1. Protein Tyrosine Kinase/RTK
  2. RET
  3. RPI-1

RPI-1 

Cat. No.: HY-101246
Handling Instructions

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.

For research use only. We do not sell to patients.

RPI-1 Chemical Structure

RPI-1 Chemical Structure

CAS No. : 269730-03-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
25 mg USD 200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

297.31

Formula

C₁₇H₁₅NO₄

CAS No.
SMILES

O=C1NC2=C(C=C(OC)C(OC)=C2)/C1=C/C3=CC=C(O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (420.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3635 mL 16.8175 mL 33.6349 mL
5 mM 0.6727 mL 3.3635 mL 6.7270 mL
10 mM 0.3363 mL 1.6817 mL 3.3635 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (7.00 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

RPI-1RPI1RPI 1REToraltyrosinekinaseproliferationphosphorylationmedullarythyroidcarcinomaTTcellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
RPI-1
Cat. No.:
HY-101246
Quantity:
MCE Japan Authorized Agent: