甲磺酸马赛替尼 T8544

Product Introduction
Bioactivity


英文名: Masitinib mesylate

描述: Masitinib mesylate (AB-1010 mesylate) 是一种生物口服可利用的选择性 c-Kit 抑制剂，IC50 为 200 nM。它还抑制 PDGFRα/β，IC50值为540/800 nM，对 LynB 的 IC50为510 nM。它的毒性低，有抗增殖和促凋亡活性。

体外活性: 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].

体内活性: Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs[2]

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

溶解度: DMSO : 25 mg/mL (42.03 mM)


关键字: SCFR | PDGFR | c-Kit | Apoptosis | AB 1010 | AB 1010 Mesylate | Src | CD117 | Masitinib | Platelet-derived growth factor receptor | AB1010 | FGFR | Masitinib mesylate | Masitinib Mesylate | AB-1010 | Inhibitor | AB1010 Mesylate | Fibroblast growth factor receptor | inhibit | AB-1010 Mesylate

相关产品: Vincristine sulfate | CAY10505 | Maytansinol | Momelotinib | GSK-3β inhibitor 3 | K858 (Racemic) | Benzyl isothiocyanate | PU02 | Nitidine chloride | Rabeprazole sodium

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library

甲磺酸马赛替尼 T8544信息由TargetMol中国为您提供，如您想了解更多关于甲磺酸马赛替尼 T8544报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途