[TaiClone] Tosedostat

[TaiClone] Tosedostat

 

 

tcsc0003570

Specifications

Purity / Grade

>98%

 

Solubility

DMSO : 25 mg/mL (61.51 mM; Need ultrasonic and warming)

 

Smiles

smiles

Misc Information

Alternative Names

CHR-2797

Observed Molecular Weight

406.47

Product Description

Tosedostat is an aminopeptidase inhibitor.

IC50 & Target: Aminopeptidase[1]

 

In Vitro: Treatment of HL-60 cells with Tosedostat (CHR-2797) leads to an increase in the secretion of Stanniocalcin 2 (STC2) protein into the growth medium. Increases in SLC7A11 expression are detectable at 60 nM Tosedostat and as early as 2 h posttreatment. The IC50s for inhibition of proliferation by Tosedostat in U-937 and HuT 78 cell lines are 10 nM and >10 μM, respectively. Tosedostat treatment increases expression of amino acid deprivation response (AADR) genes in U-937 cells but not in HuT 78 cells[1]. By 24 h with 0.01 μM Tosedostat the mean MCA production is reduced to 77.8% of the untreated control cells; similarly the MCA production is reduced to 51.3% with 1 μM, 38.5% with 5 μM, and 35.3% with 10 μM Tosedostat[2].

 

In Vivo: Tosedostat (CHR-2797) is active as an anticancer agent in vivo in rodent cancer models, and a dose-response relationship has been shown in two models. The effect of Tosedostat is less apparent when the tumor burden is higher before treatment[1].

Information

CAS No

238750-77-1

FormulaC21H30N2O6

Clinical Information

clinical

information

Pathway

Metabolic Enzyme/Protease

Target

Aminopeptidase