Flumatinib
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 Specifications
CAS Number
895519-90-1
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.
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