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

328011
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      328011-10MG
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          Glass bottle 10 mg
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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
          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

          Documentation

          Certificates of Analysis

          TitleLot Number
          328011

          References

          Reference overview
          Ercan, D., et al. 2012. Cancer Discovery 2, 934.
          Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.
          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.

          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 +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 Standard Handling
          ReferencesErcan, D., et al. 2012. Cancer Discovery 2, 934.
          Aronov, A.M., et al. 2009. J. Med. Chem. 52, 6362.