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.

• 別名: 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
• 実験式（ヒル表記法）: C₂₄H₂₇ClN₆O₃ · xHCl
• CAS番号: 944341-54-2
• 分子量: 482.96 (free base basis)
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: beige
• 溶解性: DMSO: 25 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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