For research use only.
CAS No. 426219-18-3
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.
Purity & Quality Control
Choose Selective P450 (e.g. CYP17) Inhibitors
|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.|
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.  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.  TAK-700 shows the inhibitory activity against monkey 17,20-lyase and 17-hydroxylase with IC50 of 27 nM and 38 nM, respectively.  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. 
|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.  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. |
|In vitro||DMSO||61 mg/mL (198.47 mM)|
|Ethanol||8 mg/mL (26.02 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01808040||Completed||Drug: TAK700||Post Menopausal Hormone Receptor Positive Breast Cancer||University of Wisconsin Madison|Millennium Pharmaceuticals Inc.||November 2012||Phase 1|
|NCT01666314||Completed||Drug: Orteronel|Drug: Orteronel Placebo|Drug: Prednisone||Prostate Cancer||Millennium Pharmaceuticals Inc.|Takeda||August 20 2012||Phase 1|Phase 2|
|NCT01549951||Completed||Drug: Orteronel+Prednisone||Prostate Cancer||Millennium Pharmaceuticals Inc.||May 2012||Phase 2|
|NCT01084655||Completed||Drug: TAK-700|Drug: Docetaxel|Drug: Prednisone||Prostate Cancer||Millennium Pharmaceuticals Inc.|Takeda||July 2010||Phase 1|Phase 2|
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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