1. PROTAC Vitamin D Related/Nuclear Receptor
  2. PROTACs Androgen Receptor
  3. A031

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。

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A031 Chemical Structure

A031 Chemical Structure

CAS No. : 2682255-44-1

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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。
1.19 Pharmacokinetic 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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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A031
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HY-148777
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