234490

PD 153035

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀ = 25 pM; K_i = 6 pM).

• Synonyme(s) : PD 153035, AG 1517, 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline, SU 5271, Compound 32
• Formule empirique (notation de Hill) : C₁₆H₁₄BrN₃O₂
• CAS Number: 153436-54-5
• Poids moléculaire : 360.21
• Numéro MDL: MFCD00934896
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥97% (HPLC)
• Forme: solid
• Puissance: 25 pM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• Chaîne SMILES: Brc1cc(ccc1)Nc2ncnc3c2cc(c(c3)OC)OC
• InChI: 1S/C16H14BrN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
• Clé InChI: LSPANGZZENHZNJ-UHFFFAOYSA-N

Description

Description générale

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀ = 25 pM; K_i = 6 pM). Rapidly suppresses autophosphorylation of EGFR at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells. Also selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. A 10 mM (500 µg/139 µl) solution of PD 153035 (Cat. No. 234491) in DMSO is also available.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
EGFR

Product competes with ATP.

Reversible: yes

Target K_i: 6 pM against epidermal growth factor receptor (EGFR)

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Bridges, A.J., et al. 1996. J. Med. Chem. 39, 267.
Fry, D.W., et al. 1994. Science265, 1093.

Informations légales

Sold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.

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 1