Cofttek holdings limited

PDGFR&FGFR

Masitinib (AB1010) (790299-79-5)

Masitinib(AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet.

Not Intended for Therapeutic Use. For research use only.

CAS: 790299-79-5 Category

Masitinib (AB1010) (790299-79-5) Description:

Masitinib, also known as AB1010, is an orally bioavailable and multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity. Masitinib selectively binds to and inhibits both the wild-type and mutated forms of the stem cell factor receptor (c-Kit; SCFR); platelet-derived growth factor receptor (PDGFR); fibroblast growth factor receptor 3 (FGFR3); and, to a lesser extent, focal adhesion kinase (FAK). As a consequence, tumor cell proliferation may be inhibited in cancer cell types that overexpress these receptor tyrosine kinases (RTKs). Masitinib was approved for veterinary use.

Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, Masitinib demonstrates weak inhibition of Abl and c-Fms. Masitinib more strongly inhibits degranulation, cytokine production, and bone marrow mast cell migration than imatinib. In Ba/F3 cells expressing human wild-type Kit, Masitinib inhibits SCF (stem cell factor)-induced cell proliferation with an IC50 of 150 nM, while the IC50 for inhibition of IL-3-stimulated proliferation is at approximately >10 µM. In Ba/F3 cells expressing PDGFRα, Masitinib inhibits PDGF-BB-stimulated proliferation and PDGFRα tyrosine phosphorylation with IC50 of 300 nM. Masitinib also causes inhibition of SCF-stimulated tyrosine phosphorylation of human Kit in mastocytoma cell-lines and BMMC. Masitinib inhibits Kit gain-of-function mutants, including V559D mutant and Δ27 mouse mutant with IC50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC50 of 10 and 30 nM, respectively. Masitinib inhibits cell growth and PDGFR phosphorylation in two novel ISS cell lines, which suggest that Masitinib displays activity against both primary and metastatic ISS cell line and may aid in the clinical management of ISS.

Masitinib (AB1010) (790299-79-5) Specifications:

Product Name Masitinib (AB1010)
Synonym AB-1010; AB 1010; AB1010; Masitinib. Brand name: Kinavet; Masivet
Chemical Name 4-[(4-methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)-1,3-thiazol-2-yl]amino}phenyl)benzamide.
Purity ≥98% (HPLC)
CAS Number 790299-79-5
Molecular Formula C28H30N6OS
Molecular Weight 498.649 g/mol
Monoisotopic Mass 498.22 g/mol
MDL number MFCD09954132
InChIKey WJEOLQLKVOPQFV-UHFFFAOYSA-N
InChi Code InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32)
SMILES O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4
Form Powder
Color white
Solubility  .DMSO 100 mg/mL (200.55 mM)

Water Insoluble

Alcohol 4 mg/mL (8.02 mM)

Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application a tyrosine-kinase inhibitor

 


=

RIDADR NONH for all modes of transport

References:

[1]. Cadot P, Hensel P, Bensignor E, Hadjaje C, Marignac G, Beco L, Fontaine J, Jamet JF, Georgescu G, Campbell K, Cannon A, Osborn SC, Messinger L, Gogny-Goubert M, Dubreuil P, Moussy A, Hermine O. Masitinib decreases signs of canine atopic dermatitis: a multicentre, randomized, double-blind, placebo-controlled phase 3 trial. Vet Dermatol. 2011 Dec;22(6):554-64. doi: 10.1111/j.1365-3164.2011.00990.x. Epub 2011 Jun 13. PubMed PMID: 21668810.

[2]. Georgin-Lavialle S, Lhermitte L, Suarez F, Yang Y, Letard S, Hanssens K, Feger F, Renand A, Brouze C, Canioni D, Asnafi V, Chandesris MO, Aouba A, Gineste P, Macintyre E, Mansfield CD, Moussy A, Lepelletier Y, Dubreuil P, Hermine O. Mast cell leukemia: identification of a new c-Kit mutation, dup(501-502), and response to masitinib, a c-Kit tyrosine kinase inhibitor. Eur J Haematol. 2012 Jul;89(1):47-52. doi: 10.1111/j.1600-0609.2012.01761.x. Epub 2012 Apr 28. PubMed PMID: 22324351.

[3]. Characterization of in vivo metabolites in rat urine following an oral dose of masitinib by liquid chromatography tandem mass spectrometry. Kadi AA, Amer SM, Darwish HW, Attwa MW. Chem Cent J. 2018 May 15;12(1):61. doi: 10.1186/s13065-018-0429-y. PMID: 29766296

[4]. Decrease of cocaine, but not heroin, self-administration and relapse by the tyrosine kinase inhibitor masitinib in male Sprague Dawley rats. Belin-Rauscent A, Lacoste J, Hermine O, Moussy A, Everitt BJ, Belin D. Psychopharmacology (Berl). 2018 May;235(5):1545-1556. doi: 10.1007/s00213-018-4865-0. Epub 2018 Mar 8. PMID: 29520592

[5]. LC-MS/MS method for the quantification of masitinib in RLMs matrix and rat urine: application to metabolic stability and excretion rate. Amer SM, Kadi AA, Darwish HW, Attwa MW. Chem Cent J. 2017 Dec 22;11(1):136. doi: 10.1186/s13065-017-0365-2. PMID: 29274040

1 review for Masitinib (AB1010) (790299-79-5)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The Masitinib (AB1010) (790299-79-5) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *