Gimeracil (Synonyms: Gimestat)

Name: Gimeracil
Brand: MedChemExpress
SKU: HY-17469
Rating: 5.0 (2 reviews)

Cat. No.: HY-17469 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 103766-25-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
25 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
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5 g		Get quote

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Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Gimeracil

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Biological Activity
Purity & Documentation
References
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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].

MedChemExpress (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].

MedChemExpress (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

Appearance

Solid

Color

White to light brown

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (687.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (17.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.72%

Select Batch:

Data Sheet (277 KB) SDS (392 KB)

COA (250 KB) LCMS (460 KB)

Handling Instructions (2659 KB)

References

[1]. Masaru Takagi, et al. Gimeracil sensitizes cells to radiation via inhibition of homologous recombination. Radiother Oncol. 2010 Aug;96(2):259-66. [Content Brief]

[2]. Koh-Ichi Sakata, et al. Gimeracil, an inhibitor of dihydropyrimidine dehydrogenase, inhibits the early step in homologous recombination. Cancer Sci. 2011 Sep;102(9):1712-6. [Content Brief]

[3]. Masakazu Fukushima, et al. Gimeracil, a component of S-1, may enhance the antitumor activity of X-ray irradiation in human cancer xenograft models in vivo. Oncol Rep. 2010 Nov;24(5):1307-13. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	6.8710 mL	34.3548 mL	68.7096 mL	171.7741 mL
	5 mM	1.3742 mL	6.8710 mL	13.7419 mL	34.3548 mL
	10 mM	0.6871 mL	3.4355 mL	6.8710 mL	17.1774 mL
	15 mM	0.4581 mL	2.2903 mL	4.5806 mL	11.4516 mL
	20 mM	0.3435 mL	1.7177 mL	3.4355 mL	8.5887 mL
	25 mM	0.2748 mL	1.3742 mL	2.7484 mL	6.8710 mL
	30 mM	0.2290 mL	1.1452 mL	2.2903 mL	5.7258 mL
	40 mM	0.1718 mL	0.8589 mL	1.7177 mL	4.2944 mL
	50 mM	0.1374 mL	0.6871 mL	1.3742 mL	3.4355 mL
	60 mM	0.1145 mL	0.5726 mL	1.1452 mL	2.8629 mL
	80 mM	0.0859 mL	0.4294 mL	0.8589 mL	2.1472 mL
	100 mM	0.0687 mL	0.3435 mL	0.6871 mL	1.7177 mL

Gimeracil Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gimeracil103766-25-2GimestatOthersLu-99LC-11KB/C3PAN-4radiotherapyDNArepairInhibitorinhibitorinhibit

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Gimeracil (Synonyms: Gimestat)

Customer Review

Gimeracil Related Antibodies

2 Publications Citing Use of MCE Gimeracil

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Gimeracil Related Antibodies

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Complete Stock Solution Preparation Table

Gimeracil Related Classifications

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