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539652 PKCβII/EGFR Inhibitor - CAS 145915-60-2 - Calbiochem

539652
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₀H₁₃F₂N₃O₂ 145915-60-2

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539652-2MG
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      Plastic ampoule 2 mg
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      Description
      OverviewA cell-permeable symmetrical phthalimide compound that acts as a potent, reversible, and ATP-competitive inhibitor of EGFR and PKC isozymes α, βI, and βII (IC50 = 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM, respectively). Only weakly inhibits the activity of a panel of 16 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulin-stimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro. Also reported to exhibit antitumor activity in mice in vivo.
      Catalogue Number539652
      Brand Family Calbiochem®
      SynonymsCG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353
      References
      ReferencesKouroedov, A., et al. 2004. Circulation 110, 91.
      Lee, S.W., et al. 2003. Bone 32, 217.
      Perrotti, D., et al. 1998. EMBO J. 17, 4442.
      Chalfant, C.E., et al. 1996. Mol. Endocrinol. 10, 1273.
      Buchdunger, E., et al. 1995. Clin. Cancer Res. 1, 813.
      Trinks, U., et al. 1994. J. Med. Chem. 37, 1015.
      Product Information
      CAS number145915-60-2
      ATP CompetitiveY
      FormOrange solid
      Hill FormulaC₂₀H₁₃F₂N₃O₂
      Chemical formulaC₂₀H₁₃F₂N₃O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetEGFR
      Primary Target IC<sub>50</sub>0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM against EGFR and PKC isozymes α, βI, and βII, 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

      PKCβII/EGFR Inhibitor - CAS 145915-60-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PKCβII/EGFR Inhibitor - CAS 145915-60-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      539652

      References

      Reference overview
      Kouroedov, A., et al. 2004. Circulation 110, 91.
      Lee, S.W., et al. 2003. Bone 32, 217.
      Perrotti, D., et al. 1998. EMBO J. 17, 4442.
      Chalfant, C.E., et al. 1996. Mol. Endocrinol. 10, 1273.
      Buchdunger, E., et al. 1995. Clin. Cancer Res. 1, 813.
      Trinks, U., et al. 1994. J. Med. Chem. 37, 1015.

      Brochure

      Title
      PKC Pathway Poster PDF ( 676 KB )
      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.

      Revision11-January-2010 RFH
      SynonymsCG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353
      DescriptionA cell-permeable, potent, ATP-competitive, and reversible inhibitor of EGFR and PKC isozymes α, βI, and βII (IC50 = 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM, respectively). Only weakly inhibits the activity of a panel of 16 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulin-stimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro. Also reported to exhibit antitumor activity in mice in vivo.
      FormOrange solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number145915-60-2
      Chemical formulaC₂₀H₁₃F₂N₃O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (20 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
      ReferencesKouroedov, A., et al. 2004. Circulation 110, 91.
      Lee, S.W., et al. 2003. Bone 32, 217.
      Perrotti, D., et al. 1998. EMBO J. 17, 4442.
      Chalfant, C.E., et al. 1996. Mol. Endocrinol. 10, 1273.
      Buchdunger, E., et al. 1995. Clin. Cancer Res. 1, 813.
      Trinks, U., et al. 1994. J. Med. Chem. 37, 1015.