TH 1217

Modify Date: 2024-01-14 19:28:02

TH 1217 Structure
TH 1217 structure
Common Name TH 1217
CAS Number 1862212-48-3 Molecular Weight 491.09
Density N/A Boiling Point N/A
Molecular Formula C20H17BCl2N4O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of TH 1217


TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19[1][2].

 Names

Name TH1217

 TH 1217 Biological Activity

Description TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19[1][2].
Related Catalog
Target

IC50: 47 nM (dCTPase)[1]

In Vitro TH1217 (compound 30) inhibits dCTPase and enhances aqueous solubility (>100 μM) and improves plasma stability in vitro(t4h=86%)[1]. TH1217 presents suitable mouse microsomal half-lives (109 minutes)[1]. TH1217 displays well cell permeability (8.66×10-6/1.30×10-3 cm/s) and CYP inhibition[1].
References

[1]. Llona-Minguez S, et, al. Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1. Med Chem. 2016 Feb 11; 59(3): 1140-1148.

[2]. Gordon DE, et, al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22; 2020.03.22.002386.

 Chemical & Physical Properties

Molecular Formula C20H17BCl2N4O6
Molecular Weight 491.09
Storage condition -20°C