1. Vitamin D Related/Nuclear Receptor PROTAC
  2. Androgen Receptor PROTACs
  3. AZ'3137

AZ‘3137 (Compound 22) 是一种口服有效的 PROTAC 类的雄激素受体 (AR) 降解剂, DC50 值为 22 nM。AZ‘3137 可以抑制 LNCaP 的细胞增殖,GI50 值为 74 nM。 AZ‘3137 可以抑制前列腺癌小鼠中的 AR 信号传导和肿瘤生长 (红色: AR 拮抗剂; 蓝色: CRBN ligand (HY-A0003); 黑色: linker)。

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AZ'3137 Chemical Structure

AZ'3137 Chemical Structure

CAS No. : 2960179-55-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker)[1].

体外研究
(In Vitro)

AZ'3137 (Compound 22) 可以抑制 AR 信号传导和前列腺癌细胞系 LNCaP 的细胞增殖[1]

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

Cell Proliferation Assay[1].

Cell Line: LNCaP cells
Concentration: 0-10 μM
Incubation Time: 7 days
Result: Inhibited the proliferation of LNCaPs with a GI50 value of 74 nM.
体内研究
(In Vivo)

AZ'3137 (Compound 22) 在前列腺癌小鼠中抑制肿瘤生长[1]

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

Animal Model: Immunocompromised NOD SCID male mice implanted with C4-2 cell subcutaneous tumors[1].
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily
Result: Degraded AR and inhibited tumor growth.
分子量

801.87

Formula

C43H47F4N7O4

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
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  • 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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产品名称:
AZ'3137
目录号:
HY-162702
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