RPI-1

SKU: orb1223165

Description

RPI-1 is an ATP-dependent RET kinase inhibitor. Oral treatment with RPI-1 caused growth arrest or regression in 81% treated tumors. Following treatment suspension, tumor inhibition was maintained (51%, P<0.05, 100 days) and cures were achieved in 2/11 mice. In vivo effects of RPI-1 were reflected in activation of BAD, cleavage of caspases, apoptotic DNA fragmentation and inhibition of VEGF production observed in in vitro RPI-1-treated TT cells..

Key Properties

• CAS Number: 269730-03-2
• MW: 297.31
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₅NO₄
• SMILES: COc1c(cc2c(c1)/C(=C/c1ccc(cc1)O)/C(=O)N2)OC
• Target: AChR
• Solubility: In Vitro: DMSO : 125 mg/mL (420.44 mM)

Bioactivity

• In Vivo:
  RPI-1 (50, 100 mg/kg; p.o. ; twice a day for 10 days) inhibits the tumor growth of TT xenografts by 81%. Animal model: 8-to 11-week-old female athymic nude CD-1 mice (bearing TT cells). Dosage: 50, 100 mg/kg. Administration: p.o. ; twice a day for 10 days. Result: A dose-dependent effect on tumor growth was observed, with a dose of 2*50 mg/kg/day resulting in less tumor weight inhibition than the 2*100 mg/kg/day dose after 10 days of treatment.
• In Vitro:
  TPC-1 cells are sensitive to the growth inhibitory effect of RPI-1 with an IC50 of 5.1 μM, following 72 hours of treatment. RPI-1 (7.5-60 μM) inhibits Ret/Ptc1 autophosphorylation in TPC-1 cells. RPI-1 inhibitory effects in the TPC-1 cell culture conditions lead to inhibition of pathways involving JNK2 and AKT. The RPI-1 IC50 value for cell proliferation is 3.6 μM in NIH3T3 cells expressing the Ret mutant compared with 16 μM in non-transfected NIH3T3 cells, and that for colony formation in soft agar was 2.4 μM and 26 μM in RET mutant-transfected and H-RAS-transfected NIH3T3 cells, respectively. In NIH3T3 cells expressing the Ret mutant, Ret protein and tyrosine phosphorylation were undetectable after 24 hours of RPI-1 treatment. In TT cells, RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RPI-1 | RPI1 | RPI 1

Quick Database Links

Gene Symbol

AChR