Masitinib mesylate - CAS 1048007-93-7
Catalog number: 1048007-93-7
Category: Inhibitor
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Masitinib mesylate is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
AB-1010; AB 1010; AB1010
Canonical SMILES:
1.The cKit Inhibitor, Masitinib, Prevents Diabetes-Induced Retinal Vascular Leakage.
Kim SR1, Im JE2, Jeong JH3, Kim JY2, Kim JT4, Woo SJ5, Sung JH6, Park SG1, Suh W2. Invest Ophthalmol Vis Sci. 2016 Mar 1;57(3):1201-6. doi: 10.1167/iovs.15-18065.
PURPOSE: Stem cell factor (SCF) has recently demonstrated activity as a novel endothelial permeability factor that contributes to the development of diabetes-induced hyperpermeable retinal vasculature. This study investigated the therapeutic potential of masitinib, a pharmacologic inhibitor of the SCF receptor cKit, for prevention of diabetes-induced breakdown of blood retinal barrier (BRB).
2.Local release of masitinib alters in vivo implantable continuous glucose sensor performance.
Avula M1, Jones D2, Rao AN3, McClain D2, McGill LD4, Grainger DW5, Solzbacher F6. Biosens Bioelectron. 2016 Mar 15;77:149-56. doi: 10.1016/j.bios.2015.08.059. Epub 2015 Sep 14.
Continuous glucose monitoring (CGM) sensors are often advocated as a clinical solution to improve long-term glycemic control in the context of diabetes. Subcutaneous sensor inflammatory response, fouling and fibrous encapsulation resulting from the host foreign body response (FBR) reduce sensor sensitivity to glucose, eventually resulting in sensor performance compromise and device failure. Several combination device strategies load CGM sensors with drug payloads that release locally to tissue sites to mitigate FBR-mediated sensor failure. In this study, the mast cell-targeting tyrosine kinase inhibitor, masitinib, was released from degradable polymer microspheres delivered from the surfaces of FDA-approved human commercial CGM needle-type implanted sensors in a rodent subcutaneous test bed. By targeting the mast cell c-Kit receptor and inhibiting mast cell activation and degranulation, local masitinib penetration around the CGM to several hundred microns sought to reduce sensor fibrosis to extend CGM functional lifetimes in subcutaneous sites.
3.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 J1, Lukesova S1,2, Kopecky J3, Grim J3, Papik Z4, Kolarova R4, Navratilova B5, Dubreuil P6,7, Agopian J7, Mansfield C7, Moussy A7, Hermine O7,8. 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.
BACKGROUND: Malignant melanoma in the gastrointestinal tract may be primary or metastatic. Mucosal melanoma is a quite rare and aggressive disease, growing hidden and diagnosed with a certain delay which makes treatment difficult.
4.Autoimmune-like hepatitis during masitinib therapy in an amyotrophic lateral sclerosis patient.
Salvado M1, Vargas V1, Vidal M1, Simon-Talero M1, Camacho J1, Gamez J1. World J Gastroenterol. 2015 Sep 28;21(36):10475-9. doi: 10.3748/wjg.v21.i36.10475.
We report a case of acute severe hepatitis resulting from masitinib in a young amyotrophic lateral sclerosis patient. Hepatotoxicity induced by masitinib, a tyrosine kinase inhibitor, is usually transient with mild elevation of transaminases, although acute hepatitis has been not reported to date. The hepatitis was resolved after masitinib was discontinued and a combination of prednisone and azathioprine was started. The transaminases returned to baseline normal values five months later. This is the first case in the hepatitis literature associated with masitinib. The autoimmune role of this drug-induced liver injury is discussed. Physicians should be aware of this potential complication.
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CAS 1048007-93-7 Masitinib mesylate

Masitinib mesylate
(CAS: 1048007-93-7)

Masitinib mesylate is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.

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CAS 1048007-93-7 Masitinib mesylate

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