Masitinib mesylate

SKU: orb1298847

Description

Masitinib mesylate is an orally active, selective tyrosine kinase inhibitor targeting c-Kit, PDGFRα/β, and Lyn. It is widely used in preclinical research for investigating mast cell disorders, cancers, and inflammatory diseases, with applications in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1048007-93-7
• MW: 594.75
• Purity: 99.92%
• Formula: C₂₉H₃₄N₆O₄S₂
• SMILES: CS(O)(=O)=O.CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nc(cs3)-c3cccnc3)c2)CC1
• Target: Src,c-Kit,FAK,PDGFR,Apoptosis,FGFR
• Solubility: DMSO:50 mg/mL (84.07 mM)

Bioactivity

• Target IC50:
  PDGFRβ:800 nM |PDGFRα:540 nM |LynB:510 nM|c-Kit:200 nM
• In Vivo:
  Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs
• In Vitro:
  In vitro, masitinib had greater activity and selectivity against KIT than imatinib, inhibiting recombinant human wild-type KIT with an half inhibitory concentration (IC50) of 200±40 nM and blocking stem cell factor-induced proliferation and KIT tyrosine phosphorylation with an IC50 of 150±80 nM in Ba/F3 cells expressing human or mouse wild-type KIT. Masitinib also potently inhibited recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, masitinib demonstrated weak inhibition of ABL and c-Fms and was inactive against a variety of other tyrosine and serine/threonine kinases. This highly selective nature of masitinib suggests that it will exhibit a better safety profile than other tyrosine kinase inhibitors; indeed, masitinib-induced cardiotoxicity or genotoxicity has not been observed in animal studies. Molecular modelling and kinetic analysis suggest a different mode of binding than imatinib, and masitinib more strongly inhibited degranulation, cytokine production, and bone marrow mast cell migration than imatinib. Furthermore, masitinib potently inhibited human and murine KIT with activating mutations in the juxtamembrane domain. In vivo, masitinib blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant.

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

Apoptosis, AB-1010, AB1010 Mesylate, AB-1010 mesylate, AB-1010 Mesylate, AB1010, AB 1010, AB 1010 Mesylate, c-Kit, cKit, CD117, Platelet-derived growth factor receptor, Lyn, Kit, inhibit, Fibroblast growth factor receptor, FGFR3, FGFR, FAK, Masitinib, Masitinib mesylate, Masitinib Mesylate, LCK, Inhibitor, PDGFRβ, PDGFRα, PDGFR, Src, SCFR

Compound Identifiers

PubChem CID

25024769