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

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      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
          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.