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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.

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

554340
  
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Overview

Replacement Information

Key Spec 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
Catalogue Number GTIN
554340 0

Documentation

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

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.