1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. AMG-458

AMG-458 

Cat. No.: HY-14723
Handling Instructions

AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.

For research use only. We do not sell to patients.

AMG-458 Chemical Structure

AMG-458 Chemical Structure

CAS No. : 913376-83-7

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Description

AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively[1].

IC50 & Target[1]

human c-Met

1.2 nM (Ki)

mouse c-Met

2.0 nM (Ki)

V1092I

1.1 nM (Ki)

D1228H

2.2 nM (Ki)

M1250T

4.1 nM (Ki)

H1094R

0.5 nM (Ki)

Y1230H

4.5 nM (Ki)

VEGDR2

4100 nM (Ki)

In Vivo

AMG-458 (orally, 30, 100 mg/kg) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight[1].

Animal Model: NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model[1].
Dosage: 10, 30, 100 mg/kg.
Administration: Orally q.d. or b.i.d.
Result: With an ED50 of ∼12 mg/kg and an ED90 of ∼ 34 mg/kg in NIH-3T3/TPR-Met model.
With an ED50 of ∼16 mg/kg and an ED90 of ∼ 59 mg/kg in U-87 MG human glioblastoma xenograft model.
Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight.
Animal Model: Balb/c mouse and SD rat[1].
Dosage: 1 mg/kg (Pharmacokinetic Analysis).
Administration: IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid).
Result: Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, Vss (L/kg) values of 0.31 and 0.62, t1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.
Molecular Weight

539.58

Formula

C₃₀H₂₉N₅O₅

CAS No.

913376-83-7

SMILES

O=C(C1=C(C)N(CC(C)(O)C)N(C2=CC=CC=C2)C1=O)NC3=NC=C(OC4=CC=NC5=CC(OC)=CC=C45)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AMG-458AMG458AMG 458c-Met/HGFRInhibitorinhibitorinhibit

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