G-749

SKU: orb1305257

Description

G-749 is a novel, potent small-molecule FLT3 inhibitor effective against both wild-type and mutant FLT3 kinases. It demonstrates sustained inhibitory activity, making it a valuable research tool for investigating acute myeloid leukemia (AML) in both cellular and animal models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1457983-28-6
• MW: 521.41
• Purity: >99.99% (May vary between batches)
• Formula: C₂₅H₂₅BrN₆O₂
• SMILES: CN1CCC(CC1)Nc1nc(Nc2ccc(Oc3ccccc3)cc2)c2c(n1)c(Br)c[nH]c2=O
• Target: TAM Receptor,FLT,Aurora Kinase,Apoptosis,c-RET
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Aurora B:6 nM|FLT3:0.4 nM|FLT3 (D835Y):0.6 nM|Mer:1 nM|RET:9 nM
• In Vivo:
  In primary cells from AML patients, G-749 was able to inhibit cell proliferation by inducing apoptosis. In BaF3 cell lines stably expressing FLT3-ITD/N676D, FLT3-ITD/F691L, FLT3-D835Y, or FLT3-D835Y/N676D (IC50 <10 nM), G-749 showed significant inhibitory activity.
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• In Vitro:
  In primary cells from AML patients, G-749 was able to inhibit cell proliferation by inducing apoptosis. In BaF3 cell lines stably expressing FLT3-ITD/N676D, FLT3-ITD/F691L, FLT3-D835Y, or FLT3-D835Y/N676D (IC50 <10 nM), G-749 showed significant inhibitory activity.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cRET, Denfivontinib, drug, Cluster of differentiation antigen 135, CD135, acute, Apoptosis, AML, Aurora Kinase, AuroraKinase, Aurora B, inhibit, kinase, myeloid, Mer, Fms-like, Fms like tyrosine kinase 3, FLT3, FLT3 (D835Y), G 749, G749, G-749, Inhibitor, leukemia, tyrosine, TAMReceptor, TAM Receptor, resistance, RET, receptor

Compound Identifiers

PubChem CID

78357765