G-749
作者：齐岳
发布时间：2023-08-22
09:28:17
点击数：
产品名称：G-749
产品描述：
| 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 | 521.419 |
| 分子式 | C25H25BrN6O2 |
| CAS No. | 1457983-28-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
H2O: <1 mg/mL
DMSO: 23 mg/mL (44.1 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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