Capecitabine is an oral prodrug that is converted to its active metabolite, 5-FU, by thymidine phosphorylase.

DNA/RNA Synthesis^[1]

Capecitabine is an anti-cancer chemotherapy drug. It is classified as an antimetabolite. Capecitabine is converted into 5′-deoxy-5-fluorocytidine (5′DFCR), 5′-deoxy-5-fluorouridine (5′DFUR) and 5-FU by carboxylesterases (CES1 and 2), cytidine deaminase (CDD), and thymidine phosphorylase (TP), in both liver and tumour. Capecitabine induces a significant cytotoxic effect in vitro only at high concentrations. Mean IC₅₀ values vary from 860 μM in COLO205 cells to 6000 μM in HCT8 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.

A pharmacokinetic/pharmacodynamic study is carried out in mice bearing HCT 116 xenografts receiving 0.52 and 2.1 mmol/kg/d of Capecitabine by oral gavage. Capecitabine administered at 0.52 mmol/kg/day induces partial control of HCT 116 xenografts tumour growth: growth rate =7.5±0.5 on day 21. Capecitabine 2.1 mmol/kg/day achieves complete control of tumor growth during the treatment period: growth rate =1±0.2 on day 21^[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.

359.35

C₁₅H₂₂FN₃O₆

154361-50-9

卡培他滨

Room temperature in continental US; may vary elsewhere.

DMSO : 250 mg/mL (695.70 mM; Need ultrasonic)

H₂O : ≥ 33.33 mg/mL (92.75 mM)

* “≥” means soluble, but saturation unknown.

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。-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： PBS

  Solubility: 25 mg/mL (69.57 mM); Clear solution; Need ultrasonic
• 2.

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

  Solubility: ≥ 2.08 mg/mL (5.79 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.79 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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

• 3.

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

  Solubility: ≥ 2.08 mg/mL (5.79 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.79 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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
• 4.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.79 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.79 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. PharmD CM, et al. Capecitabine: A review. Clinical Therapeutics. 2005 Jan; 27(1): 23-44.

  [2]. Guichard SM, et al. Gene expression predicts differential capecitabine metabolism, impacting on both pharmacokinetics and antitumour activity. Eur J Cancer. 2008 Jan;44(2):310-7.

HCT 116, HCT8, HCT15, HT29, SW620 and COLO205 human colon cancer cells are used. Cells are plated on day 1 in 96-well plates at a density of 2500 cells/well for HCT 116, 3500 cells/well for HCT8 and HT29, 5000 cells/well for HCT15, 6000 cells/well for SW620 and 7000 cells/wells for COLO205 in a volume of 150 μL/well. All cell lines are treated on day 2 with increasing concentrations of Capecitabine (0.1-10 mM), 5′DFCR (10 nM-100 μM), 5′DFUR (2.5-500 μM) or 5-FU (0.5-250 μM) for 24 h. After drug exposure, cells are washed once with cold PBS and placed in 200 μL of drug-free medium for 72 h after the end of drug exposure. The cells are then fixed with trichloroacetic acid and stained with sulforhodamine B. Optical densities are measured at 540 nm with a Biohit BP-800. The results are based on three independent experiments performed in triplicate^[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]
Six-week-old C57/Bl6 Nu/Nu mice are used. Bilateral HCT 116 xenografts are obtained by subcutaneous injection of 10⁷ cells/flank. Animals bearing HCT 116 xenografts are treated with vehicle or Capecitabine 0.52 or 2.1 mmol/kg (563 and 2250 mg/m², respectively) given once daily for 5 consecutive days/week by oral gavage for 3 weeks (days 0-4, 7-11, 14-18). Animals are culled on day 0 at 15, 30 min, 1, 2, 4, 8 and 24 h, and prior to planned treatment on days 7 and 14 after the start of treatment. Three animals per time-point are analysed. At the time of collection, blood is collected in heparin, and plasma isolated and stored at −80°C. The liver is removed immediately and stored in RNAlater solution. Tumours are macro-dissected to remove fibrotic tissue and blood vessels and snap-frozen in liquid nitrogen.

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]. PharmD CM, et al. Capecitabine: A review. Clinical Therapeutics. 2005 Jan; 27(1): 23-44.

  [2]. Guichard SM, et al. Gene expression predicts differential capecitabine metabolism, impacting on both pharmacokinetics and antitumour activity. Eur J Cancer. 2008 Jan;44(2):310-7.