A 484954

Modify Date: 2024-01-13 19:06:35

A 484954 structure	Common Name	A 484954
	CAS Number	142557-61-7	Molecular Weight	289.29000
	Density	1.522±0.06 g/cm3 (20 ºC 760 Torr)	Boiling Point	N/A
	Molecular Formula	C₁₃H₁₅N₅O₃	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	N/A
	Symbol	GHS06	Signal Word	Danger

Use of A 484954

A-484954 is a highly selective eukaryotic elongationfactor-2 (eEF2) inhibitor, with an IC50 of 280 nM.

Name	7-amino-1-cyclopropyl-3-ethyl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide
Synonym	More Synonyms

Description	A-484954 is a highly selective eukaryotic elongationfactor-2 (eEF2) inhibitor, with an IC50 of 280 nM.
Related Catalog	Signaling Pathways >> Neuronal Signaling >> CaMK Research Areas >> Cancer
Target	IC50: 280 nM (eEF2)[1].
In Vitro	A-484954 is a highly selective eEF2K inhibitor with an IC50 value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin[1].
In Vivo	A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery[2]. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation[3].
References	[1]. Chen Z, et al. 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor. J Biol Chem. 2011 Dec 23;286(51):43951-8. [2]. Kodama T, et al. Mechanisms underlying the relaxation by A484954, a eukaryotic elongation factor 2 kinase inhibitor, in rat isolated mesenteric artery. J Pharmacol Sci. 2018 May;137(1):86-92. [3]. Kameshima S, et al. Eukaryotic elongation factor 2 kinase mediates monocrotaline-induced pulmonary arterial hypertension via reactive oxygen species-dependent vascular remodeling. Am J Physiol Heart Circ Physiol. 2015 May 15;308(10):H1298-305.

Density	1.522±0.06 g/cm3 (20 ºC 760 Torr)
Molecular Formula	C₁₃H₁₅N₅O₃
Molecular Weight	289.29000
Exact Mass	289.11700
PSA	127.72000
LogP	0.40840
Appearance of Characters	white to beige
Storage condition	2-8°C
Water Solubility	DMSO: soluble 3mg/mL, clear (warmed)

A 484954 MSDS(Chinese)

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H301-H315-H319-H335
Precautionary Statements	P261-P301 + P310-P305 + P351 + P338
Hazard Codes	T
Risk Phrases	R25-36/37/38
Safety Phrases	S26-45
RIDADR	UN 2811 6.1 / PGIII

Kinome_3822

7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide

X5939

7-Amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxo-pyrido[2,3-d]pyrimidine-6-carboxamide

A 484954

A-484954

DC Chemicals Limited
China
Product Name: A-484954
Price: $450.0/100mg $900.0/250mg $1800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 7-Amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Price: ￥1100/10 mM * 1 mL in DMSO

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A 484954

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