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

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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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

AMG-458 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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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)

Cellular Effect
Cell Line Type Value Description References
NIH3T3 ED50
12 mg/kg
Compound: 17
Antitumor activity in TPR-Met expressing human NIH3T3 cells xenografted in po dosed mouse assessed as tumor growth inhibition after 24 hrs
Antitumor activity in TPR-Met expressing human NIH3T3 cells xenografted in po dosed mouse assessed as tumor growth inhibition after 24 hrs
[PMID: 18553959]
PC-3 IC50
60.1 nM
Compound: 59e, AMG-458
Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
[PMID: 22320327]
U-87MG ATCC ED50
16 mg/kg
Compound: 17
Antitumor activity in human U87MG cells xenografted orally dosed CD1 NU/NU mouse assessed as tumor growth inhibition after 14 days
Antitumor activity in human U87MG cells xenografted orally dosed CD1 NU/NU mouse assessed as tumor growth inhibition after 14 days
[PMID: 18553959]
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

Formula

C30H29N5O5
CAS No.
Appearance

Solid

Color

Off-white to pink

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8533 mL 9.2665 mL 18.5329 mL 46.3323 mL
5 mM 0.3707 mL 1.8533 mL 3.7066 mL 9.2665 mL
10 mM 0.1853 mL 0.9266 mL 1.8533 mL 4.6332 mL
15 mM 0.1236 mL 0.6178 mL 1.2355 mL 3.0888 mL
20 mM 0.0927 mL 0.4633 mL 0.9266 mL 2.3166 mL
25 mM 0.0741 mL 0.3707 mL 0.7413 mL 1.8533 mL
30 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5444 mL
40 mM 0.0463 mL 0.2317 mL 0.4633 mL 1.1583 mL
50 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9266 mL
60 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7722 mL
80 mM 0.0232 mL 0.1158 mL 0.2317 mL 0.5792 mL
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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.

Keywords:

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

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