1. Apoptosis GPCR/G Protein MAPK/ERK Pathway Protein Tyrosine Kinase/RTK
  2. Apoptosis Raf Ras ROS Kinase MDM-2/p53
  3. Antitumor agent-60

Antitumor agent-60 (compound 20) 是一种有效的抗肿瘤活性分子,靶向 RAS-RAF 信号通路,能与 CRAF 结合,Kd 值为 721.3 nM。Antitumor agent-60 通过将细胞阻滞在 G2/M 期诱导细胞凋亡 (apoptosis)。Antitumor agent-60 能提高癌细胞中 p53ROS 水平,造成细胞核呈椭圆形和不规则形态。Antitumor agent-60 在 A549 肿瘤移植模型中表现出一定的抑制肿瘤生长能力。

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Antitumor agent-60 Chemical Structure

Antitumor agent-60 Chemical Structure

CAS No. : 865784-65-2

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生物活性

Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model[1].

IC50 & Target

IC50: 12 nM in A549, 19 nM in OVCaR-3, 29 nM in SGC-7901, 22 nM in HCT-116[1]
Kd: 721.3 nM (CRAF RBD)[1]

分子量

508.54

Formula

C24H28O10S

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.

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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:
Antitumor agent-60
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HY-146432
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