Carmofur是 5-氟尿嘧啶的衍生物,是一种抗肿瘤药物。它是一种酸性神经酰胺酶抑制剂,用于治疗乳腺癌和结直肠癌。它抑制 SARS-CoV-2主要蛋白酶,还抑制 Vero E6 细胞 SARS-CoV-2,EC50为 24.3 μM。
产品描述
Carmofur is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. Carmofur has been known to induce leukoencephalopathy.
体外活性
Carmofur is one of the masked compounds of 5-FU, which was modified for more potent antineoplastic activity and less toxicity. Carmofur is converted in vivo into 5-FU directly or via intermetabolites, such as 1-(carboxypentylcarbamoyl)-5-fluorouracil and/or 1-(carboxypropylcarbomoyl)-5-fluorouraci. Carmofur and its metabolites gradually accumulate in the brain during continuous administration and are removed very slowly. Carmofur has potent neurotoxicity which can produce severe leucoencephalopathy resembling methotrexate leucoencephalopathy both clinically and on brain CT, together with a cerebellar syndrome similar to that following 5-FU neurotoxicity. [1]
Cas No.
61422-45-5
分子式
C11H16FN3O3
分子量
257.265
别名
HCFU;卡莫氟
储存和溶解度
H2O:<1 mgml
DMSO:49 mg/mL (190.5 mM)
Ethanol:10 mg/mL (38.87 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years