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RPI-1

本半岛bd体育手机客户端不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

269730-03-2

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

半岛bd体育手机客户端介绍

RPI-1 是一种特异性的口服 2-吲哚酮 Ret 酪氨酸激酶抑制剂。 RPI-1 抑制人甲状腺髓样癌 TT 细胞的增殖、Ret 酪氨酸磷酸化、Ret 蛋白表达以及 PLCgamma、ERK 和 AKT 的激活。抗肿瘤活性。

Cas No.	269730-03-2
化学名	1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one
Canonical SMILES	COC1=C(OC)C=C(/C(C(N2)=O)=C/C3=CC=C(O)C=C3)C2=C1
分子式	C₁₇H₁₅NO₄
分子量	279.3
溶解度	≤1mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端描述	RPI-1 is an ATP-dependent Ret tyrosine kinase and inhibitor [1]. RPI-1 also inhibits c-Met activation and expression [2]. The ret proto-oncogene encodes a receptor protein tyrosine kinase involved in the etiology of human tumors. RET loss of function mutations are associated with the development of Hirschsprung's disease, and gain of function mutations are associated with the development of various types of human cancer, including medullary thyroid carcinoma, multiple endocrine neoplasias, pheochromocytoma and parathyroid hyperplasia. In NIH3T3 fibroblasts expressing the Ret/ptc1 target tyrosine kinase (NIH3T3ptc1), RPI-1 preferentially inhibited the anchorage-independent growth with IC50 value of 0.97 μM [1]. In the N592 SCLC and H460 NSCLC cell lines, RPI-1 dose-dependently inhibited Met phosphorylation. In H460 cells, RPI-1 also inhibited HGF-induced Met tyrosine phosphorylation in a dose-dependent way [2]. In mice implanted s.c. with H460 cells, RPI-1 with 100 and 150 mg/kg significantly reduced the mean number of macroscopic lung metastases by 57% and 75%, respectively. In primary s.c. growing H460 tumors, RPI-1 exhibited significant antiangiogenic effect [2]. References: [1]. Lanzi C, Cassinelli G, Pensa T, et al. Inhibition of transforming activity of the ret/ptc1 oncoprotein by a 2-indolinone derivative. Int J Cancer. 2000 Feb 1;85(3):384-90. [2]. Cassinelli G, Lanzi C, Petrangolini G, et al. 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.