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Tosedostat

Chemical Structure : Tosedostat

CAS No.: 238750-77-1

Tosedostat (CHR-2797;CHR2797)

Catalog No.: PC-70071Not For Human Use, Lab Use Only.

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.

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Biological Activity

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.
Tosedostat (CHR-2797) exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity for transformed over nontransformed cells.
Tosedostat (CHR-2797) inhibits phosphorylation of mTOR substrates and reduces protein synthesis in HL-60 cells.

Physicochemical Properties

M.Wt 406.479
Formula C21H30N2O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Krige D, et al. Cancer Res. 2008 Aug 15;68(16):6669-79.

2. Moore HE, et al. Mol Cancer Ther. 2009 Apr;8(4):762-70.

3. Reid AH, et al. Clin Cancer Res. 2009 Aug 1;15(15):4978-85.

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