Flumatinib

• Description:

  Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].

• Product Name Alternative:

  HHGV678

• UNSPSC:

  12352005

• Target:

  Bcr-Abl; c-Kit; PDGFR

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Flumatinib.html

• Purity:

  99.94

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C(NC1=CC(NC2=NC=CC(C3=CC=CN=C3)=N2)=C(C)N=C1)C4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4

• Molecular Formula:

  C29H29F3N8O

• Molecular Weight:

  562.59

• References & Citations:

  [1]Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24 (10) :1807-9.|[2]Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2013 Nov 10.|[3]Gong A, et al. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38 (8) :1328-40.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Citation 01:

  PLoS One. 2024 Nov 1;19 (11) :e0308647.|Cell Rep Methods. 2023 Oct 23;3 (10) :100599.

• CAS Number:

  [895519-90-1]