324877

Focal Adhesion Kinase Inhibitor I

The Focal Adhesion Kinase Inhibitor I, also referenced under CAS 4506-66-5, controls the biological activity of Foca Adhesion Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: Focal Adhesion Kinase Inhibitor I, FAK Inhibitor I, 1,2,4,5-Benzenetetraamine, 4HCl, NSC 667249
• 実験式（ヒル表記法）: C₆H₁₀N₄ · 4HCl
• CAS番号: 4506-66-5
• 分子量: 284.01
• MDL番号: MFCD00012970
• UNSPSCコード: 12352200
• NACRES: NA.54

特性

• 品質水準: 100
• アッセイ: ≥95% (elemental analysis)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: gray
• 溶解性: water: 14 mg/mL; DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• InChI: 1S/C6H10N4.4ClH/c7-3-1-4(8)6(10)2-5(3)9;;;;/h1-2H,7-10H2;4*1H
• InChI Key: BZDGCIJWPWHAOF-UHFFFAOYSA-N

詳細

詳細

A cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK (Cat. No. 324876) autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC₅₀<1 µM) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 (Cat. No. 662067) autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-α, Pyk2, and PI 3-K (p110δ/p85α). Reported to inhibit BT474 proliferation both in cultures in vitro (IC₅₀ ~10 µM) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).

A cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC₅₀<1 M) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-α, Pyk2, and PI 3-K (p110δ/p85α). Reported to inhibit BT474 proliferation both in cultures in vitro (IC₅₀ ~10 M) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).

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 6 months at -20°C.

その他情報

Golubovskaya, V.M., et al. 2008. J. Med. Chem.51, 7405.

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