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554340 RET Receptor Tyrosine Kinase Inhibitor - CAS 269730-03-2 - Calbiochem

The RET Receptor Tyrosine Kinase Inhibitor, also referenced under CAS 269730-03-2, controls the biological activity of RET Receptor Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1,3-Dihydro-5,6-dimethoxy-3-((4-hydroxyphenyl)methylene)-2H-indol-2-one, RPI-1

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      Overview

      Replacement Information

      Key Specifications Table

      CAS #Empirical Formula
      269730-03-2C₁₇H₁₅NO₄
      Description
      OverviewA cell-permeable, indolinone-based ATP-competitive tyrosine kinase inhibitor that is known to target Ret (IC50 = 170 nM), EGFR, and Met. Selectively reverts the morphologic phenotype of ret oncogene- (PTC1 & MEN2A), but not H-Ras-, transformed NIH3T3 in a reversible manner. RPI-1 effectively inhibits the autophosphorylation of PTC1, MEN2A, and Met (IC50 against Met Tyr1234/1235 in N592 ≤7.5 µM) in cancer cells, and concomitant receptor down-regulation has also been reported to occur in NIH3T3MEN2A and in small cell lung carcinoma cell line N592. Orally available in mice and is efficacious in inhibiting MEN2A- and Met-mediated tumorigenesis both in vitro (IC50 against NIH3T3MEN2A and TT proliferation = 3.6 and 7.2 µM, respectively) and in various murine xenograft models in vivo (50 to 150 mg/kg, b.i.d.).

      This product has been discontinued.
      Catalogue Number554340
      Brand Family Calbiochem®
      Synonyms1,3-Dihydro-5,6-dimethoxy-3-((4-hydroxyphenyl)methylene)-2H-indol-2-one, RPI-1
      References
      ReferencesRizzi, E., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3962.
      Cassinelli, G., et al. 2006. Mol. Cancer Ther. 5, 2388.
      Petrangolini, G., et al. 2006. Biochem. Pharmacol. 72, 405.
      Cuccuru, G., et al. 2004. J. Natl. Cancer Inst. 96, 1006.
      Lanzi, C., et al. 2000. Int. J. Cancer 85, 384.
      Product Information
      CAS number269730-03-2
      FormBrown solid
      Hill FormulaC₁₇H₁₅NO₄
      Chemical formulaC₁₇H₁₅NO₄
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C. Isomerization occurs slowly in solution, equilibrium concentration of E:Z is ~2:1 in DMSO after 10 days at room temperature.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      554340 0

      Documentation

      RET Receptor Tyrosine Kinase Inhibitor - CAS 269730-03-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      RET Receptor Tyrosine Kinase Inhibitor - CAS 269730-03-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      554340

      References

      Reference overview
      Rizzi, E., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3962.
      Cassinelli, G., et al. 2006. Mol. Cancer Ther. 5, 2388.
      Petrangolini, G., et al. 2006. Biochem. Pharmacol. 72, 405.
      Cuccuru, G., et al. 2004. J. Natl. Cancer Inst. 96, 1006.
      Lanzi, C., et al. 2000. Int. J. Cancer 85, 384.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision25-May-2011 RFH
      Synonyms1,3-Dihydro-5,6-dimethoxy-3-((4-hydroxyphenyl)methylene)-2H-indol-2-one, RPI-1
      DescriptionA cell-permeable, indolinone-based ATP-competitive tyrosine kinase inhibitor that is known to target Ret (IC50 = 170 nM), EGFR, and Met. Selectively reverts the morphologic phenotype of ret oncogene- (PTC1 & MEN2A), but not H-Ras-, transformed NIH3T3 in a reversible manner. RPI-1 effectively inhibits the autophosphorylation of PTC1, MEN2A, and Met (IC50 against Met Tyr1234/1235 in N592 ≤7.5 µM) in cancer cells, and concomitant receptor down-regulation has also been reported to occur in NIH3T3MEN2A and in small cell lung carcinoma cell line N592. Orally available in mice and is efficacious in inhibiting MEN2A- and Met-mediated tumorigenesis both in vitro (IC50 against NIH3T3MEN2A and TT proliferation = 3.6 and 7.2 µM, respectively) and in various murine xenograft models in vivo (50 to 150 mg/kg, b.i.d.).
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number269730-03-2
      Chemical formulaC₁₇H₁₅NO₄
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (25 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C. Isomerization occurs slowly in solution, equilibrium concentration of E:Z is ~2:1 in DMSO after 10 days at room temperature.
      Toxicity Standard Handling
      ReferencesRizzi, E., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3962.
      Cassinelli, G., et al. 2006. Mol. Cancer Ther. 5, 2388.
      Petrangolini, G., et al. 2006. Biochem. Pharmacol. 72, 405.
      Cuccuru, G., et al. 2004. J. Natl. Cancer Inst. 96, 1006.
      Lanzi, C., et al. 2000. Int. J. Cancer 85, 384.