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ASP9521

Cat. No. M8976
ASP9521 Structure
Synonym:

ASP-9521

Size Price Availability Quantity
5mg USD 300 In stock
10mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

ASP9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3. ASP9521 inhibited conversion of androstenedione (AD) into testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 in a concentration-dependent manner (IC50,human: 11 nmol/L; IC50,monkey: 49 nmol/L). ASP9521 showed >100-fold selectivity for AKR1C3 over the isoform AKR1C2. In LNCaP-AKR1C3 cells, ASP9521 suppressed AD-dependent PSA production and cell proliferation.

In vivo, single oral administration of ASP-9521 (3 mg/kg) inhibits AD-induced intratumoural T production in CWR22R xenografts, and this inhibitory effect is maintained for 24 h. After oral administration, ASP-9521 is rapidly eliminated from plasma, while its intratumoural concentration remained high. The bioavailability of ASP9521 after oral administration (1 mg/kg) is 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively.

Protocol
Cell Experiment
Cell lines LNCaP-AKR1C3 cells stably expressing human AKR1C3
Preparation method 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.
Concentrations 0.3-100 nM
Incubation time 24 h
Animal Experiment
Animal models Mice carrying HEK293 or HEK293-AKR1C3 tumours
Formulation 0.5 % methyl cellulose
Dosages 3 mg/kg
Administration single oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 330.42
Formula C19H26N2O3
CAS Number 1126084-37-4
Purity >98%
Solubility DMSO: ≥ 100 mg/mL
Storage at -20°C
References

In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
Kikuchi A, et al. Invest New Drugs. 2014 Oct;32(5):860-70. PMID: 24981575.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ASP9521, ASP-9521 supplier, inhibitors

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