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Gimeracil CAS: 103766-25-2

Category: Inhibitors
Product Name: Gimeracil
Cat No: I000224
CAS No: 103766-25-2
Synonyms: 5-chloro-4-hydroxy-1H-pyridin-2-one
Molecular Formula: C5H4ClNO2
Molecular Weight: 145.5
SMILES: ClC(C(O)=C1)=CN([H])C1=O
InChI: None
InChIKey: ZPLQIPFOCGIIHV-UHFFFAOYSA-N
Solubility: DMSO 29 mg/ml
Target: Dehydrogenase
Storage: powder
CAS 103766-25-2,Gimeracil
  • Description

Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.
IC50 Value:
Target: DPYD
in vitro: Gimeracil had radiosensitizing effects by partially inhibiting homologous recombination (HR) in the repair of DNA double strand breaks. Tail moments in neutral comet assay increased in gimeracil-treated cells. Gimeracil restrained the formation of foci of Rad51 and replication protein A (RPA), whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2. Gimeracil did not sensitize DPYD-depleted cells [1]. Gimeracil inhibited DNA DSB repair. It did not sensitize cells deficient in HR but sensitized those deficient in NHEJ. In SCneo assay, Gimeracil reduced the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1 [2].
in vivo:

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Tegafur/gimeracil/oteracil (TS-1)-induced erythroderma with an extensive mucosal involvement and hand-foot syndrome. Matsuda K, Namiki T, Ueno M, Hashimoto T, Hanafusa T, Yokozeki H.Eur J Dermatol. 2017 Apr 17. doi: 10.1684/ejd.2017.2999. [Epub ahead of print] No abstract available. PMID: 28414195
2:Acral lentiginosis associated with tegafur/gimeracil/oteracil (TS-1). Park YJ, Soh BW, Lee ES.Eur J Dermatol. 2017 Apr 1;27(2):209-210. doi: 10.1684/ejd.2016.2953. No abstract available. PMID: 28251899
3:Short-term clinical effect of conformal radiotherapy combined with tegafur gimeracil oteracil potassium in treating recurrent esophagus cancer. Jiao Y, Shen Y, Yan H, Liu Y, Tan H, Li J.Pak J Med Sci. 2016 Sep-Oct;32(5):1141-1145. PMID: 27882010 Free PMC Article
4:Gimeracil Exerts Radiosensitizing Effects on Oral Squamous Cell Carcinoma Cells In Vitro and In Vivo. Harada K, Ferdous T, Ueyama Y.Anticancer Res. 2016 Nov;36(11):5923-5930. PMID: 27793917
5:Efficacy and safety of S-1 (tegafur, gimeracil, and oteracil potassium) concurrent with 3-dimensional conformal radiotherapy for newly diagnosed squamous cell carcinoma of the lung in elderly patients. Wang T, Zhang SF, Qiu MQ, Li QL.Cancer Radiother. 2016 May;20(3):181-6. doi: 10.1016/j.canrad.2015.12.004. Epub 2016 Apr 7. PMID: 27068497
6:Comment on "Tegafur gimeracil oter combined with oxaliplatin for advanced colorectal cancer." Is it cost effectiveness? Berretta M, Di Francia R.Eur Rev Med Pharmacol Sci. 2016;20(1):5-6. No abstract available. PMID: 26813446 Free Article
7:[The Importance of Medication History Management by Hospital and Community Pharmacists for Oral Anticancer Drug S-1(Tegafur/Gimeracil/Oteracil Potassium)--A Retrospective Study]. Maeda M, Saito Y, Makino Y, Iwase H, Hayashi Y.Gan To Kagaku Ryoho. 2016 Jan;43(1):79-83. Japanese. PMID: 26809530
8:[Comparison of the efficacy and safety of capecitabine or tegafur, gimeracil and oteracil potassium capsules combined with oxaliplatin chemotherapy regimens in the treatment of advanced gastric cancer]. Wan Y, Hui H, Wang X, Wu J, Sun S.Zhonghua Zhong Liu Za Zhi. 2016 Jan;38(1):28-34. doi: 10.3760/cma.j.issn.0253-3766.2016.01.006. Chinese. PMID: 26796803
9:A clinical exploration of neoadjuvant chemotherapy with tegafur, gimeracil, and oteracil potassium capsules combined with oxaliplatin for advanced gastric cancer. Lv X, Zhang L, Huang R, Song W.Int J Clin Exp Med. 2015 Oct 15;8(10):19030-6. eCollection 2015. PMID: 26770529 Free PMC Article
10:Tegafur gimeracil oter combined with oxaliplatin for advanced colorectal cancer. Yang ZH, Ren J, Yi LJ, Zheng JH, Wei H.Eur Rev Med Pharmacol Sci. 2015 Sep;19(18):3391-6. PMID: 26439033 Free Article


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