328007 ERK Inhibitor II, FR180204 - CAS 865362-74-9 - Calbiochem

328007
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₁₃N₇ 865362-74-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      328007-1MG
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          Plastic ampoule 1 mg
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          Description
          OverviewA cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC50 = 510 nM and 330 nM; Ki = 310 nM and 140 nM, respectively). Exhibits ~20-fold greater selectivity over p38α (IC50 = 10 µM) and shows little activity towards IKKα, MEK1, MKK4, PDGFRα, PKCα, Src, and Syk even at concentrations as high as 30 µM. Shown to inhibit TGF-β−induced AP-1 activation in Mv1Lu epithelial cells (IC50 = 3.1 µM). ERK Inhibitor II, Negative Control is also available (Cat. No. 328008). Also available as a 10 mM solution in DMSO (Cat. No. 328010).
          Catalogue Number328007
          Brand Family Calbiochem®
          Synonyms5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
          References
          ReferencesOhori, M., et al. 2005. Biochem. Biophys. Res. Commun. 336, 357.
          Product Information
          CAS number865362-74-9
          ATP CompetitiveY
          FormYellow solid
          Hill FormulaC₁₈H₁₃N₇
          Chemical formulaC₁₈H₁₃N₇
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetERK1 and ERK2
          Primary Target IC<sub>50</sub>510 nM and 330 nM
          Primary Target K<sub>i</sub>310 nM and 140 nM, against ERK1 and ERK2, respectively
          Purity≥98% 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 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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          328007

          References

          Reference overview
          Ohori, M., et al. 2005. Biochem. Biophys. Res. Commun. 336, 357.
          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.

          Revision16-January-2012 RFH
          Synonyms5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
          DescriptionA cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC50 = 510 nM and 330 nM; Ki = 310 nM and 140 nM, respectively). Exhibits ~20-fold greater selectivity over p38α (IC50 = 10 µM) and shows little activity towards IKKα, MEK1, MKK4, PDGFRα, PKCα, Src, and Syk even at concentrations as high as 30 µM. Shown to inhibit TGF-β−induced AP-1 activation in Mv1Lu epithelial cells (IC50 of 3.1 µM). ERK Inhibitor II, Negative Control is also available (Cat. No. 328008). Also available in InSolution™ format (Cat. No. 328010).
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number865362-74-9
          Chemical formulaC₁₈H₁₃N₇
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (10 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
          ReferencesOhori, M., et al. 2005. Biochem. Biophys. Res. Commun. 336, 357.