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

AMG-458 

Cat. No.: HY-14723 Purity: 98.18%
COA 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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solid
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10 mg USD 310 In-stock
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Based on 1 publication(s) in Google Scholar

AMG-458 Related Antibodies

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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]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Formula

C30H29N5O5
CAS No.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (92.66 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8533 mL 9.2665 mL 18.5329 mL
5 mM 0.3707 mL 1.8533 mL 3.7066 mL
10 mM 0.1853 mL 0.9266 mL 1.8533 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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AMG-458 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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Keywords:

AMG-458913376-83-7AMG458AMG 458c-Met/HGFRInhibitorinhibitorinhibit

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