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328011 ERK Inhibitor VIII, VX-11e - CAS 896720-20-0 - Calbiochem

328011
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328011-10MG
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      Description
      OverviewA cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2 nM against Erk2; [ATP] = 65 µM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852 nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4 µM; IC50 ≥1 µM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48 nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100 nM WZ4002 with or without 1 µM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo.
      Catalogue Number328011
      Brand Family Calbiochem®
      SynonymsVX-11e, (S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide
      References
      ReferencesErcan, D., et al. 2012. Cancer Discovery 2, 934.
      Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.
      Product Information
      CAS number896720-20-0
      FormYellowish-white powder
      Hill FormulaC₂₄H₂₀Cl₂FN₅O₂
      Chemical formulaC₂₄H₂₀Cl₂FN₅O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetERK
      Purity≥98% by Chiral 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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      328011-10MG 04055977195620