Cat. No.: HY-B0016

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Capecitabine

29 Cited Publications

Customer Review

Based on 29 publication(s) in Google Scholar

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

For research use only. We do not sell to patients.

Purity: 99.99%
CAS No.: 154361-50-9
Formula: C₁₅H₂₂FN₃O₆
Molecular Weight:359.35

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Capecitabine Chemical Structure

CAS No.: 154361-50-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (29)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

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

IC₅₀ & Target

DNA/RNA Synthesis^[1]

All DNA/RNA Synthesis Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	34.2 μM Compound: Cape	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35300092]
HeLa	IC₅₀	0.05 mg/mL Compound: 4a, Capecitabine	Cytotoxicity against human HeLa cells after 3 days MTT assay Cytotoxicity against human HeLa cells after 3 days MTT assay	[PMID: 22796042]
KG-1	IC₅₀	8.9 μM Compound: Cape	Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35300092]
MCF7	IC₅₀	0.71 mg/mL Compound: 4a, Capecitabine	Cytotoxicity against human MCF7 cells after 3 days MTT assay Cytotoxicity against human MCF7 cells after 3 days MTT assay	[PMID: 22796042]
NCI-H69	IC₅₀	0.3 mg/mL Compound: 4a, Capecitabine	Cytotoxicity against human NCI-H69 cells after 3 days MTT assay Cytotoxicity against human NCI-H69 cells after 3 days MTT assay	[PMID: 22796042]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 154361-50-9
Appearance Solid
Molecular Weight 359.35
Formula C₁₅H₂₂FN₃O₆
Color White to off-white
SMILES

O[C@H]1[C@@H](O)[C@H](N2C=C(C(NC(OCCCCC)=O)=NC2=O)F)O[C@@H]1C
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (29)

All In Vivo Efficacy StudyHistological Imaging/StainingIHCWBCell Proliferation/Viability Assay

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Journal Impact Factor

Cancer Cell

Dissecting genetic and immune drivers of heterogeneous responses to neoadjuvant immunochemotherapy in gastric cancer. [Abstract]

2026 Apr 13;44(4):809-830.e11. PMID: 41720086
Cancer Cell

Chemotherapy triggers immune evasion by fostering LEPR+ Kupffer cell differentiation in liver metastases. [Abstract]

2026 Mar 9;44(3):658-675.e12. PMID: 41687606
ACS Nano

Single-Molecule-Based, Label-Free Monitoring of Molecular Glue Efficacies for Promoting Protein-Protein Interactions Using YaxAB Nanopores. [Abstract]

2024 Nov 12;18(45):31451-31465. PMID: 39482865
Adv Sci (Weinh)

Lactylation of HDAC1 Confers Resistance to Ferroptosis in Colorectal Cancer. [Abstract]

2025 Jan 31:e2408845. PMID: 39888307

Capecitabine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan 31:e2408845. [Abstract]

Dose-response curves of HCT116 to Capecitabine (0-100 μM; 24 h).
J Clin Invest

DNA topoisomerase II inhibition potentiates osimertinib's therapeutic efficacy in EGFR-mutant non-small cell lung cancer models. [Abstract]

2024 Mar 7;134(10):e172716. PMID: 38451729

Capecitabine purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Mar 7;134(10):e172716. [Abstract]

The given cell lines were treated with 250 nM osimertinib (Osim), 1.25 μM Etoposide (VP-16), 125 nM Doxorubicin (DXR), 5 nM Paclitaxel, 10 μM Cisplatin, 25 μM Carboplatin, 25 nM Gemcitabine, 20 nM 5-Fluorouracil (5-FU), 25 μM Cyclophosphamide, 25 μM Capecitabine, or 10 nM Vincristine alone or in combination for 3 days. Cell numbers were then measured using the SRB assay.
J Adv Res

Targeting PLA2G16, a lipid metabolism gene, by Ginsenoside Compound K to suppress the malignant progression of colorectal cancer. [Abstract]

2021 Jun 12:36:265-276. PMID: 35127176

Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276. [Abstract]

Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) inhibited the growth of xenograft tumors.

Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276. [Abstract]

H&E staining to detect tumor necrosis in mice models treated with Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) .

Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276. [Abstract]

IHC detected the expression of Ki-67 in tumor tissue of mice models treated with Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) .

Capecitabine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2021 Jun 12:36:265-276. [Abstract]

Ginsenoside Compound K (GCK) and Capecitabine (359 mg/kg; i.g.; 5 days/week for 3 weeks and stop for 1 week) decreased the protein expressions of N-cadherin, ZEB1, MMP-9, MMP-2 and Vimentin in vivo.
Biomaterials

Immune modulation of the liver metastatic colorectal cancer microenvironment via the oral CAPOX-mediated cGAS-STING pathway. [Abstract]

2024 Oct:310:122625. PMID: 38820768
Cancer Lett

Dihydroartemisinin inhibits the development of colorectal cancer by GSK-3β/TCF7/MMP9 pathway and synergies with capecitabine. [Abstract]

2024 Feb 1:582:216596. PMID: 38101610
Cancer Lett

IRE1α-targeting downregulates ABC transporters and overcomes drug resistance of colon cancer cells. [Abstract]

2020 Apr 28;476:67-74. PMID: 32061752
Cell Death Dis

NOD2 reduces the chemoresistance of melanoma by inhibiting the TYMS/PLK1 signaling axis. [Abstract]

2024 Oct 1;15(10):720. PMID: 39353904
Nano Lett

Nanopore Signatures of Nucleoside Drugs. [Abstract]

2023 Oct 25;23(20):9437-9444. PMID: 37818841
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Cell Death Discov

A novel SRSF3 inhibitor, SFI003, exerts anticancer activity against colorectal cancer by modulating the SRSF3/DHCR24/ROS axis. [Abstract]

2022 May 2;8(1):238. PMID: 35501301
J Med Chem

Fluorocyclopropyl-Containing Tacrine Derivatives as Potent and Selective Dual CDK2/CDK9 Inhibitors for the Treatment of Colorectal Cancer. [Abstract]

2025 Nov 27;68(22):24326-24357. PMID: 41239996
Cancer Cell Int

In vitro co-culture systems of hepatic and intestinal cells for cellular pharmacokinetic and pharmacodynamic studies of capecitabine against colorectal cancer. [Abstract]

2023 Jan 31;23(1):14. PMID: 36717845
Breast Cancer Res

Multi-receptor targeted therapy of breast cancer and brain metastases with a novel QUAD-drug conjugate. [Abstract]

2025 Oct 27;27(1):189. PMID: 41146202
Int J Cancer

Establishment of patient-derived organoids for guiding personalized therapies in breast cancer patients. [Abstract]

2024 Jul 15;155(2):324-338. PMID: 38533706
Int Immunopharmacol

Metronomic capecitabine with rapamycin exerts an immunosuppressive effect by inducing ferroptosis of CD4+ T cells after liver transplantation in rat. [Abstract]

2023 Aug 23;124(Pt A):110810. PMID: 37625370
ACS Omega

A LRELHLNNN-Gal‑3 Modified Adipose Decellularized Scaffold To Construct Colorectal Cancer Model for Anticancer Drug Screening and Immunotherapy. [Abstract]

2025 Oct 30;10(44):52931-52943. PMID: 41244442
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Biochem Eng J

2022: 108722.
Heliyon

HMGA2 promotes resistance against paclitaxel by targeting the p53 signaling pathway in colorectal cancer cells. [Abstract]

2024 May 20;10(11):e31431. PMID: 38845972
Front Oncol

Patient-Derived Xenograft Models for Intrahepatic Cholangiocarcinoma and Their Application in Guiding Personalized Medicine. [Abstract]

2021 Jul 13:11:704042. PMID: 34327143
In Vitro Model

Colorectal carcinoma organoid and cancer-associated fibroblasts co-culture system for drug evaluation. [Abstract]

2025 Mar 5;4(1):31-44. PMID: 40160212
Open Life Sci

Systemic investigation of inetetamab in combination with small molecules to treat HER2-overexpressing breast and gastric cancers. [Abstract]

2023 Jan 10;18(1):20220535. PMID: 36694697
In Vitro Cell Dev Biol Anim

Breast cancer organoids from malignant pleural effusion-derived tumor cells as an individualized medicine platform. [Abstract]

2021 May;57(5):510-518. PMID: 33950403
Journal of Nanostructures

2025.
Patent

US20230101335A1.
Research Square Preprint

2022 Feb.

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (695.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 12.5 mg/mL (34.79 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7828 mL

13.9140 mL

27.8280 mL

5 mM

0.5566 mL

2.7828 mL

5.5656 mL

10 mM

0.2783 mL

1.3914 mL

2.7828 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 20 mg/mL (55.66 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.7828 mL	13.9140 mL	27.8280 mL	69.5701 mL
	5 mM	0.5566 mL	2.7828 mL	5.5656 mL	13.9140 mL
	10 mM	0.2783 mL	1.3914 mL	2.7828 mL	6.9570 mL
	15 mM	0.1855 mL	0.9276 mL	1.8552 mL	4.6380 mL
	20 mM	0.1391 mL	0.6957 mL	1.3914 mL	3.4785 mL
	25 mM	0.1113 mL	0.5566 mL	1.1131 mL	2.7828 mL
	30 mM	0.0928 mL	0.4638 mL	0.9276 mL	2.3190 mL
DMSO	40 mM	0.0696 mL	0.3479 mL	0.6957 mL	1.7393 mL
	50 mM	0.0557 mL	0.2783 mL	0.5566 mL	1.3914 mL
	60 mM	0.0464 mL	0.2319 mL	0.4638 mL	1.1595 mL
	80 mM	0.0348 mL	0.1739 mL	0.3479 mL	0.8696 mL
	100 mM	0.0278 mL	0.1391 mL	0.2783 mL	0.6957 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Capecitabine

29 Cited Publications

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Capecitabine

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Publications Citing Use of MedChemExpress (MCE) Capecitabine

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Publications (29)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Capecitabine Related Classifications

Cat. No.: HY-B0016