513033

PD 168393

A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC₅₀ = 700 pM).

• Synonyme(s) : PD 168393, 4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline
• Formule empirique (notation de Hill): C₁₇H₁₃BrN₄O
• Numéro CAS: 194423-15-9
• Poids moléculaire : 369.22
• Numéro MDL: MFCD02179207
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 200 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22)
• Clé InChI: HTUBKQUPEREOGA-UHFFFAOYSA-N

Description

Description générale

A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC₅₀ = 0.70 nM). Does not inhibit other protein kinases. Acts by binding to the catalytic domain of the EGFR with a 1:1 stoichiometry and alkylating Cys⁷⁷³. Excellent antitumor agent in vivo.

A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC₅₀ = 700 pM). Does not inhibit other protein kinases. Acts by binding to the catalytic domain of the EGFR with a 1:1 stoichiometry and alkylating Cys⁷⁷³. Excellent antitumor agent in vivo.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
EGFR

Product competes with ATP.

Reversible: no

Target IC₅₀: 700 pM against EGFR

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Avoid freeze/thaw cycles of solutions.

Autres remarques

Fry, D.W., et al. 1998. Proc. Natl. Acad. Sci USA 95, 12022.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable