G-749CAS号： 1457983-28-6分子式： C25H25BrN6O2分子量： 521.41描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
G-749 is a novel selective inhibitor of FLT3 kinase as a therapeutics for AML with IC50 value of 0.4 nM for wild-type FLT31.
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| 纯度 |
>98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
G-749, G749, G 749, CS-3343
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| 外观 |
Powder
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| 可溶性/溶解性 |
DMSO Solubility: 24 mg/mL warmed (46.02 mM)
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| 生物活性 | |
| 靶点 |
FLT3 ,FLT3 (D835Y) ,Mer ,Aurora B ,RET
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| In vitro(体外研究) |
In FLT3-WT-bearing RS4-11 cells and FLT3-ITD-harboring MV4-11 and Molm-14 cells, G-749 potently inhibits autophosphorylation of FLT3 with IC50 of ≤8 nM. In leukemia cells, G-749 shows antiproliferative activity by inducing apoptosis. In BaF3 cell lines that stably express FLT3-ITD/N676D, FLT3-ITD/F691L, FLT3-D835Y, or FLT3-D835Y/N676D, G-749 shows strong inhibitory activity with IC50 of
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| In vivo(体内研究) |
In MV4-11 xenograft mice, G-749 (30 mg/kg p.o.) effectively inhibits the FLT3 pathway and significant inhibits tumor growth. In an orthogonal model of bone marrow engraftment using Molm-14 cells, G-749 (20 mg/kg p.o.) also inhibits tumor growth and increases survival.
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分子结构图
