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Gimeracil

Cat. No. M3960
Gimeracil Structure
Synonym:

Gimestat

Size Price Availability Quantity
10mM*1mL in DMSO USD 60  USD60 In stock
25mg USD 55  USD55 In stock
50mg USD 75  USD75 In stock
100mg USD 95  USD95 In stock
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Quality Control & Documentation
Biological Activity

Gimeracil (5-chloro-2, 4-dihydroxypyridine) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood.Gimeracil had radiosensitizing effects by partially inhibiting homologous recombination (HR) in the repair of DNA double strand breaks.The inhibitors of DPYD, such as gimeracil, could enhance the efficacy of radiotherapy through partial suppression of HR-mediated DNA repair.

Chemical Information
Molecular Weight 145.54
Formula C5H4ClNO2
CAS Number 103766-25-2
Solubility (25°C) DMSO 29mg/ml
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Wang HF, et al. Cell Biochem Biophys. The Clinical Evaluation of Tegafur Gimeracil Oteracil Combined with THP and DDP for Second-Line Treatment of Advanced Cardiac Carcinoma.

[2] Sakata K, et al. Cancer Sci. Gimeracil, an inhibitor of dihydropyrimidine dehydrogenase, inhibits the early step in homologous recombination.

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Keywords: Gimeracil, Gimestat supplier, inhibitors, activators


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