OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI₅₀s in the nanomolar range in human cancer lines.

OSBP/ORP4^[1].

OSW-1 has a strong inhibitory effect on colon carcinoma cells with low cytotoxicity on normal cells. The anti-proliferative effects of OSW-1 on SW480 and LoVo colon carcinoma cells are characterized by measuring cell viability using the CCK8 assay, and compared the results with other clinical anticancer agents. SW480 and LoVo cell lines are derived from a Dukes’ stage B colon carcinoma and a colon carcinoma metastatic nodule, which represent non-metastatic and metastatic carcinomas, respectively. OSW-1 exhibits not only extremely strong anticancer activity in SW480 and LoVo cell lines with an IC₅₀ of nanomolar concentration, but is also more potent than other anticancer agents by 10-100 times, with a lower cytotoxic effect on normal epithelial cells. These results indicate that OSW-1 has a powerful anticancer effect, but lower cytotoxic effect on normal cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

To ascertain whether or not OSW-1 is as effective in vivo, a nude mouse model inoculated by LoVo cells is adopted, in which OSW-1 treatment is performed when tumors became palpable. The results show that the size of tumors in treated mice is smaller on average than control mice. The significant difference is observed from the 15-17 th day following treatment, and this difference is gradually increased until the animals are sacrificed. Compared with the control group, the tumor weight of the OSW-1-treated group significantly decreases (P<0.05). Additionally, no apparent side effects are observed in OSW-1-treated mice. These results demonstrate that OSW-1 has powerful effects on suppressing colon tumor growth without significant side effects in vivo^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

873.03

C₄₇H₆₈O₁₅

145075-81-6

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

DMSO : 100 mg/mL (114.54 mM; Need ultrasonic)

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°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 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: ≥ 2.5 mg/mL (2.86 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (2.86 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 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-CD in saline)

  Solubility: ≥ 2.5 mg/mL (2.86 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (2.86 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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: ≥ 2.5 mg/mL (2.86 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (2.86 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Burgett AW, et al. Natural products reveal cancer cell dependence onoxysterol-binding proteins.Nat Chem Biol. 2011 Aug 7;7(9):639-47.

  [2]. Zhang Y, et al, Effective cytotoxic activity of OSW-1 on colon cancer by inducing apoptosis in vitro and in vivo.Oncol Rep. 2017 Jun;37(6):3509-3519.

To observe the effect of OSW-1 on cell viability, the colon cancer cell lines LoVo and SW480 cells are seeded in 96-well plates at a concentration of 1×10⁵ cells/well. Following overnight incubation, the cells are treated with several concentrations of OSW-1 (11.25, 22.5, 45, 90, 180 ng/mL) and incubated at 37°C in 5% CO₂ for 24, 48, and 72 h. Cell viability analysis is determined using a Cell Counting Kit-8 Assay. Each assay is performed in quintuplicate and repeated three times^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[2]
Four-week-old male nude mice are used. Animals are acclimatized to the animal housing facility for a period of 7 days before the beginning of the experiments. LoVo human colon cancer cells (5×10⁶ cells in 100 μL) are injected subcutaneously into the right flank of 18 nude mice. When the tumor becomes palpable, the nude mice are randomized into two groups: i) intraperitoneal injection of PBS (500 μL) daily in 9 nude mice; and ii) intraperitoneal injection of OSW-1 (0.01 mg/kg diluted in PBS in 500 μL) daily in 9 nude mice. The body weights of the animals and tumor size are recorded every day, and the tumor volume is calculated^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Burgett AW, et al. Natural products reveal cancer cell dependence onoxysterol-binding proteins.Nat Chem Biol. 2011 Aug 7;7(9):639-47.

  [2]. Zhang Y, et al, Effective cytotoxic activity of OSW-1 on colon cancer by inducing apoptosis in vitro and in vivo.Oncol Rep. 2017 Jun;37(6):3509-3519.