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G-749

Catalog No. T2620   CAS 1457983-28-6
Synonyms: resistance, tyrosine, AML, G749, G-749, FLT3, acute, kinase, myeloid, G 749, Cluster of differentiation antigen 135, inhibit, receptor, Inhibitor, leukemia, drug, Fms like tyrosine kinase 3, Fms-like, CD135, Apoptosis

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.

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G-749, CAS 1457983-28-6
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.
Targets&IC50 FLT3:0.4 nM, Aurora B:6 nM, Mer:1 nM, FLT3 (D835Y):0.6 nM, RET:9 nM
Kinase Assay 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.
Cell Research 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)
Synonyms resistance, tyrosine, AML, G749, G-749, FLT3, acute, kinase, myeloid, G 749, Cluster of differentiation antigen 135, inhibit, receptor, Inhibitor, leukemia, drug, Fms like tyrosine kinase 3, Fms-like, CD135, Apoptosis
Molecular Weight 521.419
Formula C25H25BrN6O2
CAS No. 1457983-28-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

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 )

Citations

References and Literature
1. Lee HK, et al. Blood. 2014, 123(14), 2209-2219.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Autophagy Compound Library Hematonosis Compound Library Inhibitor Library Cell Cycle Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Apoptosis Compound Library Epigenetics Compound Library Angiogenesis related Compound Library

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