| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 250 mg/mL (420.34 mM), Sonication is recommended.
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| Keywords | Src | SCFR | Platelet-derived growth factor receptor | PDGFRβ | PDGFRα | PDGFR | Masitinib mesylate | Masitinib | Lyn | LCK | Kit | Inhibitor | inhibit | Fibroblast growth factor receptor | FGFR3 | FGFR | FAK | c-Kit | cKit | CD117 | Apoptosis | AB-1010 Mesylate | AB1010 Mesylate | AB-1010 | AB1010 | AB 1010 Mesylate | AB 1010 |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Ferulic Acid | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
