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

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Key Spec Table

CAS #Empirical Formula
213743-31-8C₂₃H₂₂N₄O

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428205-1MG
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      Kst.-Ampulle 1 mg
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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
      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
      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
      Global Trade Item Number
      Bestellnummer GTIN
      428205-1MG 04055977210071