Masitinib

• CAT Number: I004893
• CAS Number: 790299-79-5
• Molecular Formula: C₂₈H₃₀N₆OS
• Molecular Weight: 498.64
• Purity: ≥95%
• Target: c-Kit
• Solubility: DMSO: ≥ 26 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 200 nM (Kit); 540 nM/800 nM(PDGFRα/β) [1]
• IUPAC Name: 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-yl-1,3-thiazol-2-yl)amino]phenyl]benzamide
• InChI: 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)
• InChIKey: WJEOLQLKVOPQFV-UHFFFAOYSA-N
• SMILES: CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC(=CS4)C5=CN=CC=C5

Masitinib (Cat.No:I004893) is a tyrosine kinase inhibitor used in the treatment of certain types of cancer and inflammatory diseases. It targets and inhibits specific enzymes, including c-Kit, PDGFR, and Lyn kinase, which are involved in cell proliferation and immune response. Masitinib shows potential in the treatment of conditions such as gastrointestinal stromal tumors, mast cell tumors, and systemic mastocytosis.

Reference

1:Can binimetinib, encorafenib and masitinib be more efficacious than currently available mutation-based targeted therapies for melanoma treatment? Turner MC, Rossfeld K, Salama AK, Tyler D, Beasley G.Expert Opin Pharmacother. 2017 Apr;18(5):487-495. doi: 10.1080/14656566.2017.1299710. Epub 2017 Mar 22. Review. PMID: 28277830 2:Masitinib for treatment of severely symptomatic indolent systemic mastocytosis: a randomised, placebo-controlled, phase 3 study. Lortholary O, Chandesris MO, Bulai Livideanu C, Paul C, Guillet G, Jassem E, Niedoszytko M, Barete S, Verstovsek S, Grattan C, Damaj G, Canioni D, Fraitag S, Lhermitte L, Georgin Lavialle S, Frenzel L, Afrin LB, Hanssens K, Agopian J, Gaillard R, Kinet JP, Auclair C, Mansfield C, Moussy A, Dubreuil P, Hermine O.Lancet. 2017 Feb 11;389(10069):612-620. doi: 10.1016/S0140-6736(16)31403-9. Epub 2017 Jan 7. PMID: 28069279 3:Presumed masitinib-induced nephrotic syndrome and azotemia in a dog. Devine L, Polzin DJ.Can Vet J. 2016 Jul;57(7):752-6. PMID: 27429464 Free PMC Article4:Post-paralysis tyrosine kinase inhibition with masitinib abrogates neuroinflammation and slows disease progression in inherited amyotrophic lateral sclerosis. Trias E, Ibarburu S, Barreto-Núñez R, Babdor J, Maciel TT, Guillo M, Gros L, Dubreuil P, Díaz-Amarilla P, Cassina P, Martínez-Palma L, Moura IC, Beckman JS, Hermine O, Barbeito L.J Neuroinflammation. 2016 Jul 11;13(1):177. doi: 10.1186/s12974-016-0620-9. PMID: 27400786 Free PMC Article5:Antiproliferative effects of masitinib and imatinib against canine oral fibrosarcoma in vitro. Milovancev M, Helfand SC, Marley K, Goodall CP, Löhr CV, Bracha S.BMC Vet Res. 2016 Jun 4;12:85. doi: 10.1186/s12917-016-0712-x. PMID: 27259510 Free PMC Article6:Clinical response of masitinib mesylate in the treatment of canine macroscopic mast cell tumours. Grant J, North S, Lanore D.J Small Anim Pract. 2016 Jun;57(6):283-90. doi: 10.1111/jsap.12480. Epub 2016 May 2. PMID: 27136424 7:The cKit Inhibitor, Masitinib, Prevents Diabetes-Induced Retinal Vascular Leakage. Kim SR, Im JE, Jeong JH, Kim JY, Kim JT, Woo SJ, Sung JH, Park SG, Suh W.Invest Ophthalmol Vis Sci. 2016 Mar;57(3):1201-6. doi: 10.1167/iovs.15-18065. PMID: 26978025 8:Rapid and clinically significant response to masitinib in the treatment of mucosal primary esophageal melanoma with somatic KIT exon 11 mutation involving brain metastases: A case report. Prosvicova J, Lukesova S, Kopecky J, Grim J, Papik Z, Kolarova R, Navratilova B, Dubreuil P, Agopian J, Mansfield C, Moussy A, Hermine O.Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2015 Dec;159(4):695-7. doi: 10.5507/bp.2015.061. Epub 2015 Nov 27. PMID: 26725706 Free Article9:Autoimmune-like hepatitis during masitinib therapy in an amyotrophic lateral sclerosis patient. Salvado M, Vargas V, Vidal M, Simon-Talero M, Camacho J, Gamez J.World J Gastroenterol. 2015 Sep 28;21(36):10475-9. doi: 10.3748/wjg.v21.i36.10475. PMID: 26420975 Free PMC Article10:Local release of masitinib alters in vivo implantable continuous glucose sensor performance. Avula M, Jones D, Rao AN, McClain D, McGill LD, Grainger DW, Solzbacher F.Biosens Bioelectron. 2016 Mar 15;77:149-56. doi: 10.1016/j.bios.2015.08.059. Epub 2015 Sep 14. PMID: 26402593