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Safety Information

324877

Sigma-Aldrich

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.

Synonym(s):

Focal Adhesion Kinase Inhibitor I, FAK Inhibitor I, 1,2,4,5-Benzenetetraamine, 4HCl, NSC 667249

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About This Item

Empirical Formula (Hill Notation):
C6H10N4 · 4HCl
CAS Number:
Molecular Weight:
284.01
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54

Quality Level

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

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).
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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

324877-1.1ML:
324877-MG:
324877-5MG:


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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