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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Masitinib (AB1010), 血小板衍生生长因子受体抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Masitinib (AB1010)是一种新型的Kit和PDGFRα/β抑制剂，IC50分别为200 nM和540 nM/800 nM，但对ABL和c-Fms抑制作用较弱。Phase 3A tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor.
Information
Masitinib is a novel inhibitor forKit (c-Kit)andPDGFRα/βwithIC50of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
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. In contrast, 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 IC50 of 150 nM, while the IC50 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 IC50 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 IC50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC50 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.
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 PO) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. The combination of masitinib/gemcitabine shows synergy in vitro on proliferation of gemcitabine-refractory cell lines Mia Paca2 and Panc1, and to a lesser extent on Mia Paca-2 pancreatic tumours in Nog璖CID mice.
Cell Data
cell lines：
Concentrations：0.1 nM - 10 μM
Incubation Time：48 hours
Powder Purity:≥99%
规格
别名
马赛替尼(AB1010)
英文别名
N-(4-methyl-3-(4-(pyridin-3-yl)thiazol-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Masitinib (AB1010)
生化机理
马西替尼是一种新型的Kit（c-Kit）和PDGFRα/β抑制剂，IC50为200 nM和540 nM/800 nM，对ABL和c-Fms的抑制作用较弱。第 3 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
血小板衍生生长因子受体抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC(=CS4)C5=CN=CC=C5
分子量
498.65
Reaxy-Rn
12083382
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12083382&ln=
技术文档
高级数据
产品属性
| ALogP | 4.3 |
|---|
关联靶点（人）
DDR2
Tchem
含盘状结构域受体 2(Discoidin domain-containing receptor 2)
(1 活性数据)
CSF1R
Tclin
巨噬细胞集落刺激因子 1 受体(Macrophage colony-stimulating factor 1 receptor)
(1 活性数据)
DDR1
Tchem
上皮盘状结构域受体 1(Epithelial discoidin domain-containing receptor 1)
(1 活性数据)
PDGFRA
Tclin
血小板衍生生长因子受体α(Platelet-derived growth factor receptor alpha)
(2 活性数据)
PDGFRB
Tclin
血小板衍生的生长因子受体β(Platelet-derived growth factor receptor beta)
(2 活性数据)
BCR
Tclin
断点簇区域蛋白质(Breakpoint cluster region protein)
(1 活性数据)
SLC25A6
Tchem
ADP/ATP转位酶3(ADP/ATP translocase 3)
(1 活性数据)
ACOX1
Tchem
过氧化物酶体酰基辅酶A氧化酶1(Peroxisomal acyl-coenzyme A oxidase 1)
(1 活性数据)
ABL1
Tclin
酪氨酸蛋白激酶ABL1(Tyrosine-protein kinase ABL1)
(7 活性数据)
KIT
Tclin
肥大细胞/干细胞生长因子受体试剂盒(Mast/stem cell growth factor receptor Kit)
(7 活性数据)
NQO2
Tchem
核糖二氢烟酰胺脱氢酶[醌](Ribosyldihydronicotinamide dehydrogenase [quinone])
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 76 mg/mL (301.3 mM); Ethanol: 15 mg/mL (59.46 mM); DMSO: 3 mg/mL (11.89 mM);
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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