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HomeProduct name listASP-9521

ASP-9521

ASP-9521 Structural

What is ASP-9521?

Description

ASP9521 is an inhibitor of 17β-hydroxysteroid dehydrogenase type 5/aldo-keto reductase 1C3 (17β-HSD5/AKR1C3; IC50 = 120 nM). 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.

The Uses of ASP-9521

ASP 9521 is a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3). AKR1C3 is a promising therapeutic target in castration-resistant prostate cancer

Properties of ASP-9521

Boiling point: 543.9±30.0 °C(Predicted)
Density  1.183±0.06 g/cm3(Predicted)
storage temp.  Sealed in dry,Store in freezer, under -20°C
solubility  DMSO:52.26(Max Conc. mg/mL);158.16(Max Conc. mM)
DMF:10.0(Max Conc. mg/mL);30.26(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.51(Max Conc. mM)
Ethanol:36.35(Max Conc. mg/mL);110.01(Max Conc. mM)
form  A crystalline solid
pka 15.23±0.29(Predicted)
color  Light yellow to yellow

Safety information for ASP-9521

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for ASP-9521

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