化合物简介
Brilanestrant (INN) (developmental code names GDC-0810, ARN-810, RG-6046, RO-7056118) is a non-steroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Aragon Pharmaceuticals and is under development by Genentech for the treatment of locally advanced or metastatic estrogen receptor (ER)-positive breast cancer. As of September 2016, it is in phase II clinical trials for this indication. Similarly to tamoxifen, a SERM, brilanestrant shows some capacity to activate the ER in certain contexts and possesses weak estrogenic activity in the rat uterus, and unlike fulvestrant, which is currently the only SERD to have been marketed, brilanestrant is not a steroid and is orally bioavailable and does not need to be administered by intramuscular injection. Brilanestrant has been found to be active in tamoxifen- and fulvestrant-resistant in vitro models of human breast cancer. Side effects observed in clinical studies of brilanestrant thus far have included diarrhea, nausea, and fatigue of mostly mild-to-moderate severity.
基本信息
- 中文名称：
- (E)-3-[4-[(E)-2-(2-氯-4-氟苯基)-1-(1H-吲唑-5-基)丁-1-烯-1-基]苯基]-2-丙烯酸
- 中文别名：
- ARN-810
- 英文名称：
- GDC-0810
- 英文别名：
- ARN-810;
(E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid;
- CAS号：
- 1365888-06-7
- 分子式：
- C3H8N2O
- 分子量：
- 88.10840
- 精确质量：
- 88.06370
- PSA：
- 49.49000
物化性质
- 外观与性状：
- 固体粉末
- 可溶性：
- Soluble in DMSO, not in water
- 储存条件：
- Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
