Napabucasin (BBI608) is aSTAT3inhibitor which blocks stem cell activity incancercells.

Napabucasin inhibits the expressions of stemness markers and kill stemness-high cancer cells isolated from several kinds of tumors except PCa. Napabucasin not only inhibits cell proliferation, cell motility, cell survival, colony formation ability, and tumorigenic potential of PCa cells, and increases cell apoptosis and sensitivity to docetaxel, but also effectively blocks sphere formation of PrCSCs and kill them as well as inhibits stemness gene expression. Napabucasin inhibits cell proliferation in PC-3 cells and 22RV1 cells at 48, 72, 96, and 120 h (P<0.05). Cell motility and colony formation ability are closely correlated with the process of tumor metastasis. Napabucasin significantly decreases colony formation and cell motility ability of PCa cell lines in vitro (P<0.05). The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin are significantly decreased from day 2 to 5 compared with the control group (P<0.05)^[1].

Napabucasin (40 mg/kg) or Docetaxel significantly reduces xenograft tumor growth and tumor volume (TV) compared with PBS (P<0.05). Notably, while no differences are observed between the Napabucasin and the docetaxel groups in PC-3 mouse xenograft models, the TV in Napabucasin group is even lower than docetaxel group in 22RV1 mouse xenograft models (P<0.05). Additionally, Napabucasin or docetaxel also significantly reduces tumor weight compared with PBS (P<0.05)^[1].

240.21

Solid

C₁₄H₈O₄

83280-65-3

Room temperature in continental US; may vary elsewhere.

DMSO : 4.44 mg/mL(18.48 mM;Need ultrasonic)

H₂O :< 0.1 mg/mL(insoluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: 0.5 mg/mL (2.08 mM); Suspended solution; Need ultrasonic

  此方案可获得 0.5 mg/mL (2.08 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 0.5 mg/mL (2.08 mM); Suspended solution; Need ultrasonic

  此方案可获得 0.5 mg/mL (2.08 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 0.5 mg/mL (2.08 mM); Clear solution

  此方案可获得 ≥ 0.5 mg/mL (2.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。