Masitinib (mesylate)

Masitinib mesylate (AB-1010 mesylate) 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 mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity[1][2][4].

Product Specifications

CAS Number

[1048007-93-7]

Product Name Alternative

AB-1010 mesylate

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; c-Kit; FGFR; PDGFR; Src

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/masitinib-mesylate.html

Purity

99.98

Solubility

1M HCl : 100 mg/mL (ultrasonic; adjust pH to 1 with HCl) |DMSO : ≥ 30 mg/mL

Smiles

O=C(NC1=CC=C(C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4.CS(=O)(O)=O

Molecular Formula

C29H34N6O4S2

Molecular Weight

594.75

Precautions

H302, H315, H319, H335

References & Citations

[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.|[3]Hahn KA, et al. Masitinib is safe and effective for the treatment of canine mast cell tumors. J Vet Intern Med, 2008, 22 (6), 1301-1309.|[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.