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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-G-749
G-749

Chemical Structure : G-749

CAS No.: 1457983-28-6

G-749 (Denfivontinib, G 749, G749)

货号: PC-42981Not For Human Use, Lab Use Only.

Denfivontinib (G-749) is a potent, broad-spetrum FLT-3 inhibitor with IC50 of 0.4 and 0.6 nM against wt FLT-3 and FLT3-D835Y mutant, respectively.

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

生物&药学活性

Denfivontinib (G-749) is a potent, broad-spetrum FLT-3 inhibitor with IC50 of 0.4 and 0.6 nM against wt FLT-3 and FLT3-D835Y mutant, respectively.
G-749 also shows potent and sustained inhibition of the FLT3 mutants including FLT3-ITD, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays.
G-749 also inhibits RTKs Ret, FLT1, Axl, Fms, FGFR-1/3 (IC50=9-30 nM), and Aurora A and B (IC50=6-24 nM) inhibits autophosphorylation of FLT3 with IC50 of <8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells.
G-749  shows potent antileukemic activity in patient blasts harboring FLT3-ITD, FLT3-TKD, and FLT3-ITD/TKD mutations through inhibition of pFLT3 and pERK1/2 both in vitro and in vivo, overcomes drug resistance of AC220 and/or PKC412.

物理化学性质&存储条件

分子量 521.409
分子式 C25H25BrN6O2
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

DMSO: 25 mg/mL

Chemical Name/SMILES

Pyrido[4,3-d]pyrimidin-5(6H)-one, 8-bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]-

参考文献

1. Lee HK, et al. Blood. 2014 Apr 3;123(14):2209-19.

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