| Description |
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP)[1].
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| Related Catalog |
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| In Vitro |
A031 (0.125-1.000 μM) 对雄激素受体具有抑制作用，IC50 值小于 0.25 μM[1]。 A031 (2 μM; 2-4.5 h) 可降低 VCaP 细胞系中雄激素受体蛋白水平[1]。 Western Blot Analysis[1] Cell Line: VCaP cell lines Concentration: 2 μM Incubation Time: 2, 3.5 and 4.5 hours Result: Reduced the AR protein level, and AR proteins was almost degraded after 4.5 h treatment.
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| In Vivo |
A031 (2.8，8.3 和 25 μM；加入到培养溶液中，共五天) 能抑制斑马鱼中前列腺肿瘤的生长。 1.19Pharmacokinetic Properties of A031 in Rats[1]. Rats IV 1 mg/kg t1/2 (h) 0.57 Cmax (ng/mL) 14366.2 AUClast (h·ng/mL) 1773.8 AUCINF_pred (h·ng/mL) 1773.8 Vz_pred (L/kg) 0.47 Cl_pred (L/h/kg) 0.57 Animal Model: Wild type AB strain zebrafish with human prostate cancer (VCap) cells transplantatio[1] Dosage: 2.8, 8.3 and 25 μM Administration: Aqueous solution culture, at 35℃, for 5 days Result: Inihibited tumor growth with growth inhibition rates of 28%, 55% and 61% at 2.8, 8.3 and 25 μM, respectively.
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| References |
[1]. Chen L, et al. Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer. Eur J Med Chem. 2021 Apr 15;216:113307.
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