Flumatinib (mesylate)

Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model[1][2].

Product Specifications

CAS Number

[895519-91-2]

Product Name Alternative

HHGV678 mesylate

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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-mesylate.html

Purity

99.80

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 50 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.CS(=O)(O)=O

Molecular Formula

C30H33F3N8O4S

Molecular Weight

658.69

Precautions

H302, H315, H319, H335

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.