Home Metabolism P450 (e.g. CYP17) inhibitor - Androgen Receptor inhibitor Orteronel For research use only.

Orteronel

Synonyms: TAK-700

Orteronel(TAK-700) 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). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.

Orteronel Chemical Structure

Orteronel Chemical Structure

CAS No. 426219-18-3

Purity & Quality Control

Orteronel Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Biological Activity

Description Orteronel(TAK-700) 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). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.
Targets
17,20-lyase (Human) [1] 17,20-lyase (Rat) [1]
38 nM 54 nM
In vitro
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 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]
Animal Research Animal Models Adult male cynomolgus monkeys.
Dosages ≤1 mg/kg
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01808040 Completed
Post Menopausal Hormone Receptor Positive Breast Cancer
University of Wisconsin Madison|Millennium Pharmaceuticals Inc.
 November 2012 Phase 1
NCT01666314 Completed
Prostate Cancer
Millennium Pharmaceuticals Inc.|Takeda
 August 20 2012 Phase 1|Phase 2
NCT01549951 Completed
Prostate Cancer
Millennium Pharmaceuticals Inc.
 May 2012 Phase 2
NCT01084655 Completed
Prostate Cancer
Millennium Pharmaceuticals Inc.|Takeda
 July 2010 Phase 1|Phase 2
NCT01046916 Completed
Prostate Cancer
Millennium Pharmaceuticals Inc.
 May 2010 Phase 2

Chemical Information & Solubility

Molecular Weight 307.35 Formula

C18H17N3O2
CAS No. 426219-18-3 SDF Download Orteronel SDF
Smiles CNC(=O)C1=CC2=C(C=C1)C=C(C=C2)C3(CCN4C3=CN=C4)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 61 mg/mL ( (198.47 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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