Art. -Nr.: HY-14723

AMG-458

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

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Reinheit: 98.41%
CAS. Nr.: 913376-83-7
Formel: C₃₀H₂₉N₅O₅
Molecular Weight:539.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AMG-458 Chemical Structure

CAS. Nr.: 913376-83-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with K_i 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
CT26	IC₅₀	120 nM Compound: 17	Inhibition of HGF-mediated c-Met phosphorylation in mouse CT26 cells Inhibition of HGF-mediated c-Met phosphorylation in mouse CT26 cells	[PMID: 18553959]
HUVEC	IC₅₀	690 nM Compound: 17	Inhibition VEGFR2-mediated survival of HUVEC Inhibition VEGFR2-mediated survival of HUVEC	[PMID: 18553959]
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 nM Compound: 17	Inhibition of HGF-mediated c-Met phosphorylation in human PC3 cells Inhibition of HGF-mediated c-Met phosphorylation in human PC3 cells	[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, V_ss (L/kg) values of 0.31 and 0.62, t_1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.

Chemical Information

CAS. Nr. 913376-83-7
Appearance Solid
Molecular Weight 539.58
Formel C₃₀H₂₉N₅O₅
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

Verweise

[1]. Longbin Liu, et al. Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem. 2008 Jul 10;51(13):3688-91. [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, 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

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-458

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-458 Related Classifications

HY-14723 Related Classifications