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Gilteritinib

Chemical Structure : Gilteritinib

CAS No.: 1254053-43-4

Gilteritinib (ASP2215, ASP-2215)

货号: PC-43033Not For Human Use, Lab Use Only.

Gilteritinib (ASP2215) is a potent FLT3/AXL inhibitor with IC50 of 0.73 nM/0.29 nM respectively; also inhibits LTK and ALK (IC50=0.35 nM and 1.2 nM respectively).

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

生物&药学活性

Gilteritinib (ASP2215) is a potent FLT3/AXL inhibitor with IC50 of 0.73 nM/0.29 nM respectively; also inhibits LTK and ALK (IC50=0.35 nM and 1.2 nM respectively).
Gilteritinib (ASP2215) shows >800-fold selectivity over c-Kit.
Gilteritinib (ASP2215) inhibits the growth of Ba/F3 cells expressing either FLT3-ITD, FLT3-D835Y, FLT3-ITD-D835Y, FLT3-ITD-F691 L, and FLT3-ITD-F691I, with IC50 of 1.8 nM, 1.6 nM, 2.1 nM, 22 nM, and 49 nM, respectively.
Gilteritinib (ASP2215) is orally bioactive.

物理化学性质&存储条件

分子量 552.7115
分子式 C29H44N8O3
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

Ethanol: 100 mM

Chemical Name/SMILES

2-Pyrazinecarboxamide, 6-ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-

参考文献

1. Mori M, et al. Invest New Drugs. 2017 May 17. doi: 10.1007/s10637-017-0470-z.

2. Lee LY, et al. Blood. 2017 Jan 12;129(2):257-260.

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