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521231 PDGFR Tyrosine Kinase Inhibitor II - CAS 249762-74-1 - Calbiochem

521231
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₁H₁₈N₂O₃ 249762-74-1

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521231-1MGCN
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      塑膠安瓿;塑膠針藥瓶 1 mg
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      Description
      OverviewA cell-permeable bis(1H-2-indolyl)-1-methanone compound that acts as a highly selective, ATP-competitive and reversible inhibitor of platelet-derived growth factor (PDGF) receptor tyrosine kinase (IC50 = 1.1 µM in Swiss 3T3 cells for PDGFR). Also potently inhibits Flt3 (Fms-like tyrosine kinase 3) activity (IC50 = 6.2 µM for hPDGFβ-R-mFlt3 and 50 nM in EOL-1 cells). Sensitizes 32D cells to radiation-induced apoptosis and inhibits proliferation of TEL-Flt3-transfected BA/F3 cells (IC50 < 300 nM). May also serve as a prodrug form of the Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I (Cat. No. 521230) in cells.
      Catalogue Number521231
      Brand Family Calbiochem®
      Synonyms(5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone, [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate, D-65476
      References
      ReferencesMahboobi, S., et al. 2002. J. Med. Chem. 45, 1002.
      Teller, S., et al. 2002. Leukemia 16, 1528.
      Product Information
      CAS number249762-74-1
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₂₁H₁₈N₂O₃
      Chemical formulaC₂₁H₁₈N₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPDGFR in swiss 3T3 cells
      Primary Target IC<sub>50</sub>1.1 µM inhibiting PDGFR in swiss 3T3 cells; 6.2 µ M for hPDGFβ-R-mFlt3 and 50 nM in EOL-1 cells
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PDGFR Tyrosine Kinase Inhibitor II - CAS 249762-74-1 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      PDGFR Tyrosine Kinase Inhibitor II - CAS 249762-74-1 - Calbiochem Certificates of Analysis

      TitleLot Number
      521231

      References

      Reference overview
      Mahboobi, S., et al. 2002. J. Med. Chem. 45, 1002.
      Teller, S., et al. 2002. Leukemia 16, 1528.
      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.

      Revision12-January-2010 RFH
      Synonyms(5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone, [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate, D-65476
      DescriptionProdrug form of Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I (Cat. No. 521230) that acts as a highly selective, cell-permeable, ATP-competitive, and reversible inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine kinase (IC50 = 1.1 µM, Swiss 3T3 cells). Also potently inhibits Fms-like tyrosine kinase 3 (Flt3) activity (IC50 = 6.2 µM for PDGFRβ-mFlt3 and 50 nM in EOL-1 cells). Reported to sensitize 32D cells to radiation-induced apoptosis. Also shown to inhibit proliferation of TEL-Flt3-transfected BA/F3 cells (IC50 > 300 nM).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number249762-74-1
      Chemical formulaC₂₁H₁₈N₂O₃
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesMahboobi, S., et al. 2002. J. Med. Chem. 45, 1002.
      Teller, S., et al. 2002. Leukemia 16, 1528.