ASP-9521 |
| Catalog No.GC32936 |
ASP-9521은 인간 AKR1C3에 대해 IC50이 11nM인 강력하고 선택적이고 경구로 이용 가능한 AKR1C3 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1126084-37-4
Sample solution is provided at 25 µL, 10mM.
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ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
AKR1C3 is a promising therapeutic target in castrationresistant prostate cancer, as combination of an AKR1C3 inhibitor and a gonadotropin-releasing hormone analogue may lead to complete androgen blockade.ASP-9521 inhibits conversion of androstenedione (AD) into androstenediol and testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 in a concentrationdependent manner (IC50, human: 11 nM; IC50,monkey: 49 nM). ASP-9521 shows more than 100-fold selectivity for AKR1C3 over the isoform AKR1C2. In LNCaP-AKR1C3 cells, ASP-9521 suppresses AD-dependent PSA production and cell proliferation[1].
In CWR22R xenografts, single oral administration of ASP-9521 (3 mg/kg) inhibits AD-induced intratumoural T production and this inhibitory effect is maintained for 24 h. After oral administration, ASP-9521is rapidly eliminated from plasma, while its intratumoural concentration remained high. The bioavailability of ASP-9521 after oral administration (1 mg/kg) is 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively[1].
[1]. Kikuchi A, et al. In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).Invest New Drugs. 2014 Oct;32(5):860-70.
Cell experiment: | LNCaP-AKR1C3 cells stably expressing human AKR1C3 are seeded in 96-well plates at 10000 cells/100 μL/well in RPMI-1640 medium supplemented with heat-inactivated charcoal-dextran-stripped FBS (1 % for the PSA expression assay and T measurement and 5 % for the cell proliferation assay). After 24 h incubation, AD is added to each well with or without ASP-9521 (0.3-100 nM). The cell culture media are collected 24 h after administration of AD to measure T concentration and 6 days after administration of AD to measure cell proliferation using Cell-Titer Glo assay[1]. |
Animal experiment: | Mice carrying HEK293 or HEK293-AKR1C3 tumours with similar sizes are selected and randomly divided into 5 groups (N=3 for each group). All groups are treated with ASP-9521 (single oral administration; 3 mg/kg). Plasma (from the central vein) and tumour tissues are collected at 0.25, 0.5, 1, 2 and 4 h after administration of ASP-9521, and ASP-9521 concentrations are determined using the HPLCMS/MS method[1]. |
References: [1]. Kikuchi A, et al. In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).Invest New Drugs. 2014 Oct;32(5):860-70. | |
| Cas No. | 1126084-37-4 | SDF | |
| Canonical SMILES | O=C(N1CCC(CC(C)(O)C)CC1)C(N2)=CC3=C2C=CC(OC)=C3 | ||
| Formula | C19H26N2O3 | M.Wt | 330.42 |
| Solubility | DMSO : ≥ 300 mg/mL (907.94 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0265 mL | 15.1323 mL | 30.2645 mL |
| 5 mM | 0.6053 mL | 3.0265 mL | 6.0529 mL |
| 10 mM | 0.3026 mL | 1.5132 mL | 3.0265 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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