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抑制劑描述：

產(chǎn)品名稱：Imatinib

產(chǎn)品別名：伊馬替尼

英文別名：STI571

靶點：PDGFR ,c-Kit ,v-Abl

CAS：152459-95-5

純度：＞98%

外觀：微黃色至白色結(jié)晶性粉末

保存方法：﹣20℃冷藏長期儲存。冰袋運輸

描述：

Imatinib (STI571)是一種多靶點酪氨酸激酶抑制劑，作用于v- v-Abl， c-Kit和PDGFR 時，IC50分別為0.6， 0.1和0.1 μM。

溶解性：DMSO : 30 mg/mL (60.1 mM)

體外研究：

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.

體內(nèi)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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