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Napabucasin {[allProObj[0].p_purity_real_show]}

货号:A113651 同义名: BBI608

Napabucasin(BBI608)是一种STAT3抑制剂,阻断癌细胞中的干细胞活性。

Napabucasin 化学结构 CAS号:83280-65-3
Napabucasin 化学结构
CAS号:83280-65-3
Napabucasin 3D分子结构
CAS号:83280-65-3
Napabucasin 化学结构 CAS号:83280-65-3
Napabucasin 3D分子结构 CAS号:83280-65-3
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Napabucasin 纯度/质量文件 产品仅供科研

货号:A113651 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 STAT1 STAT3 STAT5 其他靶点 纯度
Nifuroxazide 98%
Fludarabine 98%
Artesunate 98%
BP-1-102 +++

STAT3, Kd: 504 nM

99%+
Niclosamide ++

STAT3, IC50: 0.7 μM

98%
Napabucasin 98%
Cryptotanshinone ++

STAT3, IC50: 4.6 μM

98%
Stattic +

STAT3, IC50: 5.1 μM

98%
NSC 74859 +

STAT3, IC50: 86 μM

99%+
Ochromycinone 98%
HO-3867 97%
C188-9 ++++

STAT3, Kd: 4.7 nM

99%+
HJC0152 98%
SH5-07 97%
SH-4-54 ++++

STAT3, Kd: 300 nM

+++

STAT5, Kd: 464 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Napabucasin 生物活性

靶点
  • STAT3

描述 Napabucasin targets stemness markers, effectively killing stemness-high cancer cells from various tumors, except in prostate cancer (PCa). It inhibits PCa cell proliferation, motility, survival, and colony formation, while increasing apoptosis and sensitivity to docetaxel. Napabucasin also blocks sphere formation and kills prostate cancer stem cells (PrCSCs) and suppresses stemness gene expression. In PC-3 and 22RV1 cells, it reduces proliferation significantly from day 2 to 5 compared to controls (P<0.05) [1].
体内研究

Napabucasin (40 mg/kg) or Docetaxel significantly reduces tumor growth and volume in xenograft models, with Napabucasin showing even lower tumor volumes than Docetaxel in 22RV1 models (P<0.05). Both treatments also significantly reduce tumor weight compared to PBS (P<0.05) [1].

体外研究

Napabucasin targets stemness markers, effectively killing stemness-high cancer cells from various tumors, except in prostate cancer (PCa). It inhibits PCa cell proliferation, motility, survival, and colony formation, while increasing apoptosis and sensitivity to docetaxel. Napabucasin also blocks sphere formation and kills prostate cancer stem cells (PrCSCs) and suppresses stemness gene expression. In PC-3 and 22RV1 cells, it reduces proliferation significantly from day 2 to 5 compared to controls (P<0.05) [1].

Napabucasin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human DU145 cells Function assay 72 h Anticancer activity against human DU145 cells after 72 hrs by XTT assay, IC50=0.02304 μM 18829316
human HaCaT cells Function assay 48 h Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy, IC50=0.5 μM 22845014
human HaCaT cells Proliferation assay Antiproliferative activity against human HaCaT cells, IC50=0.5 μM 10479319
KB cells Cytotoxic assay Effective cytotoxic dose against KB cells was evaluated, ED50=4.2 μM 9873618

Napabucasin 动物研究

Dose Mice: 40 mg/kg[3] (i.p.)
Administration i.p.

Napabucasin 参考文献

[1]Zhang Y, et al. Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin. Cancer Med. 2016 Jun;5(6):1251-8.

Napabucasin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.16mL

0.83mL

0.42mL

20.82mL

4.16mL

2.08mL

41.63mL

8.33mL

4.16mL

Napabucasin 技术信息

CAS号83280-65-3
分子式C14H8O4
分子量 240.211
别名 BBI608
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 4 mg/mL(16.65 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

5% DMSO+40% PEG 300+5% Tween 80+water 1 mg/mL

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