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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-Selitrectinib
Selitrectinib

Chemical Structure : Selitrectinib

CAS No.: 2097002-61-2

Selitrectinib (LOXO-195, LOXO195)

货号: PC-60901Not For Human Use, Lab Use Only.

LOXO-195 (Selitrectinib, LOXO195) is a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively.

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纯度 & COA & 质检文件 纯度: 98.79% (HPLC) Select Batch:

生物&药学活性

LOXO-195 (Selitrectinib, LOXO195) is a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively.
LOXO-195 also diplays high potentcy against mutant TrkA G595R, TrkA G667C, TrkC G623R and TrkC G696A with IC50 of 2.0, 9.8, 2.3 and <2.5 nM, respectively.
LOXO-195 overcomes acquired resistance mediated by recurrent kinase domain (solvent front and xDFG) mutations identified in multiple patients.

物理化学性质&存储条件

分子量 380.427
分子式 C20H21FN6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(13E,14E,22R,6R)-35-fluoro-6-methyl-7-aza-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridina-2(1,2)-pyrrolidinacyclooctaphan-8-one

参考文献

1. Drilon A, et al. Cancer Discov. 2017 Sep;7(9):963-972.

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