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

324832
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₁₉ClFN₇ • 2HCl • 2H₂O 196612-93-8

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      324832-5MG
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          Plastic ampoule 5 mg
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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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Brochure

          Title
          Biologics 33.1 ( 1.37 MB )
          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 +2°C to +8°C
          Hygroscopic
          Protect from light
          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.