Masitinib mesylate

Dangerous Goods

CAS number：1048007-93-7 molecular formula：C29H34N6O4S2

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compound introduction

Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit ( IC 50 =200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β ( IC 50 s=540/800 nM), Lyn ( IC 50 = 510 nM for LynB), Lck , and, to a lesser extent, FGFR3 and FAK . Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity. In Vitro 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. 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 IC 50 of 150 nM, while the IC 50 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 IC 50 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 IC 50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Masitinib inhibits tumour growth and increases the median survival time in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity or genotoxicity . ? Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 200 nM (Kit), 540 nM (PDGFRα), 800 nM (PDGFRβ), 510 nM (LynB)

Specs

Chinese alias	甲磺酸马赛替尼
English alias	A927557 \| Masitinib Mesylate Salt; Masitinib mesilate;AB 1010 Mesylate pound>>AB1010 Mesylate pound>>AB-1010 Mesylate \| OXYBUTYNIN [MI] \| 4-((4-Methylpiperazin-1-yl)methyl)-N-(4-methyl-3-((4-pyridin-3-yl-1,3-thiazol-2-yl)amino)phenyl)benzamide methanesulp
CAS number	1048007-93-7	molecular formula	C29H34N6O4S2
molecular weight	594.8 g/mol	Exact mass	≥99%
PSA	164.000 Å²	logp	-

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Safety information

pictogram：

GHS08 , GHS07

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Hazard Statement：

H351: 怀疑引起遗传缺陷 H302: 吞食有害 H361: 怀疑破坏生育力或未出生的孩子

Statement of Preventive Measures：

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P203: 使用前，获取、阅读并遵守所有安全说明。 P301+P317: 如果被吞咽：请寻求医疗帮助。 P318: 如果暴露或担心，请就医。