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233100 CL-387,785 - CAS 194423-06-8 - Calbiochem

A cell-permeable and irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC₅₀ = 250-490 pM) as well as EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo (IC₅₀ = 5 nM).

CL-387,785 - CAS 194423-06-8 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide, EKI-785

Primary Target: EGFR kinase activity
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233100
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
194423-06-8C₁₈H₁₃BrN₄O

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      Description
      OverviewA cell-permeable and irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM) as well as EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo (IC50 = 5 nM). Blocks EGF-mediated growth in A431 cells. Inhibits proliferation of EGFR or c-ErbB2 expressing cells (IC50 = 31-125 nM) by covalently binding to the EGFR.
      Catalogue Number233100
      Brand Family Calbiochem®
      SynonymsN-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide, EKI-785
      References
      ReferencesSweeney, W.E., et al. 2000. Kidney Int. 57, 33.
      Discafani, C.M., et al. 1999. Biochem. Pharmacol. 57, 917.
      Sweeney, W.E., et. al. 1999. Kidney Int. 56, 406.
      Product Information
      CAS number194423-06-8
      ATP CompetitiveN
      FormPale yellow solid
      Hill FormulaC₁₈H₁₃BrN₄O
      Chemical formulaC₁₈H₁₃BrN₄O
      Hygroscopic Hygroscopic
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetEGFR kinase activity
      Primary Target IC<sub>50</sub>250-490 pM inhibiting EGF-receptor (EGFR) kinase activity in vivo; 5 nM inhibiting EGF-stimulated autophosphorylation of tyrosine residues in the EGFR in vivo
      Purity≥95% 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 -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      233100-1MGCN 04055977217612

      Documentation

      CL-387,785 - CAS 194423-06-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      CL-387,785 - CAS 194423-06-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      233100

      References

      Reference overview
      Sweeney, W.E., et al. 2000. Kidney Int. 57, 33.
      Discafani, C.M., et al. 1999. Biochem. Pharmacol. 57, 917.
      Sweeney, W.E., et. al. 1999. Kidney Int. 56, 406.
      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.

      Revision05-April-2011 RFH
      SynonymsN-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide, EKI-785
      DescriptionA cell-permeable and irreversible inhibitor of EGF-stimulated autophosphorylation of tyrosine residues in the epidermal growth factor receptor (EGFR) in vivo (IC50 = 250-490 pM) and blocks EGF-mediated growth. Also inhibits proliferation of cells that overexpress EGFR or c-Erb-2 (IC50 = 31-125 nM) by covalently binding to EGFR.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number194423-06-8
      Chemical formulaC₁₈H₁₃BrN₄O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (200 mg/ml)
      Storage Protect from light
      -20°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
      Toxicity Standard Handling
      ReferencesSweeney, W.E., et al. 2000. Kidney Int. 57, 33.
      Discafani, C.M., et al. 1999. Biochem. Pharmacol. 57, 917.
      Sweeney, W.E., et. al. 1999. Kidney Int. 56, 406.