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