RPI-1 |
| Catalog No.GC13194 |
RPI-1 est un inhibiteur spécifique de la 2-indolinone Ret tyrosine kinase disponible par voie orale. RPI-1 inhibe la prolifération, la phosphorylation de la tyrosine Ret, l'expression de la protéine Ret et l'activation de PLCgamma, ERK et AKT dans les cellules TT du carcinome médullaire de la thyroÏde humaine. Activité antitumorale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 269730-03-2
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 269730-03-2 | SDF | |
| Chemical Name | 1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one | ||
| Canonical SMILES | COC1=C(OC)C=C(/C(C(N2)=O)=C/C3=CC=C(O)C=C3)C2=C1 | ||
| Formula | C17H15NO4 | M.Wt | 279.3 |
| Solubility | ≤1mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5804 mL | 17.9019 mL | 35.8038 mL |
| 5 mM | 0.7161 mL | 3.5804 mL | 7.1608 mL |
| 10 mM | 0.358 mL | 1.7902 mL | 3.5804 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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