What is Capecitabine?
Capecitabine is an antimetabolic fluorouracil deoxynucleoside carbamate product that can be converted into 5-FU in vivo, which can inhibit cell division and interfere with RNA and protein synthesis. It is suitable for the further treatment of advanced primary or metastatic breast cancer which is ineffective by paclitaxel and chemotherapy schemes including anthracycline antibiotics.
| Product name | Capecitabine |
| CAS | 154361-50-9 |
| Molecular formula | C15H22FN3O6 |
| Molecular weight | 359.35 |
| EINECS Number | 604-948-1 |
| Storage condition | 2-8°C |
| Melting point | 110-121°C |
| Solubility | H2O: soluble 10mg/mL, transparent (heated) |
| Appearance | White to off-white powder |
| Boiling point | 517.6±60.0 °C at 760 mmHg |
| Density | 1.49±0.1 g/cm3(Predicted) |
How does capecitabine work?
Capecitabine powder can be quickly absorbed by intestinal mucosa and converted into an intermediate product called 5- deoxy -5-fluorouridine in liver. Subsequently, this intermediate enters the tumor tissue and is converted into 5- fluorouracil (5-FU).
People should be familiar with 5-FU. This is one of the earliest anti-tumor drugs synthesized in the world, and it is also the most widely used anti-pyrimidine drug in the world. 5-FU plays an anti-tumor role mainly by inhibiting DNA synthesis of tumor cells.
Product Specification
| Item | Specification | Results |
| Appearance | White or off-white solid powder | Complies |
| Identification | By IR | Complies |
| By HPLC | Complies | |
| Solubility | Soluble in DMF,sparingly soluble in THF, slightly soluble in methanol and acetonitrile, very sightly soluble in ethanol and dichloromethane,insoluble in water |
Complies |
| Polymorphic Form | Polymorphic form 1 | Complies |
| Melting Point | 211C~216℃ | 212.8℃~214.9C |
| Water Content | ≤0.50% | 0.10% |
| Heavy Metals | ≤20ppm | Complies |
| Residue on Ignition | ≤0.20% | 0.09% |
| Rela ted Substance | Any single impurity:≤0.10% | 0.06% |
| Total Impurities:≤1.00% | 0.16% | |
| Assay (on the anhydrous basis) |
98.0%~102.0% | 99.94% |
| Particle Size | D90:≤100μm | Complies |
| Conclusion: | Conform with enterprise specification. | |
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What are the effects of Capecitabine?
Capecitabine works by interfering with nucleic acid synthesis, blocking energy metabolism and angiogenesis, and has anti-tumor effects.
1. Interfering with nucleic acid synthesis
Capecitabine is an oral chemotherapy drug that can be converted into an active metabolite, fluorouracil, by the inner wall environment of tumor cells, thereby inhibiting the synthesis of DNA and RNA. This effect can cause cancer cell growth to be inhibited or stop in a specific growth period, thereby controlling its proliferation ability.
2. Blocking energy metabolism
Capecitabine powder can affect the energy supply of tumor tissue by interfering with key enzymes in the folate metabolic pathway. Insufficient energy supply will limit the division rate of cancer cells and prompt them to consume reserve glycogen to maintain survival.
3. Inhibiting angiogenesis
Capecitabine can reduce the production of multiple factors required for new blood vessel formation, and to a certain extent, indirectly kill micro-metastases; it can also reduce the permeability of existing capillaries, increase the pressure inside the tumor and promote liquefaction and absorption of necrotic areas.
4. Reversing drug resistance
A systematic study of tumor cell models that have developed multidrug resistance found that capecitabine can restore the sensitivity of these cells to paclitaxel and other commonly used anticancer drugs.
5. Improving the quality of life of patients
Compared with traditional chemotherapy regimens, it can reduce the physical discomfort and psychological burden caused by symptoms such as nausea, vomiting, and hair loss, and help improve patients' daily activities and overall quality of life.
HTML5 atlas of Capecitabine
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Biological activity of Agmatine sulfate:
| Describe | Capecitabine is an orally available prodrug that is converted to its active metabolite, Fluorouracil (FU), by thymidine phosphorylase. |
| In vitro studies | Capecitabine is an anticancer chemotherapeutic agent. It is classified as an antimetabolite. Capecitabine is converted to 5'-deoxy-5-fluorocytidine (5'DFCR), 5'-deoxy-5-fluorouridine (5'DFUR) and 5-fluorouracil (5-FU) by carboxylesterases (CES1 and 2), cytidine deaminases (CDD) and thymidine phosphorylase (TP), in the liver and tumors. Capecitabine induces significant cytotoxic effects in vitro only at high concentrations. The mean IC50 values ranged from 860 μM in COLO205 cells to 6000 μM in HCT8 cells [2]. |
| In vivo studies | A pharmacokinetic/pharmacodynamic study was conducted in mice bearing HCT 116 xenografts, receiving 0.52 and 2.1 mmol/kg/day of capecitabine by oral gavage. Capecitabine administered at 0.52 mmol/kg/day induced partial control of HCT116 xenograft tumor growth: growth rate = 7.5 ± 0.5 on day 21. Capecitabine 2.1 mmol/kg/day achieved complete control of tumor growth during treatment: growth rate = 1 ± 0.2 on day 21 [2]. |
| Cell experiments | HCT 116, HCT8, HCT15, HT29, SW620 and COLO205 human colon cancer cells were used. Cells were plated in 96-well plates on day 1 at a density of 2500 cells/well for HCT116, 3500 cells/well for HCT8 and HT29, 5000 cells/well for HCT15, 6000 cells/well for SW620 and 7000 cells/well for COLO205. The volume was 150 μL/well for COLO205. All cell lines were 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 hours. After drug exposure, cells were washed once with cold PBS and placed in 200 μL of drug-free medium for 72 hours after the end of drug exposure. The cells were then fixed with trichloroacetic acid and stained with sulforhodamine B. Optical density was measured at 540 nm using a Biohit BP-800. Results are based on three independent experiments performed in triplicate [2]. |
| Animal experiments | Mice[2] Six-week-old C57/Bl6 Nu/Nu mice were used. Bilateral HCT 116 xenografts were obtained by subcutaneous injection of 107 cells/flank. Animals bearing HCT 116 xenografts were treated with vehicle or capecitabine 0.52 or 2.1 mmol/kg (563 and 2250 mg/m2, respectively) once daily for 5 days/week by oral gavage for 3 weeks (days 0-4, 7-days 11,14-18). Animals were culled on day 0, at 15, 30 minutes, 1 hour, 2 hours, 4 hours, 8 hours, and 24 hours, and before planned treatment on days 7 and 14 after the start of treatment. Three animals were analyzed for each time point. At the time of collection, blood was collected in heparin and plasma was separated and stored at -80°C. The liver was immediately removed and stored in RNAlater solution. Tumors were macrodissected to remove fibrotic tissue and blood vessels and snap-frozen in liquid nitrogen. |
| References |
[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. |
What is the difference between capecitabine and 5-Fluorouracil?
1, the product composition is different
The main component of capecitabine is capecitabine powder, while the main component of 5-Fluorouracil is 5-Fluorouracil injection.
2, the role is different
Capecitabine can be used as adjuvant chemotherapy for colon cancer, and as monotherapy for colon cancer patients who receive fluorouracil alone. 5-Fluorouracil can be used to treat digestive tract tumors, or to treat choriocarcinoma with a large dose of 5-Fluorouracil.
3. Different side effects
The side effects of capecitabine are relatively small, and symptoms such as rash and hair loss may occur. The side effects of 5-Fluorouracil injection are relatively large, which may lead to bone marrow suppression and gastrointestinal discomfort.
What should I pay attention to when using Capecitabine powder?
1. Avoid contact and obtain special instructions before use.
2. Do not inhale Capecitabine powder.
3. Wear appropriate protective clothing and gloves.
4. In case of accident or discomfort, seek medical attention immediately (if possible, show its label).
How and where to buy Capecitabine powder wholesale?
You can trust our order because we have a good record of selling legal educational drugs.
We conduct independent laboratory tests on all products and then sell them to our respected customers.
A variety of shipping methods for you to choose
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Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
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3-7 days |
DHL, Germany DHL, Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
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By Air |
Suitable for more than 50kg. |
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15-60 days |
By Sea |
Suitable for more than 500kg. |
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FAQ：
Q1: How does Capecitabine activate and exert its effect in vivo?
A: After entering the body, it undergoes three enzymatic transformations, ultimately producing the active metabolite of fluorouracil. This metabolite targets rapidly dividing and proliferating abnormal cells, interfering with the cellular nucleic acid synthesis process.
Q2: What is the core physiological pathway that interferes with cell proliferation?
A: The active product of Capecitabine embeds itself in the cellular DNA and RNA synthesis chains, hindering the normal replication and transcription of genetic material, thus blocking the continuous division and growth of abnormal cells.
Q3: What are the advantages of Capecitabine in vivo compared to direct use of fluorouracil?
A: The prodrug form of Capecitabine can preferentially complete metabolic activation in the lesion area, with less impact on normal healthy cells, resulting in more pronounced target selectivity in vivo.
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure, or prevent any disease.
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