Small Molecular API Masitinib (CAS: 790299-79-5)

Masitinib ≤500 nM concentration when ATP competitive inhibitor. Masitinib also effectively inhibit recombinant PDGFR and intracellular kinases Lyn, and FGFR 3. However, Masitinib for ABL and c-Fms weak inhibitory effect. Masitinib effect on degranulation, cytokine production, and bone marrow mast cell migration, the inhibitory effect of a lot stronger than imatinib. When expressing human wild-type KIT of Ba / F3 cells, Masitinib inhibiting SCF (stem cell factor) induced cell proliferation, IC50 of 150 nM, and inhibit the proliferation of IL-3-stimulated, IC50 value of about> 10 μM. Ba PDGFR-α expression in the / F3 cells, Masitinib inhibiting PDGF-BB-stimulated proliferation and PDGFR-α tyrosine phosphorylation, IC50 of 300 nM. Masitinib role in mast cell tumor cell lines and BMMC, also inhibits KIT Human stimulated tyrosine phosphorylation. Masitinib effect on Ba / F3 cells, suppression function KIT mutations obtained, including V559D mutations and Δ27 mutant mice, IC50 were 3 and 5 nM. Masitinib inhibition of mast cell tumor cell lines include HMC-1α155 and cell proliferation FMA3 of, IC50 were 10 and 30 nM. [1] Masitinib role in ISS two new cell lines, inhibition of cell growth and PDGFR phosphorylation, indicating Masitinib suppress primary and metastatic cell lines ISS, and on the clinical management of ISS helpful. 

 

Masitinib ≤500 nM concentration when ATP competitive inhibitor. Masitinib also effectively inhibit recombinant PDGFR and intracellular kinases Lyn, and FGFR 3. However, Masitinib for ABL and c-Fms weak inhibitory effect. Masitinib effect on degranulation, cytokine production, and bone marrow mast cell migration, the inhibitory effect of a lot stronger than imatinib. When expressing human wild-type KIT of Ba / F3 cells, Masitinib inhibiting SCF (stem cell factor) induced cell proliferation, IC50 of 150 nM, and inhibit the proliferation of IL-3-stimulated, IC50 value of about> 10 μM. Ba PDGFR-α expression in the / F3 cells, Masitinib inhibiting PDGF-BB-stimulated proliferation and PDGFR-α tyrosine phosphorylation, IC50 of 300 nM. Masitinib role in mast cell tumor cell lines and BMMC, also inhibits KIT Human stimulated tyrosine phosphorylation. Masitinib effect on Ba / F3 cells, suppression function KIT mutations obtained, including V559D mutations and Δ27 mutant mice, IC50 were 3 and 5 nM. Masitinib inhibition of mast cell tumor cell lines include HMC-1α155 and cell proliferation FMA3 of, IC50 were 10 and 30 nM. [1] Masitinib role in ISS two new cell lines, inhibition of cell growth and PDGFR phosphorylation, indicating Masitinib suppress primary and metastatic cell lines ISS, and on the clinical management of ISS helpful.