中文名 | RPI-1 |
英文名 | 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one |
英文别名 | RPI-1 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one |
CAS | 269730-03-2 |
化学式 | C17H15NO4 |
分子量 | 297.31 |
溶解度 | 溶于DMSO |
存储条件 | 2-8°C |
产品用途 | RPI-1 是一种特异的口服 2-吲哚啉酮 Ret 酪氨酸激酶抑制剂。RPI-1 抑制人甲状腺髓样癌 TT 细胞增殖、Ret 酪氨酸磷酸化、Ret 蛋白表达及 PLCgamma、ERKs 和 AKT 的活化。具有抗肿瘤活性。 |
参考资料 展开查看 | 1: Caccia D, Miccichè F, Cassinelli G, Mondellini P, Casalini P, Bongarzone I. Dasatinib reduces FAK phosphorylation increasing the effects of RPI-1 inhibition in a RET/PTC1-expressing cell line. Mol Cancer. 2010 Oct 18;9:278. doi: 10.1186/1476-4598-9-278. PubMed PMID: 20955590; PubMed Central PMCID: PMC2967544. 2: Cassinelli G, Lanzi C, Petrangolini G, Tortoreto M, Pratesi G, Cuccuru G, Laccabue D, Supino R, Belluco S, Favini E, Poletti A, Zunino F. Inhibition of c-Met and prevention of spontaneous metastatic spreading by the 2-indolinone RPI-1. Mol Cancer Ther. 2006 Sep;5(9):2388-97. PubMed PMID: 16985073. 3: Petrangolini G, Cuccuru G, Lanzi C, Tortoreto M, Belluco S, Pratesi G, Cassinelli G, Zunino F. Apoptotic cell death induction and angiogenesis inhibition in large established medullary thyroid carcinoma xenografts by Ret inhibitor RPI-1. Biochem Pharmacol. 2006 Aug 14;72(4):405-14. PubMed PMID: 16756963. 4: Cuccuru G, Lanzi C, Cassinelli G, Pratesi G, Tortoreto M, Petrangolini G, Seregni E, Martinetti A, Laccabue D, Zanchi C, Zunino F. Cellular effects and antitumor activity of RET inhibitor RPI-1 on MEN2A-associated medullary thyroid carcinoma. J Natl Cancer Inst. 2004 Jul 7;96(13):1006-14. PubMed PMID: 15240784. 5: Lanzi C, Cassinelli G, Cuccuru G, Zaffaroni N, Supino R, Vignati S, Zanchi C, Yamamoto M, Zunino F. Inactivation of Ret/Ptc1 oncoprotein and inhibition of papillary thyroid carcinoma cell proliferation by indolinone RPI-1. Cell Mol Life Sci. 2003 Jul;60(7):1449-59. Pu |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.363 ml | 16.817 ml | 33.635 ml |
5 mM | 0.673 ml | 3.363 ml | 6.727 ml |
10 mM | 0.336 ml | 1.682 ml | 3.363 ml |
5 mM | 0.067 ml | 0.336 ml | 0.673 ml |
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