RPI-1 (CAS 269730-03-2)
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RPI-1 is a cell-permeable, indolinone-based ATP-competitive tyrosine kinase inhibitor that is known to target Ret, EGFR, and Met. Increased tumorigenicity, motility, and invasiveness have been described as biological consequences of HGF/Met deregulation in tumor cells, thus RPI-1 treatment of H460 cells resulted in a strong reduction of both colony number and size. The compound is also active at mouse NSCLC H460 xenograft tumor and metastasis model. Mechanistically RPI-1 inhibits Met phosphorylation at Tyr1234/Tyr1235, known to activate the intrinsic kinase activity. Selectively reverts the morphologic phenotype of ret oncogene- (PTC1 MEN2A), but not H-Ras-, and transformed NIH3T3 in a reversible manner. RPI-1 effectively inhibits the autophosphorylation of PTC1, MEN2A, and Met against Met in N592 in cancer cells, and concomitant receptor down-regulation has also been reported to occur in NIH3T3MEN2A and in small cell lung carcinoma cell line N592.
RPI-1 (CAS 269730-03-2) References
- Inactivation of Ret/Ptc1 oncoprotein and inhibition of papillary thyroid carcinoma cell proliferation by indolinone RPI-1. | Lanzi, C., et al. 2003. Cell Mol Life Sci. 60: 1449-59. PMID: 12943231
- Cellular effects and antitumor activity of RET inhibitor RPI-1 on MEN2A-associated medullary thyroid carcinoma. | Cuccuru, G., et al. 2004. J Natl Cancer Inst. 96: 1006-14. PMID: 15240784
- Apoptotic cell death induction and angiogenesis inhibition in large established medullary thyroid carcinoma xenografts by Ret inhibitor RPI-1. | Petrangolini, G., et al. 2006. Biochem Pharmacol. 72: 405-14. PMID: 16756963
- Inhibition of c-Met and prevention of spontaneous metastatic spreading by the 2-indolinone RPI-1. | Cassinelli, G., et al. 2006. Mol Cancer Ther. 5: 2388-97. PMID: 16985073
- Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones. | Rizzi, E., et al. 2007. Bioorg Med Chem Lett. 17: 3962-8. PMID: 17499504
- Proteomics study of medullary thyroid carcinomas expressing RET germ-line mutations: identification of new signaling elements. | Gorla, L., et al. 2009. Mol Carcinog. 48: 220-231. PMID: 18756447
- Dasatinib reduces FAK phosphorylation increasing the effects of RPI-1 inhibition in a RET/PTC1-expressing cell line. | Caccia, D., et al. 2010. Mol Cancer. 9: 278. PMID: 20955590
- Interplay between Ret and Fap-1 regulates CD95-mediated apoptosis in medullary thyroid cancer cells. | Nicolini, V., et al. 2011. Biochem Pharmacol. 82: 778-88. PMID: 21741956
- Secretome compartment is a valuable source of biomarkers for cancer-relevant pathways. | Caccia, D., et al. 2011. J Proteome Res. 10: 4196-207. PMID: 21751813
- A protein tyrosine kinase receptor, c-RET signaling pathway contributes to the enteric neurogenesis induced by a 5-HT4 receptor agonist at an anastomosis after transection of the gut in rodents. | Goto, K., et al. 2015. J Physiol Sci. 65: 377-83. PMID: 25850922
- Proteomic Identification of DNA-PK Involvement within the RET Signaling Pathway. | Burdine, LJ., et al. 2015. PLoS One. 10: e0127943. PMID: 26065416
- GDNF secreted from adipose-derived stem cells stimulates VEGF-independent angiogenesis. | Zhong, Z., et al. 2016. Oncotarget. 7: 36829-36841. PMID: 27167204
- Cofilin is a mediator of RET-promoted medullary thyroid carcinoma cell migration, invasion and proliferation. | Giardino, E., et al. 2019. Mol Cell Endocrinol. 495: 110519. PMID: 31352037
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
RPI-1, 5 mg | sc-255524 | 5 mg | $153.00 | |||
RPI-1, 10 mg | sc-255524A | 10 mg | $186.00 |