化合物G-749 T2620
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Product IntroductionBioactivity英文名: G-749描述: 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
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Product Introduction
Bioactivity
英文名: G-749
描述: 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。
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)
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.
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。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 23 mg/mL (44.1 mM)
关键字: resistance | tyrosine | AML | FLT3 | acute | kinase | myeloid | G-749 | Cluster of differentiation antigen 135 | inhibit | receptor | Inhibitor | G 749 | leukemia | drug | Fms like tyrosine kinase 3 | Fms-like | CD135 | Apoptosis
相关产品: FR 180204 | Kahweol | BX-912 | AFMK | NSC 15364 | M3541 | Angiotensin II human | Gardenin B | Vatalanib dihydrochloride | Glutathione arsenoxide hydrochloride
相关库: Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Epigenetics Compound Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
Bioactivity
英文名: G-749
描述: 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。
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)
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.
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。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 23 mg/mL (44.1 mM)
关键字: resistance | tyrosine | AML | FLT3 | acute | kinase | myeloid | G-749 | Cluster of differentiation antigen 135 | inhibit | receptor | Inhibitor | G 749 | leukemia | drug | Fms like tyrosine kinase 3 | Fms-like | CD135 | Apoptosis
相关产品: FR 180204 | Kahweol | BX-912 | AFMK | NSC 15364 | M3541 | Angiotensin II human | Gardenin B | Vatalanib dihydrochloride | Glutathione arsenoxide hydrochloride
相关库: Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Epigenetics Compound Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
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