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AMG-458

Cat. No. M1745

AMG-458 Structure

Synonym: AMG458

Size Price Availability Quantity
10mg USD 220 In stock
50mg USD 680 In stock
100mg USD 1080 In stock
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Quality Control
Biological Activity

AMG 458 is a Potent, Selective, and Orally Bioavailable c-Met Inhibitor with Ki=2.0, IC50 (CT26)=120 nM significantly inhibited tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 539.58
Formula C30H29N5O5
CAS Number 913376-83-7
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

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.
Li B et al. Int J Radiat Oncol Biol Phys. 2012 Jul 24. PMID: 22836051.

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).
Liu L et al. J Med Chem. 2008 Jul 10;51(13):3688-91. PMID: 18553959.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AMG-458, AMG458 supplier, c-Met, inhibitors

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