CAS 1002304-34-8|AMG-208

Introduction：Basic information about CAS 1002304-34-8|AMG-208, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. AMG-208 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	AMG-208
CAS Number	1002304-34-8	Molecular Weight	383.403
Density	1.3±0.1 g/cm3	Boiling Point	/
Molecular Formula	C₂₂H₁₇N₅O₂	Melting Point	/
MSDS	/	Flash Point	/

Names

Name	7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline
Synonym	More Synonyms

AMG-208 BiologicalActivity

Description	AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.IC50 value: 9.3 nMTarget: c-Metin vitro: AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 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 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]. AMG-208 is identified to be a c-MET and RON dual selective inhibitor [3].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].
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFRResearch Areas >>Cancer
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. [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. [3]. Liu X, et al. Developing c-MET pathway inhibitors for cancer therapy: progress and challenges. Trends Mol Med. 2010,16(1), 37-45.

Description

AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.IC50 value: 9.3 nMTarget: c-Metin vitro: AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 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 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]. AMG-208 is identified to be a c-MET and RON dual selective inhibitor [3].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].

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFRResearch Areas >>Cancer

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.

[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.

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

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Molecular Formula	C₂₂H₁₇N₅O₂
Molecular Weight	383.403
Exact Mass	383.138214
PSA	74.43000
LogP	4.02
Index of Refraction	1.696
InChIKey	HEAIZQNMNCHNFD-UHFFFAOYSA-N
SMILES	COc1ccc2c(OCc3nnc4ccc(-c5ccccc5)nn34)ccnc2c1
Storage condition	-20℃

Safety Information

Hazard Codes	N

Synonyms

7-Methoxy-4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline

7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline

AMG208,AMG-208

S1316_Selleck

Quinoline, 7-methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)methoxy]-

3cd8

Triazolopyridazine,4

AMG-208

AMG208

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