TAK-700 R-form is a highly selective inhibitor of 17, 20-lyase with IC50 value of 38nM . TAK-700 is a potent and selective inhibitor of the 17, 20-lyase activity of CYP17A1 which is responsible for androgen biosynthesis. Thus, TAK-700 is selected as a candidate for treatment of prostate cancer through reducing the adrenal androgen production. As an inhibitor of CYP17A1, the selectivity of TAK-700 is important to avoid causing the drug–drug interactions or side effects. TAK-700 shows potent inhibitory activity and high selectivity against 17, 20-lyase over other CYPs including 11-hydroxylase and CYP3A4. The IC50 values for 11-hydroxylase and CYP3A4 are above 1μM and above 10μM, respectively. Moreover, in a monkey model, the administration of TAK-700 is found to significantly reduce serum testosterone and DHEA levels .

Product information

CAS Number: 752243-39-3

Molecular Weight: 307.35

Formula: C18H17N3O2

Chemical Name: 6-[(7R)-7-hydroxy-5H, 6H, 7H-pyrrolo[1, 2-c]imidazol-7-yl]-N-methylnaphthalene-2-carboxamide

Smiles: CNC(=O)C1=CC2=CC=C(C=C2C=C1)[C@]1(O)CCN2C=NC=C12

InChiKey: OZPFIJIOIVJZMN-GOSISDBHSA-N

InChi: InChI=1S/C18H17N3O2/c1-19-17(22)14-3-2-13-9-15(5-4-12(13)8-14)18(23)6-7-21-11-20-10-16(18)21/h2-5,8-11,23H,6-7H2,1H3,(H,19,22)/t18-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.