RPI-1 Property

storage temp. 

Sealed in dry,2-8°C

solubility 

DMSO: >20mg/mL

form 

powder to crystal

color 

orange

Safety

Hazard Codes 

N

Risk Statements 

50/53

Safety Statements 

60-61

HS Code 

2933.79.1500

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

RPI-1 Chemical Properties,Usage,Production

Uses

RPI-?1 is RET kinase inhibitor. It can be used in biological study of composition and function of mutant Swi?/Snf complexes. It can also be used in biological study of proteomics study of medullary thyroid carcinomas expressing RET germ-line mutations and identification of new signaling elements.

Biological Activity

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.