Cat. No.: HY-12035

AMG-208

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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.

Purity: 99.86%
CAS No.: 1002304-34-8
Formula: C₂₂H₁₇N₅O₂
Molecular Weight:383.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AMG-208 Chemical Structure

CAS No.: 1002304-34-8

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]

CYP3A4

32 μM (IC₅₀)

c-Met

9 nM (IC₅₀)

All Cytochrome P450 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	46 nM Compound: 1	Inhibition of HGF-mediated human c-Met autophosphorylation expressed in human PC3 cells after 1 hr by electrochemiluminescent immunoassay Inhibition of HGF-mediated human c-Met autophosphorylation expressed in human PC3 cells after 1 hr by electrochemiluminescent immunoassay	[PMID: 19819693]

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].

MedChemExpress (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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1002304-34-8
Appearance Solid
Molecular Weight 383.40
Formula C₂₂H₁₇N₅O₂
Color White to off-white
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	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885

Solvent & Solubility

In Vitro:

DMSO : 3.33 mg/mL (8.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6082 mL

13.0412 mL

26.0824 mL

5 mM

0.5216 mL

2.6082 mL

5.2165 mL

10 mM

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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Albrecht BK, et al. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem. 2008, 51(10), 2879-2882. [Content Brief]

[2]. Boezio AA, et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Lett. 2009, 19(22), 6307-6312. [Content Brief]

[3]. Liu X, et al. Developing c-MET pathway inhibitors for cancer therapy: progress and challenges. Trends Mol Med. 2010,16(1), 37-45. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6082 mL	13.0412 mL	26.0824 mL	65.2061 mL
DMSO	5 mM	0.5216 mL	2.6082 mL	5.2165 mL	13.0412 mL

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AMG-208

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

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Highly Selective Inhibitors Library

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Anti-Gastric Cancer Compound Library

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Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AMG-208

All Cytochrome P450 Isoforms