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.

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₄H₂₇ClN₆O₃ · xHCl
• CAS-Nummer: 944341-54-2
• Molekulargewicht: 482.96 (free base basis)
• UNSPSC-Code: 12352200

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic); protect from light
• Farbe: beige
• Löslichkeit: DMSO: 25 mg/mL
• Versandbedingung: ambient
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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