Tosedostat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tosedostat (CHR-2797, CHR2797) 是一种有效的、口服生物可利用的氨肽酶抑制剂。

Tosedostat (CHR-2797, CHR2797) is a potent, orally bioavailable aminopeptidases inhibitor with IC50 of 150, 220 and 100 nM for PuSA, aminopeptidase N and leucine aminopeptidase, respectively; exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity for transformed over nontransformed cells; inhibits phosphorylation of mTOR substrates and reduces protein synthesis in HL-60 cells.Blood Cancer Phase 2 Clinical(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. 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.(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.

——

——

CHR-2797 | CHR2797

Metabolic Enzyme/Protease

Aminopeptidase

M1-aminopeptidase

Cancer

Blood cancer

238750-77-1

406.479

C21H30N2O6

>98% (HPLC)

DMSO: >10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(OC1CCCC1)[C@@H](NC([C@@H]([C@H](O)C(NO)=O)CC(C)C)=O)C2=CC=CC=C2

cyclopentyl (S)-2-((R)-2-((S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl)-4-methylpentanamido)-2-phenylacetate

(-20℃)

With Ice Pack

≥ 2 years