| Name | Masitinib mesylate |
| Description | Masitinib mesylate (AB-1010 mesylate) is a selective, orally bioavailable c-Kit inhibitor with an IC50 of 200 nM for human recombinant c-Kit, and IC50 values of 540/800 nM and 510 nM for PDGFRα/β and LynB, respectively. |
| 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[1]. |
| In vivo | Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs[2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (84.07 mM), Sonication is recommended.
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| Keywords | SCFR | PDGFR | c-Kit | Apoptosis | AB 1010 | AB 1010 Mesylate | Src | CD117 | Masitinib | Platelet-derived growth factor receptor | AB1010 | FGFR | Masitinib mesylate | Masitinib Mesylate | AB-1010 | Inhibitor | AB1010 Mesylate | Fibroblast growth factor receptor | inhibit | AB-1010 Mesylate |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Ferulic Acid |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
