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Merck
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SML2075

Sigma-Aldrich

Gimeracil

≥98% (HPLC)

别名:

5-Chloropyridine-2,4-diol, 5-chloro-4-hydroxypyridin-2(1H)-one, CDHP, Gimestat

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About This Item

经验公式（希尔记法）:
C5H4ClNO2
CAS号:
103766-25-2
分子量:
145.54
MDL號碼:
MFCD08458352
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to brown

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

InChI

1S/C5H4ClNO2/c6-3-2-7-5(9)1-4(3)8/h1-2H,(H2,7,8,9)

InChI 密鑰

ZPLQIPFOCGIIHV-UHFFFAOYSA-N

生化／生理作用

Gimeracil (5-chloro-2, 4-dihydroxypyridine) is an orally active inhibitor against dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine and the chemotherapeutic drug 5-fluorouracil (5FU). Gimeracil is shown to exhibit cancer-radiosensitizing efficacy in cultures in vitro (1 mM) and in mice in vivo (2.5-25 mg/kg, p.o.) in a DPYD-dependent manner via partial suppression of DNA repair by homologous recombination (HR).

象形圖

Exclamation mark
GHS07

訊號詞

Warning

危險聲明

H302

危險分類

Acute Tox. 4 Oral

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Keiji Koda et al.
Anticancer research, 36(10), 5325-5331 (2016-11-01)
It has not been elucidated whether the clinical efficacy of oral fluoropyrimidines for adjuvant chemotherapy of colorectal cancer varies with tumor biological characteristics. A multicenter randomized trial was performed comparing oral tegafur/gimeracil/oteracil (S-1) and uracil-tegafur/ leucovorin (UFT/LV) as adjuvant therapy
Masakazu Fukushima et al.
Oncology reports, 24(5), 1307-1313 (2010-09-30)
Chemoradiotherapy is a useful treatment strategy in patients with locally advanced cancers. In particular, combination of 5-fluorouracil (5-FU) with X-ray irradiation is effective for the treatment of some types of gastrointestinal cancers. We investigated the antitumor effects of combination treatment
T Wang et al.
Cancer radiotherapie : journal de la Societe francaise de radiotherapie oncologique, 20(3), 181-186 (2016-04-14)
This study evaluated the efficacy and safety of the combination drug tegafur, gimeracil, and oteracil potassium (S-1) concurrent with 3-dimensional conformal radiotherapy for newly diagnosed squamous cell carcinoma of the lung in elderly patients. Patients with pathologically or cytologically newly
Ryohei Nishiguchi et al.
BMJ case reports, 2016 (2016-12-10)
The most common histological classification of bile duct cancer is adenocarcinoma and squamous cell carcinoma (SCC) is relatively rare. We report a case of a 78-year-old man with SCC of the extrahepatic bile duct associated with metachronous para-aortic lymph node
Koh-Ichi Sakata et al.
Cancer science, 102(9), 1712-1716 (2011-06-15)
Gimeracil (5-chloro-2, 4-dihydroxypyridine) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood. Gimeracil was originally added to an oral fluoropyrimidine derivative S-1 to yield prolonged 5-fluorouracil concentrations in serum and tumor tissues. We have

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