G-749
作者：齊岳
發布時間：2023-08-22
09:28:17
點擊數：
產品名稱：G-749
產品描述：
| 產品描述 | G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants. |
| 靶點活性 | FLT3:0.4 nM, Aurora B:6 nM, FLT3 (D835Y):0.6 nM, Mer:1 nM, RET:9 nM |
| 體外活性 | 在Molm-14細胞骨髓移植模型中,口服 G-749（20 mg/kg）,能夠抑制腫瘤生長.在MV4-11異種移植的小鼠模型中,口服 G-749（30 mg/kg）通過抑制FLT3通路,并顯著抑制腫瘤細胞生長. |
| 體內活性 | 在AML患者的原始細胞中,G-749通過誘導細胞凋亡,能夠抑制細胞增殖。在穩定表達FLT3-ITD/N676D,FLT3-ITD/F691L,FLT3-D835Y,或FLT3-D835Y/N676D的BaF3細胞系中（IC50 <10 nM）,G-749具有顯著的抑制活性。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | G749 |
| 分子量 | 521.419 |
| 分子式 | C25H25BrN6O2 |
| CAS No. | 1457983-28-6 |
存儲
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 )
聯系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
主營產品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉換、石墨烯、光電材料、點擊化學、凝集素、載玻片、蛋白質交聯劑、脂質體、蛋白、多肽、氨基酸、糖化學等。
