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[CAS NO. 154361-50-9]  Capecitabine

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PRODUCTS SPECIFICATIONS [154361-50-9]

Catalog
HY-B0016
Brand
MCE
CAS
154361-50-9

DESCRIPTION [154361-50-9]

Overview

MDLMFCD00930626
Molecular Weight359.35
Molecular FormulaC15H22FN3O6
SMILESO[C@H]1[C@@H](O)[C@H](N2C=C(C(NC(OCCCCC)=O)=NC2=O)F)O[C@@H]1C

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

11 Publications Citing Use of MCE


Summary

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


IC50 & Target

DNA/RNA Synthesis [1]


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 IC 50 values vary from 860 μM in COLO205 cells to 6000 μM in HCT8 cells [2] .

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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT03428529 Instituto Nacional de Cancer, Brazil
Rectal Neoplasm Malignant
January 12, 2011 Phase 2|Phase 3
NCT00496704 Yonsei University|National Cancer Institute (NCI)
Colorectal Cancer
January 2007 Phase 1|Phase 2
NCT02560974 Hoffmann-La Roche
Gastric Cancer
June 2006 Phase 3

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

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

Solvent & Solubility

In Vitro:

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

H 2 O : ≥ 33.33 mg/mL ( 92.75 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

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

  • 2.

    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

  • 3.

    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

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.


Synonyms

Cytidine, 5′-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-
Carbamic acid, [1-(5-deoxy-β-D-ribofuranosyl)-5-fluoro-1,2-dihydro-2-oxo-4-pyrimidinyl]-, pentyl ester
5′-Deoxy-5-fluoro-N-[(pentyloxy)carbonyl]cytidine
Ro 09-1978/000
Capecitabine
Ro 09-1978
5′-Deoxy-5-fluoro-N4-(pentyloxycarbonyl)cytidine
Xeloda
Capecitibine
Capecytabine
Capiibine
Captabin
N4-Pentyloxycarbonyl-5′-deoxy-5-fluorocytidine
Capacetrine
Ecansya
Capecitabine Medac
Capecitabine Accord
Capecitabine Teva
Capecitabine SUN
Xeltabin

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