JTE 607 dihydrochloride

Tocris Bioscience | Catalog # 5185

Active metabolite binds CPSF3; Pro-drug
Tocris Bioscience

Key Product Details

Description

Active metabolite binds CPSF3; Pro-drug

Alternative Names

TO-207
View all Cytokine Compounds »

Product Description

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; Kd = 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.

Product Specifications for JTE 607 dihydrochloride

Molecular Weight

597.36

Formula

C25H31Cl2N3O5.2HCl

Storage

Desiccate at RT

Purity

≥98% (HPLC)

Chemical Name

N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 3 publications citing the usage of this product.

Product Documents for JTE 607 dihydrochloride

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for JTE 607 dihydrochloride

For research use only

Citations for JTE 607 dihydrochloride

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