JTE 607 dihydrochloride

Name: JTE 607 dihydrochloride
Brand: Tocris Bioscience
SKU: 5185

Tocris Bioscience, part of Bio-Techne | Catalog # 5185

Citations (3)

COA / SDS

Active metabolite binds CPSF3; Pro-drug

Key Product Details

Description:	Active metabolite binds CPSF3; Pro-drug
Alternative Names:	TO-207
Chemical Name:	N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	597.36

View Full Technical Details for JTE 607 dihydrochloride

Technical Data
Citations

Biological Activity for JTE 607 dihydrochloride

JTE 607 dihydrochloride is a pro-drug that is cleaved by carboxylesterase 1 (CES1) to its active metabolite, which then binds to cleavage and polyadenylation specificity factor 3 (CPSF3; K_d = 370 nM at human CPSF3). Treatment of A-673 cells with JTE 607 results in inhibition of mRNA cleavage and accumulation of nuclear R-loops. JTE 607 induces apoptosis in leukemia cells in vitro and prolongs survival in a mouse leukemia model. JTE 607 inhibits cytokine release and inhibits production of IL-1β, IL-8, IL-6, IL-10 and TNFα (IC₅₀ values are 5.9, 7.3, 8.8, 9.1 and 11.0 nM, respectively) from LPS-stimulated PBMCs. In a rat model of lung injury, JTE 607 reduces proinflammatory cytokine-release and attenuates lung permeability.

Compound Libraries for JTE 607 dihydrochloride

JTE 607 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for JTE 607 dihydrochloride

M. Wt	597.36
Formula	C₂₅H₃₁Cl₂N₃O₅.2HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	188791-09-5
PubChem ID	9938544
InChi Key	JUJAUEQJEWIWCQ-FJSYBICCSA-N
Smiles	ClC1=C(OCCN2CCN(C)CC2)C(Cl)=CC(C(N[C@@H](CC3=CC=CC=C3)C(OCC)=O)=O)=C1O.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for JTE 607 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	59.74	100
	DMSO	59.74	100

Preparing Stock Solutions for JTE 607 dihydrochloride

The following data is based on the product molecular weight 597.36.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.67 mL	8.37 mL	16.74 mL
5 mM	0.33 mL	1.67 mL	3.35 mL
10 mM	0.17 mL	0.84 mL	1.67 mL
50 mM	0.03 mL	0.17 mL	0.33 mL

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References for JTE 607 dihydrochloride

References are publications that support the biological activity of the product.

Ross CPSF3-dependent pre-mRNA processing as a druggable node in AML and Ewing's sarcoma. Nat.Chem.Biol. 2020 PMID: 31819276
Jian JTE-607, a cytokine release blocker, attenuates acid aspiration-induced lung injury in rats. Eur.J.Pharmacol. 2004 PMID: 15044056
Tajima JTE-607, a multiple cytokine production inhibitor, induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells. Cancer Sci. 2010 PMID: 20028380
Kakutani JTE-607, a novel inflammatory cytokine synthesis inhibitor without immunosuppression, protects from endotoxin shock in mice. Inflamm.Res. 1999 PMID: 10493164