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ASP-9521 Sale

(Synonyms: 1-[1-[(5-甲氧基-1H-吲哚-2-基)羰基]哌啶-4-基]-2-甲基丙-2-醇) 目录号 : GC32936

An inhibitor of 17β-HSD5/AKR1C3

ASP-9521 Chemical Structure

Cas No.:1126084-37-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥594.00
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5mg
¥540.00
现货
10mg
¥891.00
现货
50mg
¥3,555.00
现货
100mg
¥5,135.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

ASP9521 is an inhibitor of 17β-hydroxysteroid dehydrogenase type 5/aldo-keto reductase 1C3 (17β-HSD5/AKR1C3; IC50 = 120 nM).1 It is selective for 17β-HSD5/AKR1C3 over AKR1C2 (IC50 = 20 μM). ASP9521 inhibits conversion of androstenedione into testosterone by 17β-HSD5/AKR1C3 (IC50s = 11 and 49 nM for human and cynomolgus monkey enzymes, respectively). It inhibits androstenedione-dependent production of prostate specific androgen (PSA) in and proliferation of LNCaP cells expressing 17β-HSD5/AKR1C3. ASP9521 (3 and 10 mg/kg) inhibits androstenedione-induced intratumor testosterone production in a CWR22R prostate cancer mouse xenograft model.

1.Kikuchi, A., Furutani, T., Azami, H., 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 Drugs32(5)860-870(2014)

实验参考方法

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.

化学性质

Cas No. 1126084-37-4 SDF
别名 1-[1-[(5-甲氧基-1H-吲哚-2-基)羰基]哌啶-4-基]-2-甲基丙-2-醇
Canonical SMILES O=C(N1CCC(CC(C)(O)C)CC1)C(N2)=CC3=C2C=CC(OC)=C3
分子式 C19H26N2O3 分子量 330.42
溶解度 DMSO : ≥ 300 mg/mL (907.94 mM) 储存条件 Store at -20°C
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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
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