Product Information
Applications
Biological Information
Primary Target17,20-lyase
Secondary target17α-hydroxylase
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

CYP17A1 Inhibitor II, TAK-700 - CAS 566939-85-3 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Dreicer, R., et al. 2014. Clin. Cancer Res. 20, 1335.
Yin, L. and Hu, Q., 2014. Nat. Rev. Urol. 11, 32.
Hara, T., et al. 2013.J. Steroid Biochem. Mol. Biol. 134, 80.
Yamaoka, M., et al. 2012. J. Steroid Biochem. Mol. Biol. 129, 115.
Kaku, T., et al. 2011. Bioorg. Med. Chem. 19, 6383.

Brochure

Title
NPI Flyer- Epigenetics and Nuclear Function Feature (EMD)
New Products - Antibodies, Small Molecule, Inhibitors

Technical Info

Title
White Paper: Further considerations of antibody validation and usage. (EMD)
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision19-December-2014 JSW
Synonyms6-((7S)-7-Hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methyl-2-naphthamide, Orteronel, TAK700
DescriptionA cell-permeable, orally bioavailable (Tmax/Cmax/AUC = 1.7 h/147 ng·mL-1/727 ng·h·mL-10-24 h/monkey & 1.7 h/39 ng·mL-1/177 ng·h·mL-10-8 h/rat; 1 mg/kg p.o.), nonsteroidal, optically active naphthylmethylimidazole compound that acts as a potent, reversible, substrate-competitive inhibitor against the 17,20-lyase activity (IC50/[substrate] = 19 nM/10 nM 17α-hydroxypregnenolone/rhP450c17, 27 nM/5 µM 17α-hydroxypregnenolone/monkey adrenal microsomes, 48 nM/10 nM 17α-hydroxyprogesterone /rat testicular microsomes, 140 nM/5 µM 17α-hydroxypregnenolone/rhP450c17, 1.2 µM/5 µM 17α-hydroxyprogesterone /rat testicular microsomes) of cytochrome P450 17A1 (CYP17A1; P450c17), while inhibiting only human & monkey, but not rat, CYP17A 17α-hydroxylase activity (IC50/[substrate] = 38 nM/5 µM pregnenolone/monkey adrenal microsomes, 760 nM/5 µM pregnenolone/rhP450c17, >10 µM/5 µM progesterone/rat testicular microsomes) and exhibiting much reduced or little potency against 11β-hydroxylase activity (IC50 >1 µM/rat testicular microsomes & >10 µM/monkey adrenal microsomes) or 9 other human CYP isoforms (IC50 = 14 µM/2C19 & >30 µM/1A2, 2A6, 2B6, 2C8, 2C9, 2D6, 2E1, 3A4). Consistent with its enzyme inhibition activity, TAK-100 is shown to cause cellular progesterone built-up and reduce dehydroepiandrosterone (DHEA) & androstenedione production in human adrenocortical tumor cell NCI-H295R (IC50 = 37 & 54 nM, respectively), ATCH-stimulated primary monkey adrenal cell (IC50 = 110 & 130 nM, respectively), and hCG-stimulated primary rat testicular cell (IC50 = 210 nM against androstenedione production) cultures with greater potency and selectivity than Ketoconazole (Cat. No. 420600). Oral administration is reported to result in reduced serum steroid levels in vivo among male cynomolgus monkeys (0.3 to 10 mg/kg for single & 3 to 15 mg/kg/12 h for multiple oral dosing) with or without castration and hypophysectomized male rats (30 to 300 mg/kg for single & 37.5 to 600 mg/kg/8 h for multiple oral dosing).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number566939-85-3
Chemical formulaC₁₈H₁₇N₃O₂
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml)
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesDreicer, R., et al. 2014. Clin. Cancer Res. 20, 1335.
Yin, L. and Hu, Q., 2014. Nat. Rev. Urol. 11, 32.
Hara, T., et al. 2013.J. Steroid Biochem. Mol. Biol. 134, 80.
Yamaoka, M., et al. 2012. J. Steroid Biochem. Mol. Biol. 129, 115.
Kaku, T., et al. 2011. Bioorg. Med. Chem. 19, 6383.

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Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest