An aminopeptidase inhibitor (IC50s = 100

Tosedostat – 5 mg

Brand:
Cayman
CAS:
238750-77-1
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 23395 - 5 mg Category:

Description

An aminopeptidase inhibitor (IC50s = 100, 150, and 220 nM for LAP, PUSA, and aminopeptidase N, respectively); inhibits proliferation of human leukemia cell lines in vitro irrespective of p53, PTEN, or K-RAS mutational status (IC50s = 10-770 nM); induces up-regulation of genes in amino acid transport and metabolic pathways and inhibits phosphorylation of mTOR substrates in HL-60 cells; reduces total tumor burden and the number of spontaneous metastases in a mouse MDA-MB-435 xenograft model when administered at a dose of 100 mg/kg

Formal name: αS-[[(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]amino]-benzeneacetic acid, cyclopentyl ester

Synonyms:  CHR-2797

Molecular weight: 406.5

CAS: 238750-77-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cancer|Metabolism

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