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.
别名:
Focal Adhesion Kinase Inhibitor I, FAK Inhibitor I, 1,2,4,5-Benzenetetraamine, 4HCl, NSC 667249
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About This Item
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质量水平
方案
≥95% (elemental analysis)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
gray
溶解性
water: 14 mg/mL
DMSO: 50 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
Cl.Cl.Cl.Cl.Nc1c(cc(c(c1)N)N)N
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
一般描述
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)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Golubovskaya, V.M., et al. 2008. J. Med. Chem.51, 7405.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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