aladdin 阿拉丁 S414427 SAR439859 2114339-57-8 98%

中文名：SAR439859

英文名：SAR439859

纯度：≥98%

货号：S414427

Cas号：2114339-57-8

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

SAR439859 (compound 43d) is an orally available and nonsteroidal selectiveestrogen receptordegrader (SERD) with potential antineoplastic activity. SAR439859 is a potentestrogen receptor (ER)antagonist with EC50 of 0.2 nM for ERα degradation.

Targets

ERα (Cell-free assay) 0.2 nM(EC50)

In vitro

SAR439859 is a novel, orally bioavailable SERD with potent antagonist and degradation activities against both wild-type and mutant Y537S ER. Driven by its fluoropropyl pyrrolidinyl side chain, SAR439859 has demonstrated broader and superior ER antagonist and degrader activities across a large panel of ER+ cells, including inhibition of ER signaling and tumor cell growth.

In vivo

SAR439859 shows promising antitumor activity in breast cancer mice xenograft models. In vivo treatment with SAR439859 demonstrates significant tumor regression in ER+ breast cancer models, including MCF7-ESR1 wild-type and mutant-Y537S mouse tumors, and HCI013, a patient-derived tamoxifen-resistant xenograft tumor.

Cell Research(from reference)

Cell lines：LCC2 cells, MCF7 cells 

Concentrations：0.01-1000 nM 

Incubation Time：7 days, 4 hours 

查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/S414427.html