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CAS No.: 2152628-33-4

塞尔帕替尼 Catalog No. CSN25546

Synonyms: LOXO-292;ARRY-192;塞尔帕替尼

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.

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技术信息

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].
参考文献

[1] Subbiah V, Velcheti V, Tuch BB, et al. Selective RET kinase inhibition for patients with RET-altered cancers. Ann Oncol. 2018;29(8):1869-1876

实验方案

计算器摩尔计算器总药量计算器工作液计算器
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

技术信息

CAS号

2152628-33-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H31N7O3

运输

蓝冰

分子量

525.60

别名

LOXO-292;ARRY-192;塞尔帕替尼

溶解度

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

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