Gimestat,chlorodihydroxypyridine; CDHP;Gimeracil
| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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Gimeracil (chlorodihydroxypyridine; CDHP; Gimestat), a pyridine/pyridone analog and an approved anticancer drug, is a potent inhibitor of the dihydropyrimidine dehydrogenase (DPYD) enzyme with potential anti-neoplastic activity. It is used as an adjunct to or in combination with other anticancer therapeutics to increase the systemic concentrations and therapeutic effectiveness of other antineoplastic drugs. Gimeracil inhibits the early steps in homologous recombination for double strand breaks repair of DNA.
| ln Vitro |
The frequency of new positive clones is decreased by gemeracil. Moreover, it increases the sensitivity of S phase cells compared to G0/G1 phase cells [1]. Gimeracil inhibits HR-mediated DNA repair pathways, which may increase the effectiveness of radiation therapy [1]. While pretreatment with gigeracil increased the number of foci of Nbs1, Mre11, Rad50, and FancD2, it dramatically reduced the development of radiation-induced Rad51 and RPA foci [2].
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| ln Vivo |
Gimeracil (oral, 2.5–25 mg/kg) may prevent tumor DNA damage from X-rays from healing quickly [3].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: DLD-1, HeLa, and LC-11 cell lines. Tested Concentrations: 1 mM. Incubation Duration: 48 h. Experimental Results: Inhibits the repair of irradiation-induced DNA double strand breaks. Did not increase the c-H2AX foci residual at 24 h in unirradiated cells. |
| Animal Protocol |
Animal/Disease Models: Nude mice (Lu-99, LC-11, KB/C3 and PAN-4 tumors were xenografted)[3].
Doses: 2.5-25 mg/kg. Route of Administration: Orally. Experimental Results: demonstrated anti-tumor activity. |
| References |
[1]. Masaru Takagi, et al. Gimeracil sensitizes cells to radiation via inhibition of homologous recombination. Radiother Oncol. 2010 Aug;96(2):259-66.
[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. [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. |
| Molecular Formula |
C5H4CLNO2
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| Molecular Weight |
145.54
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| CAS # |
103766-25-2
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| Related CAS # |
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| SMILES |
ClC1=C([H])N([H])C(C([H])=C1O[H])=O
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| InChi Key |
ZPLQIPFOCGIIHV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H4ClNO2/c6-3-2-7-5(9)1-4(3)8/h1-2H,(H2,7,8,9)
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| Chemical Name |
5-chloro-2-hydroxypyridin-4(1H)-one
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (17.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (17.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (17.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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