计算溶液所需的质量、体积或浓度。
为什么选择此级别
，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 7 篇同行评审文献引用。
概述
Imatinib Mesylate (STI571)是Imatinib的甲磺酸盐，具有较好的口服生物利用度，是一种多靶点的抑制剂，同时作用于v-Abl， c-Kit和PDGFR，IC50分别为0.6 μM， 0.1 μM 和0.1 μM。A c-Abl, PDGFR, and c-kit inhibitor
Information
Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor ofv-Abl,c-KitandPDGFRwithIC50of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib M
In vitro
In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis.
In vivo
Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation.
Cell Data
cell lines：
Concentrations：~100 μM
Incubation Time：48 hours
Powder Purity:≥99%
规格
英文别名
Gleevec, Glivec, CGP-57148B | N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonic acid
规格或纯度
10mM in DMSO
英文名称
Imatinib (STI571) Mesylate
生化机理
甲磺酸伊马替尼（STI571，CGP057148B，格列卫）是伊马替尼的口服生物利用度甲磺酸盐，是v-Abl、c-Kit和PDGFR的多靶点抑制剂，在无细胞或基于细胞的试验中，IC50分别为0.6 μM、0.1 μM和0.1 μM。甲磺酸伊马替尼（STI571）诱导自噬。
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
干细胞生长因子受体抑制剂
名称和识别符
EC号
606-892-3
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=CC(=N4)C5=CN=CC=C5.CS(=O)(=O)O
分子量
589.71
Reaxy-Rn
10229624
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10229624&ln=
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 47 mg/mL (198.89 mM); Ethanol: 47 mg/mL (198.89 mM); Water: 15 mg/mL (63.47 mM);
安全和危险性（GHS）
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:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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