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Merck
CN

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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关于此项目

经验公式(希尔记法):
C6H10N4 · 4HCl
化学文摘社编号:
分子量:
284.01
UNSPSC Code:
12352200
NACRES:
NA.54
MDL number:
Assay:
≥95% (elemental analysis)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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Quality Segment

assay

≥95% (elemental analysis)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

gray

solubility

water: 14 mg/mL, DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

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

General description

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).

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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全球贸易项目编号

货号GTIN
324877-5MG04055977196061