Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor ofc-Kit(IC₅₀=200 nM for human recombinant c-Kit). It also inhibitsPDGFRα/β(IC₅₀s=540/800 nM),Lyn(IC₅₀= 510 nM for LynB),Lck, and, to a lesser extent,FGFR3andFAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity^[1][2][4].

IC50: 200 nM (Kit), 540 nM (PDGFRα), 800 nM (PDGFRβ), 510 nM (LynB)^[1]

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. In contrast, 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 IC₅₀of 150 nM, while the IC₅₀for 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 IC₅₀of 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 IC₅₀of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC₅₀of 10 and 30 nM, respectively^[1].
Masitinib 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^[2].

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^[1].
Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs^[3].

594.75

Solid

C₂₉H₃₄N₆O₄S₂

1048007-93-7

甲磺酸马赛替尼

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

1M HCl : 100 mg/mL(168.14 mM;ultrasonic and adjust pH to 1 with HCl)

DMSO : ≥ 30 mg/mL(50.44 mM)

*"≥" means soluble, but saturation unknown.

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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。