Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: aS-[[(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]amino]-benzeneacetic acid, cyclopentyl ester
Purity: ≥98%
Formula Markup: C21H30N2O6
Formula Weight: 406.5
CAS Number: 238750-77-1
Notes: Tosedostat is an inhibitor of aminopeptidases (IC50s = 100, 150, and 220 nM for LAP, PUSA, and aminopeptidase N, respectively).{37251} It inhibits proliferation of human leukemia cell lines in vitro irrespective of p53, PTEN, or K-RAS mutational status (IC50s = 10-770 nM). Tosedostat induces up-regulation of genes in amino acid transport and metabolic pathways and inhibits phosphorylation of mammalian target of rapamycin (mTOR) substrates in HL-60 cells, markers of amino acid depletion. In vivo, tosedostat (100 mg/kg) reduces total tumor burden and the number of spontaneous metastases in a mouse MDA-MB-435 xenograft model. Formulations containing tosedostat are under clinical investigation for the treatment of myeloid leukemia.
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