JTE 013

Names

[ Name ]:
JTE 013

[Synonym ]:
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]-

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₁₇H₁₉Cl₂N₇O

[ Molecular Weight ]:
408.285

[ Exact Mass ]:
407.102814

[ PSA ]:
96.76000

[ LogP ]:
4.42

[ Index of Refraction ]:
1.697

[ Storage condition ]:
-20℃

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII