产品名称 | TAK 700 - Orteronel |
产品货号 | Axon 2124 CAS [566939-85-3] MF C18H17N3O2MW 307.35 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description Potent, orally available, and highly selective inhibitor of 17,20-lyase (CYP17A1; IC50 value 19 nM and 48 nM for human and rat respectively) and of correlated androgen synthesis. TAK 700 exhibits no affinity for CYP11B 1and CYP3A4 (IC50 values >1000 nM and >10000 nM resp.), nor for other isoforms of the human CYP enzyme (IC50 values >14000 nM). When given orally to monkeys at a dose of 1 mg/kg, TAK 700 markedly reduced serum testosterone and DHEA at 5 h after administration. TAK 700 was selected for evaluation in patients in phase III clinical trials for the potential treatment of prostate cancer. References Certificates Categories Extra info T. Kaku et al. Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer. Bioorg. Med. Chem. 2011, 19(21), 6383-99. M. Yamaoka et al. Orteronel (TAK-700), a novel non-steroidal 17,20-lyase inhibitor: effects on steroid synthesis in human and monkey adrenal cells and serum steroid levels in cynomolgus monkeys. J. Steroid Biochem. Mol. Biol. 2012, 129, 115-128. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Diabetes & Metabolism Endocrinology EC 1.14.99.9 Cytochrome P450 Potent and highly selective inhibitor of 17,20-lyase (CYP17A1) Chemical name (S)-6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methyl-2-naphthamide Parent CAS No. [566939-85-3] Order Size Unit Price Stock 5 mg €105.00 In Stock |
产品价格 | 现货询价,电话:010-67529703 |
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产品品牌 | axonmedchem |
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TAK 700 - OrteronelAxon 2124 CAS [566939-85-3] MF C18H17N3O2
Description
Potent, orally available, and highly selective inhibitor of 17,20-lyase (CYP17A1; IC50 value 19 nM and 48 nM for human and rat respectively) and of correlated androgen synthesis. TAK 700 exhibits no affinity for CYP11B 1and CYP3A4 (IC50 values >1000 nM and >10000 nM resp.), nor for other isoforms of the human CYP enzyme (IC50 values >14000 nM). When given orally to monkeys at a dose of 1 mg/kg, TAK 700 markedly reduced serum testosterone and DHEA at 5 h after administration.
TAK 700 was selected for evaluation in patients in phase III clinical trials for the potential treatment of prostate cancer.
Potent and highly selective inhibitor of 17,20-lyase (CYP17A1)
Chemical name(S)-6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methyl-2-naphthamide Parent CAS No.[566939-85-3] |
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