产品
编 号：F754596
分子式：C50H61ClN10O7S
分子量：981.6
分子式：C50H61ClN10O7S
分子量：981.6
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CAS No: 2682255-44-1
产品详情
生物活性：
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).
体内研究：
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. RatsIV1 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
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.
体外研究：
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。A031 (2 μM; 2-4.5 h) 可降低 VCaP 细胞系中雄激素受体蛋白水平。
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).
体内研究：
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. RatsIV1 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
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.
体外研究：
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。A031 (2 μM; 2-4.5 h) 可降低 VCaP 细胞系中雄激素受体蛋白水平。
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