TAK-700 (Orteronel)

Catalog No.S1195

TAK-700 (Orteronel) Chemical Structure

Molecular Weight(MW): 307.35

TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.

Size Price Stock Quantity  
In DMSO USD 330 In stock
USD 147 In stock
USD 597 In stock

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Biological Activity

Description TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.
Targets
17,20-lyase (Human) [1] 17,20-lyase (Rat) [1]
38 nM 54 nM
In vitro

In vitro, TAK-700 shows the potent inhibitory activity against rat and human steroid 17,20-lyase with IC50 of 54 nM and 38 nM, respectively. While other CYP isoforms including 11-hydroxylase and CYP3A4 are not significantly affected by TAK-700. [1] In microsomes expressing human CYP isoforms, TAK-700 exhibit greater inhibitory effects on 17,20-lyase with IC50 of 19 nM compared to the other CYP isoforms. [1] TAK-700 shows the inhibitory activity against monkey 17,20-lyase and 17-hydroxylase with IC50 of 27 nM and 38 nM, respectively. [2] In monkey adrenal cells, TAK-700 inhibits the ACTH stimulated production of DHEA and androstenedione with IC50 of 110 nM and 130 nM, respectively. Moreover, TAK-700 also potently inhibits DHEA production in human adrenocortical tumor line H295R cells with IC50 of 37 nM. [2]

In vivo In cynomolgus monkeys, oral treatment of TAK-700 at a dose of 1 mg/kg markedly reduces serum testosterone and dehydroepiandrosterone (DHEA) levels. [1] Oral treatment of TAK-700 at a dose of 1 mg/kg results in favorable pharmacokinetic parameters with Tmax, Cmax, t1/2 and AUC0-24 hours of 1.7 hours, 0.147 μg/mL, 3.8 hours and 0.727 μg h/mL, respectively. [2]

Protocol

Animal Research:

[1]

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  • Animal Models: Adult male cynomolgus monkeys.
  • Formulation: TAK-700 is dissolved in 0.5% methylcellulose.
  • Dosages: ≤1 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (198.47 mM)
Ethanol 8 mg/mL (26.02 mM)
Water <1 mg/mL
In vivo 0.5% methylcellulose 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 307.35
Formula

C18H17N3O2

CAS No. 426219-18-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02053311 Suspended Prostate Cancer Swiss Group for Clinical Cancer Research June 2014 Phase 3
NCT02101684 Recruiting Metastatic or Advanced Non-resectable Granulosa Cell Ovarian Tumors Grupo Español de Tumores Huérfanos e Infrecuentes|Takeda June 2014 Phase 2
NCT02054793 Withdrawn Prostate Cancer|Castration-resistant Prostate Cancer Emmanuel Antonarakis, MD|Millennium Pharmaceuticals, Inc.|Johns Hopkins University June 2014 Phase 1|Phase 2
NCT01990209 Recruiting Metastatic Breast Cancer SCRI Development Innovations, LLC|Millennium Pharmaceuticals, Inc. March 2014 Phase 2
NCT01658527 Withdrawn Prostate Cancer European Organisation for Research and Treatment of Cancer - EORTC January 2014 Phase 2
NCT01866423 Terminated Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer University of Southern California|National Cancer Institute (NCI)|Millennium Pharmaceuticals, Inc. October 2013 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID