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

A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC₅₀ = 8 pM).

PD 158780 - CAS 171179-06-9 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-[(3-Bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyridimine

Primary Target: EGFR tyrosine kinase
513035
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
171179-06-9C₁₄H₁₂BrN₅

Products

Catalogue NumberPackaging Qty/Pack
513035-500UG Plastová ampulka 500 μg
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
Global Trade Item Number
Catalogue Number GTIN
513035-500UG 04055977198645

Documentation

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

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 Protect from light
-20°C
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.