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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 & Dephosphoryl

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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

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
      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.
      Global Trade Item Number
      Catalogue Number GTIN
      324832-5MG 04055977215717