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

The PDGFR Tyrosine Kinase Inhibitor II, also referenced under CAS 249762-74-1, controls the biological activity of PDGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphoryl

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Synonyms: (5-Butanoate-1H-2-indolyl)(1H-2-indolyl)-methanone, [2-(1H-2-Indolylcarbonyl)-1H-5-indolyl]butanoate, D-65476

Primary Target: PDGFR in swiss 3T3 cells
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521231
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Overview

Key Spec Table

CAS #Empirical Formula
249762-74-1C₂₁H₁₈N₂O₃

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521231-1MG
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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
      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
      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
      Global Trade Item Number
      Catalogue Number GTIN
      521231-1MG 04055977271355