1. Protein Tyrosine Kinase/RTK
    Metabolic Enzyme/Protease
  2. c-Met/HGFR
    Cytochrome P450
  3. AMG-208

AMG-208 

Cat. No.: HY-12035 Purity: 99.34%
Handling Instructions

AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity.

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

AMG-208 Chemical Structure

AMG-208 Chemical Structure

CAS No. : 1002304-34-8

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Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
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100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AMG-208

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity[1][2][3].

IC50 & Target[1][2]

c-Met

9 nM (IC50)

CYP3A4

32 μM (IC50)

In Vitro

AMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM[1].
Pre-incubation of AMG-208 (compound 1) with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation[2].

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

In Vivo

In male Sprague Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour[1].

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

Clinical Trial
Molecular Weight

383.40

Formula

C22H17N5O2

CAS No.
SMILES

COC1=CC=C2C(OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5)=CC=NC2=C1

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 : 3.33 mg/mL (8.69 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.34%

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AMG-208
Cat. No.:
HY-12035
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