Imatinib;STI571

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抑制剂描述：

产品名称：Imatinib

产品别名：伊马替尼

英文别名：STI571

靶点：PDGFR ,c-Kit ,v-Abl

CAS：152459-95-5

纯度：＞98%

外观：微黄色至白色结晶性粉末

保存方法：﹣20℃冷藏长期储存。冰袋运输

描述：

Imatinib (STI571)是一种多靶点酪氨酸激酶抑制剂，作用于v- v-Abl， c-Kit和PDGFR 时，IC50分别为0.6， 0.1和0.1 μM。

溶解性：DMSO : 30 mg/mL (60.1 mM)

体外研究：

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.

体内研究：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.

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