428205 Lck Inhibitor - CAS 213743-31-8 - Calbiochem

428205
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₂₃H₂₂N₄O 213743-31-8

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428205-1MG
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      Description
      OverviewA cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC50 at 5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC50 = 3.2 µM, > 33 µM, > 50 µM and > 50 µM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells) and in vivo (ED50 = 4 mg/kg in mice, ip.)
      Catalogue Number428205
      Brand Family Calbiochem®
      Synonyms4-Amino-5-(4-phenoxyphenyl)-7H-pyrrolo[3,2-d]pyrimidin-7-yl-cyclopentane
      References
      ReferencesBurchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171.
      Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.
      Product Information
      CAS number213743-31-8
      ATP CompetitiveY
      FormWhite solid
      Hill FormulaC₂₃H₂₂N₄O
      Chemical formulaC₂₃H₂₂N₄O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetLck₆₄₋₅₀₉ Y³⁹⁴
      Primary Target IC<sub>50</sub>At5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk
      Purity≥95% 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 Harmful
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Lck Inhibitor - CAS 213743-31-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Lck Inhibitor - CAS 213743-31-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      428205

      References

      Reference overview
      Burchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171.
      Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.
      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
      Synonyms4-Amino-5-(4-phenoxyphenyl)-7H-pyrrolo[3,2-d]pyrimidin-7-yl-cyclopentane
      DescriptionA cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC50 at 5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC50 = 3.2 µM, > 33 µM, > 50 µM and > 50 µM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells) and in vivo (ED50 = 4 mg/kg in mice, ip.)
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number213743-31-8
      Chemical formulaC₂₃H₂₂N₄O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (17 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 6 months at -20°C.
      Toxicity Harmful
      ReferencesBurchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171.
      Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.