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TAK-700 R-form

17, 20-lyase inhibitor CAS# 752243-39-3

TAK-700 R-form

Catalog No. BCC4203----Order now to get a substantial discount!

Product Name & Size Price Stock
TAK-700 R-form:5mg $103.00 In stock
TAK-700 R-form:10mg $175.00 In stock
TAK-700 R-form:25mg $412.00 In stock
TAK-700 R-form:50mg $721.00 In stock
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Quality Control of TAK-700 R-form

Quality Control & MSDS

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Chemical structure

TAK-700 R-form

3D structure

Chemical Properties of TAK-700 R-form

Cas No. 752243-39-3 SDF Download SDF
PubChem ID 10335364 Appearance Powder
Formula C18H17N3O2 M.Wt 307.35
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
Chemical Name 6-[(7R)-7-hydroxy-5,6-dihydropyrrolo[1,2-c]imidazol-7-yl]-N-methylnaphthalene-2-carboxamide
SMILES CNC(=O)C1=CC2=C(C=C1)C=C(C=C2)C3(CCN4C3=CN=C4)O
Standard InChIKey OZPFIJIOIVJZMN-GOSISDBHSA-N
Standard 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

TAK-700 R-form Dilution Calculator

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TAK-700 R-form Molarity Calculator

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Preparing Stock Solutions of TAK-700 R-form

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.2536 mL 16.2681 mL 32.5362 mL 65.0724 mL 81.3405 mL
5 mM 0.6507 mL 3.2536 mL 6.5072 mL 13.0145 mL 16.2681 mL
10 mM 0.3254 mL 1.6268 mL 3.2536 mL 6.5072 mL 8.134 mL
50 mM 0.0651 mL 0.3254 mL 0.6507 mL 1.3014 mL 1.6268 mL
100 mM 0.0325 mL 0.1627 mL 0.3254 mL 0.6507 mL 0.8134 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on TAK-700 R-form

TAK-700 R-form is a highly selective inhibitor of 17, 20-lyase with IC50 value of 38nM [1].

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 [1].

References:
[1] Kaku T, Hitaka T, Ojida A, et al. Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17, 20-lyase inhibitor with potential utility in the treatment of prostate cancer. Bioorganic & medicinal chemistry, 2011, 19(21): 6383-6399.

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