Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease.
IC50&Target
DNA Alkylator
体外研究
Chlorambucil can deprive the function of complementary strands of DNA molecules via alkalization-induced cross interaction, and then inhibits tumor cell proliferation. Chlorambucil (0, 2.5, 5, 10 μM) exhibits slight inhibitory effect on Raji cell apoptosis, but potently increases DR4 and DR5 mRNA expression in Raji cells. Chlorambucil (10 μM) in combination with Tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL, 80 ng/ml) has synergistic effect on Raji cell apoptosis and inhibition on proliferation.
Chlorambucil is a DNA alkylator at high doses and, at lower doses, acts as an inhibitor of synthesis of nuclear proteins, particularly histones. Increasing doses are associated with a higher frequency of apoptosis, whereas long-term maintenance therapy has been associated with mutations of the p53 gene, leading to secondary malignancies.
体内研究
Chlorambucil (0.2 mg/kg, p.o.) in combination with levamisole (5 mg/kg) has enhanced anti-cancer effect on Ehrlich ascites carcinoma which elevates apoptosis of Ehrlich ascites carcinoma and the survival rate of the mice. However, Chlorambucil exhibits adverse effects on the liver and kidneys of mice.
分子式
C14H19Cl2NO2
分子量
304.21
CAS号
305-03-3
中文名称
苯丁酸氮芥;氯氨布布西;氯氨布西;瘤可宁;氯氨布西
运输条件
Room temperature in continental US; may vary elsewhere.