RPI-1

RPI-1 - Names and Identifiers

Name	1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one
Synonyms	RPI-1 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one
CAS	269730-03-2

RPI-1 - Physico-chemical Properties

Molecular Formula	C17H15NO4
Molar Mass	297.31
Solubility	Soluble in DMSO
Storage Condition	2-8°C
Use	RPI-1 is a specific oral 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression and activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. It has anti-tumor activity.

RPI-1 - Reference

Reference

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