Masitinib mesylate
作者：齊岳
發布時間：2023-08-25
08:58:42
點擊數：
產品名稱：Masitinib mesylate
產品描述：
| 產品描述 | Masitinib 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). |
| 靶點活性 | PDGFRβ:800 nM , PDGFRα:540 nM , Kit:200 nM , LynB:510 nM |
| 體外活性 | 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]. |
| 體內活性 | Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs[2] |
| 別名 | 甲磺酸馬賽替尼, AB-1010 mesylate, 馬賽替尼 |
| 分子量 | 594.75 |
| 分子式 | C29H34N6O4S2 |
| CAS No. | 1048007-93-7 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 25 mg/mL (42.03 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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