324842

EGFR/ErbB-2/ErbB-4 Inhibitor II - CAS 944341-54-2 - Calbiochem

The EGFR/ErbB-2/ErbB-4 Inhibitor II, also referenced under CAS 944341-54-2, controls the biological activity of EGFR/ErbB-2/ErbB-4. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : EGFR/ErbB-2/ErbB-4 Inhibitor II - CAS 944341-54-2 - Calbiochem, (E)-4-Amino-6-(4-benzyloxy-3-chloro-phenylamino)-pyrimidine-5-carbaldehyde-O-(2-morpholin-4-yl-ethyl)-oxime, HCl, JNJ-28871063, HCl
• Formule empirique (notation de Hill): C₂₄H₂₇ClN₆O₃ · xHCl
• Numéro CAS: 944341-54-2
• Poids moléculaire : 482.96 (free base basis)
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: beige
• Solubilité: DMSO: 25 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

A cell-permeable aminopyrimidine oxime compound that potently inhibits EGFR/ErbB1/HER1, ErbB2/HER2/neu, and ErbB4/HER4 kinase activity (IC₅₀ = 22, 38 and 21 nM, respectively) in an ATP-competitive manner and effectively suppresses cellular receptor phosphorylation (IC₅₀ = 223 and 107 nM against basal HER2 and EGF-induced EFGR phosphorylation, respectively, in SKBR3 and A431 cultures) as well as HER2- and EGFR-dependent cancer cell proliferations (IC₅₀<1µM), while exhibiting much reduced or little activity against a panel of 202 other kniases. Reported to be orally available and blood-brain barrier permeant in both mice and rats and be efficacious in inhibiting tumor growth in several murine xenograft models (100 to 200 mg/kg/day, p.o.) in vivo.

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.

Autres remarques

Emanuel, S.L., et al. 2008. Mol. Pharmacol.73, 338.

Informations légales

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