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Gimeracil (Synonyms: Gimestat)

Cat. No.: HY-17469 Purity: 99.98%
Handling Instructions

Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD).

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

Gimeracil Chemical Structure

Gimeracil Chemical Structure

CAS No. : 103766-25-2

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
25 mg USD 60 In-stock
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50 mg USD 84 In-stock
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100 mg USD 108 In-stock
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500 mg USD 144 In-stock
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Description

Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD)[1][2].

In Vitro

Gimeracil reduces the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1[1].
Gimeracil may enhance the efficacy of radiotherapy through the suppression of HR-mediated DNA repair pathways[1].
Gimeracil pretreatment significantly restrains the formation of radiation-induced foci of Rad51 and RPA, whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2[2].

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

Cell Viability Assay[1]

Cell Line: DLD-1, HeLa, and LC-11 cell lines.
Concentration: 1 mM.
Incubation Time: 48 h.
Result: Inhibits the repair of irradiation-induced DNA double strand breaks.
Did not increase the c-H2AX foci residual at 24 h in unirradiated cells.
In Vivo

Gimeracil (2.5-25 mg/kg, orally) may inhibit the rapid repair of X-ray-induced DNA damage in tumors[3].

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

Animal Model: Nude mice (Lu-99, LC-11, KB/C3 and PAN-4 tumors were xenografted)[3].
Dosage: 2.5-25 mg/kg.
Administration: Orally.
Result: Exhibited anti-tumor activity.
Clinical Trial
Molecular Weight

145.54

Formula

C₅H₄ClNO₂

CAS No.

103766-25-2

SMILES

O=C1C=C(O)C(Cl)=CN1

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 : 100 mg/mL (687.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.8710 mL 34.3548 mL 68.7096 mL
5 mM 1.3742 mL 6.8710 mL 13.7419 mL
10 mM 0.6871 mL 3.4355 mL 6.8710 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (17.18 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (17.18 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (17.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.98%

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

GimeracilGimestatOthersLu-99LC-11KB/C3PAN-4radiotherapyDNArepairInhibitorinhibitorinhibit

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Gimeracil
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