Availability
0
Your Basket is Empty
FA64937
BIO-X

AMG 458

A potent and selective c-Met inhibitor. Anti-tumour activity demonstrated in xenograft models in vivo. Forms a thioether conjugate by reacting with thiol groups in proteins. Non-small-cell lung carcinoma (NSCLC) tumour cells that overexpress c-MET have increased sensitivity to AMG458.

Technical Data

CAS No: 913376-83-7
Product Code: FA64937
MDL No: MFCD17169989
Chemical Formula: C30H29N5O5
Molecular Weight: 539.58

References


  • Liu L et al (2008). Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem 51(13):3688-91.
  • Teffera Y et al (2008). Chemical reactivity of methoxy 4-o-aryl quinolines: identification of glutathione displacement products in vitro and in vivo. Chem Res Toxicol 21(11):2216-22.
  • Li B et al (2012). Higher levels of c-Met expression and phosphorylation identify cell lines with increased sensitivity to AMG-458, a novel selective c-Met inhibitor with radiosensitizing effects. Int J Radiat Oncol Biol Phys 84(4):e525-31.

Solubility

Stability

Further Information


Datasheets


CAS No:
913376-83-7
MDL No:
MFCD17169989
Chemical Formula:
Molecular Weight:
539.58
Product Structure
References:
1. Liu L et al (2008). Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem 51(13):3688-91.
2. Teffera Y et al (2008). Chemical reactivity of methoxy 4-o-aryl quinolines: identification of glutathione displacement products in vitro and in vivo. Chem Res Toxicol 21(11):2216-22.
3. Li B et al (2012). Higher levels of c-Met expression and phosphorylation identify cell lines with increased sensitivity to AMG-458, a novel selective c-Met inhibitor with radiosensitizing effects. Int J Radiat Oncol Biol Phys 84(4):e525-31.

For requirements greater than the catalogue prepacks email: enquiries@carbosynth.com

Custom Synthesis

For custom synthesis or special requests email: enquiries@carbosynth.com, call +44 (0)1635 578444 or fill out our contact form

Please Wait...