A031

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A031

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CAS NO:

2682255-44-1

A031 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂，对 AR 蛋白具有降解作用，IC₅₀值小于 0.25 μM。A031 抑制移植人前列腺癌 (VCaP) 的斑马鱼的肿瘤生长。

生物活性

A031 is a highly effective PROTACandrogen receptor(AR) degrader with anIC₅₀value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostatecancer(VCaP)^[1].

体外研究
(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.

体内研究
(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
t_1/2(h)	0.57
C_max(ng/mL)	14366.2
AUC_last(h·ng/mL)	1773.8
AUC_{INF_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.

分子量

981.60

Formula

C₅₀H₆₁ClN₁₀O₇S

CAS 号

2682255-44-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.