly selective small molecule. In biochemical and cell-based assays, it also effectively antagonizes wild-type and mutant ERα. In vitro comparisons with the standard of care and other experimental agents confirm, increased cell potency of H3B-6545 under continuous as well as washout treatment conditions [1]. H3B-6545, a member of a novel class of ERα antagonists refers to as selective ER covalent antagonist (SERCA), which inactivates both wild-type and mutant ERα by targeting C530 and enforcing a unique antagonist conformation [1].
体内活性: H3B-6545 is well tolerated across a broad dose range and at exposures that significantly exceed those required for efficacy in mouse xenograft models. H3B-6545 (once daily; p.o.) treatment, displays effective activity and superior efficacy to fulvestrant in the MCF-7 xenograft model with maximal antitumor activity at doses >10x below the maximum tolerated dose in mice. H3B-6545 displays superior antitumor activity to Tamoxifen and Fulvestrant in patient-derived xenograft models of estrogen receptor-positive breast cancer including models carrying ERα mutations in rats and monkeys [1].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: H3B-6545 | H3B6545 | H3B 6545 | H-3B-6545
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途