AMG-337 Property

Density 

1.44±0.1 g/cm3(Predicted)

storage temp. 

Refrigerator, under inert atmosphere

solubility 

Chloroform (Slightly), Methanol (Slightly)

form 

Solid

pka

2.10±0.20(Predicted)

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..…

AMG-337 Chemical Properties,Usage,Production

Uses

AMG 337 is a potent and selective inhibitor of mesencymal epethelial transition factor (MET factor) which has been implicated in several cancers.

Biological Activity

amg 337 is a met inhibitor.met receptor with its ligand can promote cell survival, proliferation, and invasion. the activation of met signaling is a common regulator of various human cancer types, and thus, inhibition of met signaling is an promising therapeutic opportunity for the treatment of cancer.

in vitro

amg 337 could effectively inhibit met kinase activity, and amg 337 also showed great selectivity for met when tested against a panel of over 400 protein as well as lipid kinases. in addition, amg 337 was found to inhibit hgf-dependent met phosphorylation. furthermore, amg 337 could only affect the viability of two gastric cancer cell lines with amplification of the met gene. the ic50 values of amg 337 for the two sensitive cell lines was less than 50 nm, whereas over 10 μm in all other tested cell lines [1].

in vivo

in anima study, it was found that the oral administration of amg 337 led to the dose-dependent anti-tumor efficacy in met amplified gastric cancer xenograft models, which was quite consistent with the pd modulation of met signaling [1].

IC 50

< 5 nm in enzymatic assays

References

[1] paul e. hughes, et al. amg 337, a novel, potent and selective met kinase inhibitor, has robust growth inhibitory activity in met-dependent cancer models. cancer res october 1, 2014 74; 728
[2] https://clinicaltrials. gov/ct2/show/nct01253707 term=amg+337&rank=1