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Masitinib mesylate

Catalog No. T8544 CAS 1048007-93-7

Synonyms: AB-1010 mesylate

Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).

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Masitinib mesylate, CAS 1048007-93-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 70.00
50 mg	In stock	$ 87.00
100 mg	In stock	$ 147.00
200 mg	In stock	$ 237.00
500 mg	In stock	$ 392.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 100%

Purity: 99.92%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).
Targets&IC50	PDGFRβ:800 nM , PDGFRα:540 nM , c-Kit:200 nM , LynB:510 nM
In vitro	In vitro, masitinib had greater activity and selectivity against KIT than imatinib, inhibiting recombinant human wild-type KIT with an half inhibitory concentration (IC50) of 200±40 nM and blocking stem cell factor-induced proliferation and KIT tyrosine phosphorylation with an IC50?of 150±80 nM in Ba/F3 cells expressing human or mouse wild-type KIT. Masitinib also potently inhibited recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, masitinib demonstrated weak inhibition of ABL and c-Fms and was inactive against a variety of other tyrosine and serine/threonine kinases. This highly selective nature of masitinib suggests that it will exhibit a better safety profile than other tyrosine kinase inhibitors; indeed, masitinib-induced cardiotoxicity or genotoxicity has not been observed in animal studies. Molecular modelling and kinetic analysis suggest a different mode of binding than imatinib, and masitinib more strongly inhibited degranulation, cytokine production, and bone marrow mast cell migration than imatinib. Furthermore, masitinib potently inhibited human and murine KIT with activating mutations in the juxtamembrane domain.?In vivo, masitinib blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant[1].
In vivo	Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs[2]

Synonyms	AB-1010 mesylate
Molecular Weight	594.75
Formula	C29H34N6O4S2
CAS No.	1048007-93-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (42.03 mM)

References and Literature

1. Dubreuil P, et al. Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT. PLoS One, 2009, 4(9), e7258. 2. 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. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Membrane Protein-targeted Compound Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library

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Keywords

Masitinib mesylate 1048007-93-7 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Src c-Kit PDGFR FAK FGFR SCFR AB 1010 AB 1010 Mesylate CD117 AB-1010 mesylate Masitinib Platelet-derived growth factor receptor AB1010 Masitinib Mesylate AB-1010 Inhibitor AB1010 Mesylate Fibroblast growth factor receptor inhibit AB-1010 Mesylate inhibitor

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