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TAK-700

Cat. No. M3750
TAK-700 Structure
Synonym:

Orteronel

Size Price Availability
5mg USD 100  USD100 4-7 Days
10mg USD 170  USD170 4-7 Days
25mg USD 340  USD340 4-7 Days
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Quality Control & Documentation
Biological Activity

TAK-700 (Orteronel) selectively inhibits the enzyme CYP17A1 which is expressed in testicular, adrenal, and prostatic tumor tissues. 17,20-Lyase inhibition by orteronel was tolerable and results in declines in PSA and testosterone, with evidence of radiographic responses.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Adult male cynomolgus monkeys.
Formulation TAK-700 is dissolved in 0.5% methylcellulose.
Dosages ≤1 mg/kg
Administration Administered via p.o.
Chemical Information
Molecular Weight 307.35
Formula C18H17N3O2
CAS Number 566939-85-3
Solubility (25°C) DMSO ≥ 10 mg/mL
Ethanol ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Dreicer R, et al. Clin Cancer Res. Phase I/II trial of orteronel (TAK-700)--an investigational 17,20-lyase inhibitor--in patients with metastatic castration-resistant prostate cancer.

[2] Masuo Yamaoka, et al. J Steroid Biochem Mol Biol. 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

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Keywords: TAK-700, Orteronel supplier, Androgen Receptor, inhibitors, activators


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