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Orteronel

Chemical Structure : Orteronel

CAS No.: 566939-85-3

Orteronel (TAK-700;TAK700;TAK 700)

Catalog No.: PC-42626Not For Human Use, Lab Use Only.

A highly selective CYP17A1 (17,20-lyase) inhibitor with IC50 of 17 nM for human 17,20-lyase.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A highly selective CYP17A1 (17,20-lyase) inhibitor with IC50 of 17 nM for human 17,20-lyase; shows no activity on CYP3A4 (IC50>10 uM) and CYP11B1 (IC50>1 uM); reduces both serum testosterone and dehydroepiandrosterone concentrations in monkey model at a dose of 1mg/kg.

Prostate cancer

Phase 3 Discontinued

Physicochemical Properties

M.Wt 307.3465
Formula C18H17N3O2
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

2-Naphthalenecarboxamide, 6-[(7S)-6,7-dihydro-7-hydroxy-5H-pyrrolo[1,2-c]imidazol-7-yl]-N-methyl-

References

1. Kaku T, et al. Bioorg Med Chem. 2011 Nov 1;19(21):6383-99.

2. Yamaoka M, et al. J Steroid Biochem Mol Biol. 2012 Apr;129(3-5):115-28.

3. Dreicer R, et al. Clin Cancer Res. 2014 Mar 1;20(5):1335-44.

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