Masitinib (AB1010) is a tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor with IC50 of 150 ± 80, 200 ± 40 nM for KIT tyrosine phosphorylation and the recombinant wild-type KIT. Masitinib can enhance the antiproliferative effects of gemcitabi
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Platelet-derived growth factor receptor inhibitor
Note
25mg、100mg卖完停产，不再备货
Product Description
Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. A tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor.
1.Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Castéran N, Borge L, Hajem B, Lermet A, Sippl W et al.. (2009) Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.. PLoS ONE, 4 (9):(e7258). [PMID:19789626]
2.Hahn KA, Ogilvie G, Oglivie G, Rusk T, Devauchelle P, Leblanc A, Legendre A, Powers B, Leventhal PS, Kinet JP et al.. (2008) Masitinib is safe and effective for the treatment of canine mast cell tumors.. J Vet Intern Med, 22 (6):(1301-9). [PMID:18823406]
3.Humbert M, de Blay F, Garcia G, Prud'homme A, Leroyer C, Magnan A, Tunon-de-Lara JM, Pison C, Aubier M, Charpin D et al.. (2009) Masitinib, a c-kit/PDGF receptor tyrosine kinase inhibitor, improves disease control in severe corticosteroid-dependent asthmatics.. Allergy, 64 (8):(1194-201). [PMID:19614621]
4.Tebib J, Mariette X, Bourgeois P, Flipo RM, Gaudin P, Le Loët X, Gineste P, Guy L, Mansfield CD, Moussy A et al.. (2009) Masitinib in the treatment of active rheumatoid arthritis: results of a multicentre, open-label, dose-ranging, phase 2a study.. Arthritis Res Ther, 11 (3):(R95). [PMID:19549290]
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H2315286