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513035 | PD 158780 - CAS 171179-06-9 - Calbiochem

513035
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₄H₁₂BrN₅ 171179-06-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      513035-500UG
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          Glass bottle 500 μg
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          Description
          OverviewA potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC50 = 8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC50 = 49 nM) and MDA-MB-453 (IC50 = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGFR tyrosine phosphorylation in HeLa and NIH 3T3 cells. A 10 mM (500 µg/151 µl) solution of PD 158780 (Cat. No. 513036) in DMSO is also available.
          Catalogue Number513035
          Brand Family Calbiochem®
          Synonyms4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine
          References
          ReferencesCunnick, J.M., et al. 1998. J. Biol. Chem. 273, 14468.
          Rewcastle, G.W., et al. 1998. J. Med. Chem. 41, 742.
          Product Information
          CAS number171179-06-9
          ATP CompetitiveY
          FormYellow solid
          Hill FormulaC₁₄H₁₂BrN₅
          Chemical formulaC₁₄H₁₂BrN₅
          ReversibleY
          Structure formula Image
          Applications
          Biological Information
          Primary TargetEGFR tyrosine kinase
          Primary Target IC<sub>50</sub>8 pM against EGFR tyrosine kinase activity; 49 nM, 52 nm, against heregulin-stimulated autophosphorylation in SK-BR-3 and MDA-MB-453 breast carcinomas, respectively
          Purity≥95% 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 -20°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze at -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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          513035

          References

          Reference overview
          Cunnick, J.M., et al. 1998. J. Biol. Chem. 273, 14468.
          Rewcastle, G.W., et al. 1998. J. Med. Chem. 41, 742.
          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.

          Revision12-January-2010 RFH
          Synonyms4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine
          DescriptionA potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC50 = 8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC50 = 49 nM) and MDA-MB-453 (IC50 = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase ½ (MKK½) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells.
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number171179-06-9
          Chemical formulaC₁₄H₁₂BrN₅
          Structure formula
          Purity≥95% by HPLC
          SolubilityDMSO (5 mg/ml)
          Storage -20°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesCunnick, J.M., et al. 1998. J. Biol. Chem. 273, 14468.
          Rewcastle, G.W., et al. 1998. J. Med. Chem. 41, 742.