790299-79-5
Chemical Structure
Masitinib
Synonym(s): AB1010
- CAS No.: 790299-79-5
- Formula:C28H30N6OS
- Molecular Weight:498.64
IUPAC Name: N-(4-methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
InChIKey: WJEOLQLKVOPQFV-UHFFFAOYSA-N
SMILES: O=C(NC1=CC=C(C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4
Biological Activity: Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity[1][2][4].
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Masitinib | 99.66% | Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity. | ||||||||||||||||||||
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Masitinib (Standard) | ≥98% | Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity. | ||||||||||||||||||||
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- [1]. Dubreuil P, et al. Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT. PLoS One, 2009, 4(9), e7258.
- [2]. Lawrence J, et al. Masitinib demonstrates anti-proliferative and pro-apoptotic activity in primary and metastatic feline injection-site sarcoma cells. Vet Comp Oncol, 2011, doi: 10.1111/j.1476-5829.2011.00291.x. [Content Brief]
- [4]. Marech I, et al. Masitinib (AB1010), from canine tumor model to human clinical development: where we are? Crit Rev Oncol Hematol. 2014 Jul;91(1):98-111. [Content Brief]
Keywords
