JTE-013|cas 383150-41-2|DC Chemicals

Cas No.:	383150-41-2
Chemical Name:	Pyrazolopyridine analog
Synonyms:	1-(2,6-dichloropyridin-4-yl)-3-[(1,3-dimethyl-4-propan-2-ylpyrazolo[3,4-b]pyridin-6-yl)amino]urea;JTE-013;Jte 013;S1P2 Receptor Antagonist, JTE-013;1-(1,3-Dimethyl-4-isopropyl)-1H-pyrazolo[3,4-b]pyridin-6-yl)-4-(3,5-dichloro-4-pyridinyl)-semicarbazide;pyrazolopyridine analog;CTK8F0047;MolPort-003-983-772;HMS3269A03;1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-4-(2,6-dichloro-4-pyridinyl)-semicarbazide;N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-hydrazinecarboxamide;N-(2,6-dichloropyridin-4-yl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazinecarboxamide;C17H19Cl2N7O;GTPL2917;AOB1935;SYN5010;HMS3413I20;HMS3650O1
SMILES:	ClC1C([H])=C(C([H])=C(N=1)Cl)N([H])C(N([H])N([H])C1C([H])=C(C2C(C([H])([H])[H])=NN(C([H])([H])[H])C=2N=1)C([H])(C([H])([H])[H])C([H])([H])[H])=O
Formula:	C₁₇H₁₉Cl₂N₇O
M.Wt:	408.2851
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
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.
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.

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