CAS:2152628-33-4Selpercatinib

您的位置 : 首页 / Apoptosis / c-RET / Selpercatinib

Selpercatinib Selpercatinib Cat No. FB16750Cas No. 2152628-33-4

Synonyms: LOXO-292

Selpercatinib is a potent and specific RET inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9026 mL
- 9.5129 mL
- 19.0258 mL
- 5 mM
- 0.3805 mL
- 1.9026 mL
- 3.8052 mL
- 10 mM
- 0.1903 mL
- 0.9513 mL
- 1.9026 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

2152628-33-4

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C29H31N7O3

运输

蓝冰

分子量

525.60

别名

LOXO-292

溶解度

DMSO	25.0 mg/mL (47.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

靶点数据

生物活性

描述The receptor tyrosine kinase RET can be oncogenically activated by gene fusions or point mutations. Selpercatinib is a novel, highly selective, ATP-competitive small molecule RET inhibitor designed to inhibit diverse RET fusions, activating mutations and acquired resistance mutations. Treatment with selpercatinib for 72 h potently inhibited cell proliferation in four RET fusion-positive or RET-mutant cell lines. In engineered cells, selpercatinib was 60- to 1300-fold more effective in inhibiting KIF5B-RET (−/+V804L/M) than other kinase and nonkinase targets commonly inhibited by MKIs (multikinase inhibitors). In engineered and patient-derived RET fusion-positive and RET-mutant mouse tumor models, selpercatinib (30 mg/kg twice daily) caused significant regression in all models, including those harboring RET V804M, and was well-tolerated. Animals injected intracranially with CCDC6-RET fusion-positive PDX cell suspensions were treated orally with selpercatinib (30 mg/kg twice daily). It significantly prolonged survival compared with vehicle-treated animals (median 21 days)^[1].