1. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  2. PROTACs Androgen Receptor Apoptosis
  3. PROTAC AR Degrader-8

PROTAC AR Degrader-8 (Compound NP18) 是雄激素受体 (AR) 的 PROTAC 降解剂,可在 22Rv1 细胞和 LNCaP 细胞中降解 AR-FLDC50 为 0.018 μM 和 0.14 μM 的,在 22Rv1 细胞中降解AR-V7DC50 为 0.026 μM。PROTAC AR Degrader-8 可抑制癌细胞 22Rv1 和 LNCaP 的增殖,IC50 分别为 0.038 μM 和 1.11 μM。 PROTAC AR Degrader-8 在 G2/M 期阻滞细胞周期,诱导 22Rv1 细胞发细胞凋亡 (apoptosis)。PROTAC AR Degrader-8 在小鼠和斑马鱼模型中表现出抗癌活性。

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PROTAC AR Degrader-8 Chemical Structure

PROTAC AR Degrader-8 Chemical Structure

CAS No. : 3044108-04-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model[1]. (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))

分子量

703.78

Formula

C40H41N5O7

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:
PROTAC AR Degrader-8
目录号:
HY-170329
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