≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at 2-8°C,Desiccated Ships Wet ice Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit ( IC 50 =200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β ( IC 50 s=540/800 nM), Lyn ( IC 50 = 510 nM for LynB), Lck , and, to a lesser extent, FGFR3 and FAK . Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.
In Vitro
Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. Masitinib demonstrates weak inhibition of Abl and c-Fms. Masitinib more strongly inhibits degranulation, cytokine production, and bone marrow mast cell migration than imatinib. In Ba/F3 cells expressing human wild-type Kit, masitinib inhibits SCF (stem cell factor)-induced cell proliferation with an IC 50 of 150 nM, while the IC 50 for inhibition of IL-3-stimulated proliferation is at approximately >10 μM. In Ba/F3 cells expressing PDGFRα, masitinib inhibits PDGF-BB-stimulated proliferation and PDGFRα tyrosine phosphorylation with IC 50 of 300 nM. Masitinib also causes inhibition of SCF-stimulated tyrosine phosphorylation of human Kit in mastocytoma cell-lines and BMMC. Masitinib inhibits Kit gain-of-function mutants, including V559D mutant and Δ27 mouse mutant with IC 50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC 50 of 10 and 30 nM, respectively. ?\nMasitinib inhibits cell growth and PDGFR phosphorylation in two novel ISS cell lines, which suggest that Masitinib displays activity against both primary and metastatic ISS cell line and may aid in the clinical management of ISS. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Masitinib inhibits tumour growth and increases the median survival time in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity or genotoxicity . ?\nMasitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50: 200 nM (Kit), 540 nM (PDGFRα), 800 nM (PDGFRβ), 510 nM (LynB)
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Classe | Benzene and substituted derivatives |
| Subclass | Anilides |
| Intermediate Tree Nodes | Aromatic anilides |
| Direct Parent | Benzanilides |
| Alternative Parents | Benzamides Diaminotoluenes Aniline and substituted anilines Phenylmethylamines Benzoyl derivatives Benzylamines 2,4-disubstituted thiazoles Aralkylamines N-methylpiperazines 2-amino-1,3-thiazoles Pyridines and derivatives Sulfonyls Alkanesulfonic acids Organosulfonic acids Methanesulfonates Heteroaromatic compounds Trialkylamines Amino acids and derivatives Secondary carboxylic acid amides Azacyclic compounds Organooxygen compounds Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Not available |
| Substituents | Benzanilide - Benzamide - Benzoic acid or derivatives - Diaminotoluene - Phenylmethylamine - Benzylamine - Aniline or substituted anilines - Benzoyl - 2,4-disubstituted 1,3-thiazole - Toluene - N-methylpiperazine - Aralkylamine - N-alkylpiperazine - Piperazine - Pyridine - 1,4-diazinane - 1,3-thiazol-2-amine - Thiazole - Azole - Sulfonyl - Organosulfonic acid - Organosulfonic acid or derivatives - Heteroaromatic compound - Methanesulfonate - Alkanesulfonic acid - Organic sulfonic acid or derivatives - Secondary carboxylic acid amide - Tertiary amine - Carboxamide group - Tertiary aliphatic amine - Amino acid or derivatives - Azacycle - Organoheterocyclic compound - Carboxylic acid derivative - Organosulfur compound - Amine - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Organooxygen compound - Organic oxygen compound - Organonitrogen compound - Aromatic heteromonocyclic compound |
| Descrizione | This compound belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene. |
| External Descriptors | Not available |
| Solubilità | 1M HCl : 100 mg/mL (168.14 mM; ultrasonic and adjust pH to 1 with HCl) DMSO : ≥ 30 mg/mL (50.44 mM) |
|---|---|
| Peso molecolare | 594.800 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 7 |
| Exact Mass | 594.208 Da |
| Monoisotopic Mass | 594.208 Da |
| Topological Polar Surface Area | 164.000 Ų |
| Heavy Atom Count | 41 |
| Formal Charge | 0 |
| Complexity | 788.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 2 |
