Powder: -20°C for 3 years | In solvent: -80°C for 1 year
G-749 是一种新型 FLT3 抑制剂,对 FLT3 野生型和突变体有持续的抑制作用,IC50值分别为 0.4 nM 和 0.6 nM。它可用于急性髓系白血病的耐药研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 662 | 现货 | ||
10 mg | ¥ 1,090 | 现货 | ||
25 mg | ¥ 2,380 | 现货 | ||
50 mg | ¥ 3,690 | 现货 | ||
100 mg | ¥ 5,320 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 762 | 现货 |
产品描述 | G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants. |
靶点活性 | FLT3:0.4 nM, Aurora B:6 nM, FLT3 (D835Y):0.6 nM, Mer:1 nM, RET:9 nM |
体外活性 | 在Molm-14细胞骨髓移植模型中,口服 G-749(20 mg/kg),能够抑制肿瘤生长.在MV4-11异种移植的小鼠模型中,口服 G-749(30 mg/kg)通过抑制FLT3通路,并显著抑制肿瘤细胞生长. |
体内活性 | 在AML患者的原始细胞中,G-749通过诱导细胞凋亡,能够抑制细胞增殖。在稳定表达FLT3-ITD/N676D,FLT3-ITD/F691L,FLT3-D835Y,或FLT3-D835Y/N676D的BaF3细胞系中(IC50 <10 nM),G-749具有显著的抑制活性。 |
激酶实验 | Kinase assay: Activity assays are conducted using Lance Ultra time-resolved fluorescence resonance energy transfer (TR-FRET) technology from Perkin-Elmer. Briefly, 10 ng/mL FLT3 enzyme, a serial diluted G-749, 80 nM substrate of ULight-poly-GT peptide and variable amounts of ATP (8.5 μM to 1088 μM) are mixed in kinase assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT and 0.01% Tween-20) and are added to a 384-well OptiPlate-384 in a volume of 10 μL. Kinase reactions are incubated at room temperature for up to 1 h and then stopped by the addition of 5 μL of 10 mM EDTA. A volume of 5 μL of the specific Eu-labeled-anti-phosphopeptide antibody diluted in LANCE Detection Buffer is then added to a final concentration of 2 nM. After 30-minute incubation, assay plates are incubated at 23°C and the LANCE signal is measured on an EnVision Multilabel Reader. Excitation wavelength is set at 320 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). The IC50 is calculated using nonlinear regression analysis analysis by GradPad Prism 5. |
细胞实验 | Cells are seeded at a density of 2 ×104 cells per well and treated with the indicated concentrations of test inhibitor for 72 hours at 37℃. The conditioned medium (CM) is prepared from HS-5 cell culture for 5 days under routine culture conditions, clarified by centrifugation, and used immediately. The CM is added to complete medium at a final concentration of 35%. In coculture experiments, 5 ×104 AML blast cells are plated in 24-well plates containing 1 ×104 HS-5 monolayers and then cultured for at least 48 hours before the exposure of inhibitors. Cell viability is determined by an ATPLite assay. (Only for Reference) |
别名 | G749 |
分子量 | 521.41 |
分子式 | C25H25BrN6O2 |
CAS No. | 1457983-28-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 23 mg/mL (44.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9179 mL | 9.5894 mL | 19.1788 mL | 47.9469 mL |
5 mM | 0.3836 mL | 1.9179 mL | 3.8358 mL | 9.5894 mL | |
10 mM | 0.1918 mL | 0.9589 mL | 1.9179 mL | 4.7947 mL | |
20 mM | 0.0959 mL | 0.4795 mL | 0.9589 mL | 2.3973 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
G-749 1457983-28-6 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors FLT c-RET TAM Receptor Aurora Kinase resistance tyrosine AML G749 FLT3 acute kinase myeloid Cluster of differentiation antigen 135 inhibit receptor Inhibitor G 749 leukemia drug Fms like tyrosine kinase 3 Fms-like CD135 inhibitor