Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor - COVID-19 inhibitor Carmofur

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Carmofur DNA/RNA Synthesis inhibitor

Cat.No.S1289

Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.
Carmofur DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 257.26

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 257.26 Formula

C11H16FN3O3

 Storage (From the date of receipt)
CAS No. 61422-45-5 Download SDF Storage of Stock Solutions

Synonyms HCFU Smiles CCCCCCNC(=O)N1C=C(C(=O)NC1=O)F

Solubility

In vitro
Batch:

DMSO : 51 mg/mL ( (198.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Acid ceramidase [1]
In vitro
Carmofur is one of the masked compounds of 5-FU, which was modified for more potent antineoplastic activity and less toxicity. It is converted in vivo into 5-FU directly or via intermetabolites, such as 1-(carboxypentylcarbamoyl)-5-fluorouracil and/or 1-(carboxypropylcarbomoyl)-5-fluorouraci. This compound and its metabolites gradually accumulate in the brain during continuous administration and are removed very slowly. It has potent neurotoxicity which can produce severe leucoencephalopathy resembling methotrexate leucoencephalopathy both clinically and on brain CT, together with a cerebellar syndrome similar to that following 5-FU neurotoxicity. [1]
In vivo
Carmofur or 5-FU together with Nicardipine, a Ca2+ antagonist, causes a higher level of the FU in tumor tissue and potentiation of an antitumor effect on human gastric cancer transplanted into nude mice. [2] This compound exerts almost the same growth-inhibitory effects on both tumors in therapeutic experiments using nude mice bearing parent or subcutaneously transplanted 5-FU-resistant DLD-1 cells. [3]
References

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