324674

EGFR Inhibitor

The EGFR Inhibitor, also referenced under CAS 879127-07-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: EGFR Inhibitor, Cyclopropanecarboxylic acid-(3-(6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino)-phenyl)-amide
• 実験式（ヒル表記法）: C₂₁H₁₈F₃N₅O
• CAS番号: 879127-07-8
• 分子量: 413.40
• MDL番号: MFCD13191284
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: ethanol: 25 mg/mL; DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• SMILES記法: FC(F)(F)c1cc(ccc1)Nc2ncnc(c2)Nc3cc(ccc3)NC(=O)C4CC4
• InChI: 1S/C21H18F3N5O/c22-21(23,24)14-3-1-4-15(9-14)27-18-11-19(26-12-25-18)28-16-5-2-6-17(10-16)29-20(30)13-7-8-13/h1-6,9-13H,7-8H2,(H,29,30)(H2,25,26,27,28)
• InChI Key: YOHYSYJDKVYCJI-UHFFFAOYSA-N

詳細

詳細

A cell-permeable 4,6-dianilinopyrimidine compound that acts as a potent, ATP-competitive, and highly selective inhibitor of EGFR and some EGFR mutants (IC₅₀ = 21 nM, 63 nM, and 4 nM for EGFRwt, EGFR^L858R and EGFR^L861Q, respectively) vs. erbB4/Her4 (IC₅₀ = 7.64 µM) and a panel of 55 other kinases. Shown to completely block EGF-induced EGFR autophosphorylation in U-2OS cells at 10 µM.

生物化学的／生理学的作用

Cell permeable: yes

Product competes with ATP.

Reversible: no

Target IC₅₀: 21 nM, 63 nM, and 4 nM for EGFRwt, EGFRL858R and EGFRL861Q, respectively

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

Zhang, Q., et al. 2006. J. Am. Chem. Soc.128, 2182

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable