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G-749

    
10mM in DMSO

G-749

源叶(MedMol)
T96029 一键复制产品信息
1457983-28-6
C25H25BrN6O2
521.41
8-bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]-pyrido[4,3-d]pyrimidin-5(6H)-one
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T96029-1ml促销
10mM in DMSO

¥720.00 ¥648.00

4 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: FLT3 抑制剂;FLT3 Inhibitors;;InformationG-749 G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.TargetsFLT3 (Cell-free assay); FLT3 (D835Y) (Cell-free assay); Mer (Cell-free assay); Aurora B (Cell-free assay); RET (Cell-free assay) 15501,0.4 nM; 0.6 nM; 1 nM; 6 nM; 9 nMIn vitroIn 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 <10 nM, and thus overcomes drug resistance. In blasts of AML patients, G-749 also exhibits potent antileukemia activity.In vivoIn 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.Cell Research(from reference)Cell lines:MV4-11, RS4-11, K562, HEL, and Molm-14 cells Concentrations:~1 μM Incubation Time:72 hours 
靶点: IC50: 0.4 nM (FLT3-WT), 0.6 nM (FLT3-D835Y)
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.918 ml 9.589 ml 19.179 ml
5 mM 0.384 ml 1.918 ml 3.836 ml
10 mM 0.192 ml 0.959 ml 1.918 ml
50 mM 0.038 ml 0.192 ml 0.384 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

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