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324832 EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem

The EGFR Inhibitor II, BIBX1382, also referenced under CAS 196612-93-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS

Primary Target: EGFR (ErbB-1, HER-1)
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324832
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
196612-93-8C₁₈H₁₉ClFN₇ • 2HCl • 2H₂O

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      Description
      OverviewA cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (10 mg/kg, daily, p.o.).
      Catalogue Number324832
      Brand Family Calbiochem®
      SynonymsN⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS
      References
      ReferencesSolca, F.F., et al. 2004. J. Pharm. Exp. Ther. 311, 502.
      Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun. 281, 25.
      Nuijen, B., et al. 2000. Int. J. Pharm. 194, 261.
      Product Information
      CAS number196612-93-8
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
      Chemical formulaC₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Application CommentsTocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months.
      Biological Information
      Primary TargetEGFR (ErbB-1, HER-1)
      Primary Target IC<sub>50</sub>3 nM against EGFR (ErbB-1, HER-1) in cell-free enzymatic reactions; 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells
      Purity≥97% 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 Irritant
      Storage +2°C to +8°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 3 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      324832-5MG 04055977215717

      Documentation

      EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      324832

      References

      Reference overview
      Solca, F.F., et al. 2004. J. Pharm. Exp. Ther. 311, 502.
      Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun. 281, 25.
      Nuijen, B., et al. 2000. Int. J. Pharm. 194, 261.
      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.

      Revision21-April-2011 JSW
      SynonymsN⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS
      DescriptionA cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (daily p.o. dose 10 mg/kg).
      FormYellow solid
      CAS number196612-93-8
      Chemical formulaC₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (25 mg/ml) or H₂O (1 mg/ml)
      CommentsTocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months.
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Irritant
      ReferencesSolca, F.F., et al. 2004. J. Pharm. Exp. Ther. 311, 502.
      Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun. 281, 25.
      Nuijen, B., et al. 2000. Int. J. Pharm. 194, 261.