383150-41-2

383150-41-2 structure

Name: JTE 013
Chemical Name: 1-(2,6-dichloropyridin-4-yl)-3-[(1,3-dimethyl-4-propan-2-ylpyrazolo[3,4-b]pyridin-6-yl)amino]urea
CAS Number: 383150-41-2
Molecular Formula: C₁₇H₁₉Cl₂N₇O
Molecular Weight: 408.285
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2017-07-15 17:04:48
Modify Date: 2024-01-05 09:20:43
JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively[1].

Name	1-(2,6-dichloropyridin-4-yl)-3-[(1,3-dimethyl-4-propan-2-ylpyrazolo[3,4-b]pyridin-6-yl)amino]urea
Synonyms	N-(2,6-Dichloropyridin-4-yl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazinecarboxamide JTE-013 HMS3269A03 N-(2,6-Dichloro-4-pyridinyl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazinecarboxamide S1P2 Receptor Antagonist,JTE-013 pyrazolopyridine analog Hydrazinecarboxamide, N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-

Description	JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer
Target	IC50: 17 nM (S1P2 for human) and 22 nM (S1P2 for rat)[1]
In Vitro	JTE-013 (50-200 μM; 1-3 days) reduced cell viability[1]. JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation[1]. JTE-013 displays 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM[1]. Cell Viability Assay[1] Cell Line: SK-N-AS cells Concentration: 50, 100, 150, 200 μM Incubation Time: 1-3 days Result: Reduced cell viability. Western Blot Analysis[1] Cell Line: SK-N-AS cells Concentration: 10, 100, 1000 nM Incubation Time: 30 mins Result: Reversed S1P-induced Akt inhibition and inhibited S1P-induced ERK activation.
In Vivo	JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight[1]. Animal Model: Six-week-old female athymic NCr-nu/nu nude mice[1] Dosage: 30 mg/kg Administration: Gavage; daily for 14 consecutive days Result: Reduced tumor size and tumor weight.
References	[1]. Li MH, et al. Antitumor Activity of a Novel Sphingosine-1-Phosphate 2 Antagonist, AB1, in Neuroblastoma. J Pharmacol Exp Ther. 2015 Sep;354(3):261-8.