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RPI-1

 
Catalog No.
C4239
ATP依赖性RET激酶抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 2,112.00
Ship with 10-15 days
10mg
¥ 3,412.00
Ship with 10-15 days
25mg
¥ 6,825.00
Ship with 10-15 days

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt279.3
Cas No.269730-03-2
FormulaC17H15NO4
Solubility≤1mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide
Chemical Name1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one
SDFDownload SDF
Canonical SMILESCOC1=C(OC)C=C(/C(C(N2)=O)=C/C3=CC=C(O)C=C3)C2=C1
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

质量控制

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批次:

化学结构

RPI-1