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

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Sinónimos: VX-11e, (S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide

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
      Applications
      Biological Information
      Primary TargetERK
      Purity≥98% by Chiral 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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Número de referencia GTIN
      328011-10MG 04055977195620

      Documentation

      Referencias bibliográficas

      Visión general referencias
      Ercan, D., et al. 2012. Cancer Discovery 2, 934.
      Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.
      Ficha técnica

      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.

      Revision10-May-2013 JSW
      SynonymsVX-11e, (S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide
      DescriptionA 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 be orally available in both mice (F = 67%; t1/2 = 4.4 h; Plasma conc. = 488 and 122 ng/mL, respectively, 4 h and 8 h post single 33 mg/kg oral dosage) and rats (F = 65%; t1/2 = 3 h; Plasma conc. = 329 and 267 ng/mL, respectively, 4 h and 8 h post single 10 mg/kg oral dosage) in vivo. Also reported to 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).
      FormYellowish-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number896720-20-0
      Chemical formulaC₂₄H₂₀Cl₂FN₅O₂
      Structure formulaStructure formula
      Purity≥98% by Chiral HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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 Standard Handling
      ReferencesErcan, D., et al. 2012. Cancer Discovery 2, 934.
      Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.