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

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513035-500UG
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      Plastic ampoule 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 ImageStructure formula Image
      Quality LevelMQ100
      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

      PD 158780 - CAS 171179-06-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PD 158780 - CAS 171179-06-9 - Calbiochem 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 formulaStructure 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.