269730-03-2
269730-03-2 structure
- Name: RPI-1
- Chemical Name: 2H-Indol-2-one, 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy
- CAS Number: 269730-03-2
- Molecular Formula: C17H15NO4
- Molecular Weight: 297.305
- Catalog: Research Areas Cancer
- Create Date: 2017-06-04 04:29:55
- Modify Date: 2024-01-31 13:24:30
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RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity[1].
| Name | 2H-Indol-2-one, 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy |
|---|---|
| Synonyms |
(3Z)-3-(4-Hydroxybenzylidene)-5,6-dimethoxy-1,3-dihydro-2H-indol-2-one
1,3-dihydro-5,6-dimethoxy-3-((4-hydroxyphenyl)methylene)-2H-indol-2-one 2H-Indol-2-one, 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-, (3Z)- RPI-1 |
| Description | RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity[1]. |
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| Related Catalog | |
| 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[1]. 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[2]. |
| 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%[2]. Animal Model: 8- to 11-week-old female athymic nude CD-1 mice (bearing TT cells)[2] 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*100mg/kg/day dose after 10 days of treatment. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 533.6±50.0 °C at 760 mmHg |
| Molecular Formula | C17H15NO4 |
| Molecular Weight | 297.305 |
| Flash Point | 276.5±30.1 °C |
| Exact Mass | 297.100098 |
| PSA | 67.79000 |
| LogP | 3.08 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Index of Refraction | 1.660 |
