N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[3.3.1.13,7]dec-1-ylacetamidedihydrochloride Property

Melting point:

192-219°C

storage temp. 

Desiccate at RT

solubility 

DMSO (Slightly), Methanol (Slightly), Water (Slightly, Heated)

form 

Solid

color 

Pale Yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[3.3.1.13,7]dec-1-ylacetamidedihydrochloride Chemical Properties,Usage,Production

Uses

AZ 10606120 Dihydrochloride is a P2X7 antagonist, which is a key modulator of the PI3K/GSK3β/VEGF signaling network that is characteristic to neuroblastoma progression.

Biological Activity

kd: 1.4 nm and 1.9 nm for human and rat p2x7 receptors, respectivleythe p2x7 receptor has intriguing biophysical properties, activates a diverse range of cellular events and mediates a wide range of functional effects. the p2x7 receptor is an atp-gated ion channel known for its cytotoxic activity. however, recent evidence suggests a role for p2x7 in cell proliferation. az 10606120 is a p2x7 receptor antagonist.

in vitro

binding of [3h]-az 10606120 was higher in membranes prepared from cells expressing p2x7 receptors than from control cells and was inhibited by atp suggesting labelled sites represented human p2x7 receptors. binding was reversible, saturable and modulated by p2x7 receptor ligands. the positive cooperativity observed suggests that binding of az 10606120 to one subunit in the p2x7 receptor complex enhances subsequent binding to other p2x7 subunits in the same complex. the negative cooperative effects of atp suggest that atp and az 10606120 bind at separate, interacting, sites on the p2x7 receptor [1].

in vivo

intratumor injection of az10606120 caused a strong inhibition of tumor growth in b16-inoculated c57bl/6 mice and caused in parallel a large reduction in vegf staining and vessel formation [2].

storage

Desiccate at RT

References

[1] ad michel, lj chambers, wc clay, jp condreay, ds walter and ip chessell. direct labelling of the human p2x7 receptor and identification of positive and negative cooperativity of binding. british journal of pharmacology (2007) 151, 84–95
[2] elena adinolfi, lizzia raffaghello, anna lisa giuliani, luigi cavazzini, marina capece, paola chiozzi, giovanna bianchi, guido kroemer, vito pistoia, and francesco di virgilio. expression of p2x7 receptor increases in vivo tumor growth. cancer res; 72(12); 2957–69.