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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Kit-BLU-263
BLU-263

Chemical Structure : BLU-263

CAS No.: 2505078-08-8

BLU-263 (Elenestinib, BLU263)

货号: PC-20030Not For Human Use, Lab Use Only.

Elenestinib (BLU-263, BLU263) is a potent, selective, oral next-generation KIT D816V inhibitor with IC50 of 0.2 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Elenestinib (BLU-263, BLU263) is a potent, selective, oral next-generation KIT D816V inhibitor with IC50 of 0.2 nM.
BLU-263 has ELISA IC50 of 6 nM against HMC1.2 human mast cells (V560G/D816V).
BLU-263 exhibits limited central nervous system penetration, shows potential for systemic mastocytosis (SM).

物理化学性质&存储条件

分子量 528.60
分子式 C27H29FN10O
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

(S)-2-(4-(4-(4-(5-(1-amino-1-(4-fluorophenyl)ethyl)pyrimidin-2-yl)piperazin-1-yl)pyrrolo[2,1-f][1,2,4]triazin-6-yl)-1H-pyrazol-1-yl)ethan-1-ol

参考文献

1. Dave N, et al. Safety and pharmacokinetics of BLU-263, a next-generation KIT inhibitor, in healthy volunteers[C]//Cancer Res (AACR Annual Meeting Abstracts). 2021, 122.

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