Flumatinib mesylate

SKU: orb1299437

Description

Flumatinib mesylate is a potent and selective small molecule inhibitor targeting c-Abl, PDGFRβ, and c-Kit tyrosine kinases. It has demonstrated efficacy in overcoming resistance conferred by specific KIT mutations in preclinical studies, supporting its investigation in related hematological and solid tumor research both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 895519-91-2
• MW: 658.69
• Purity: 99.82%
• Formula: C₃₀H₃₃F₃N₈O₄S
• SMILES: CS(O)(=O)=O.CN1CCN(Cc2ccc(cc2C(F)(F)F)C(=O)Nc2cnc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
• Target: PDGFR,Bcr-Abl,c-Kit
• Solubility: DMSO:70 mg/mL (106.27 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.04 mM);H2O:50 mg/mL (75.91 mM)

Bioactivity

• Target IC50:
  PDGFRβ:307.6 nM|c-ABL:1.2 nM
• In Vitro:
  In vivo study consistently suggested that flumatinib had superior efficacy compared with imatinib or sunitinib against 32D cells with the secondary mutation Y823D. Molecular modeling of flumatinib docked to the KIT kinase domain suggested a special mechanism underlying the capability of flumatinib to overcome the drug-resistance conferred by activation loop mutations. These findings suggest that flumatinib could be a promising therapeutic agent against GISTs resistant to both imatinib and sunitinib because of secondary mutations in the activation loop.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CD117, cKit, c-Kit, c-Abl, BcrAbl, Bcr-Abl, inhibit, Platelet-derived growth factor receptor, Flumatinib, Flumatinib Mesylate, Flumatinib mesylate, Inhibitor, HHGV 678, HHGV 678 Mesylate, HHGV678, HHGV-678, HHGV678 mesylate, HHGV678 Mesylate, HHGV-678 Mesylate, SCFR, PDGFR, PDGFRβ

Compound Identifiers

PubChem CID

46910592