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Imatinib
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产品介绍
产品介绍
产品信息
抗原名称
PDGFR ,c-Kit ,v-Abl
商品描述
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。
分子量
493.6
纯度
＞98%
可溶性
DMSO : 30 mg/mL (60.1 mM)
外观
微黄色至白色结晶性粉末
In vitro(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.
In vivo(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.
背景
别名
伊马替尼；STI571
分子式
C29H31N7O
CAS号
152459-95-5
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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