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AT-1420即甲基苯丙氨酸氮芥。实验表明对大鼠W-255有显著的抗瘤活性,用0.155～1mg/kg/d×7,有 81～100％抑瘤率,用0.25～1mg/kg/d×7,有50～100％肿瘤消散率,疗效与消瘤芥相似。 对小鼠S-180,肝癌、网细胞肉瘤(L_2)均有明显的抗瘤作用,用0.6～0.8mg/kg/d×7～8腹腔给药,抑瘤率分别为48～52％,28％、41～50％,对艾氏腹水癌(EAC)生命延长率为177％。作为比较,消瘤芥用量为2.5～3.5mg/kg/d,对S-37抑制率为64％。AT-1420对EAC和W-256疗效较好,但对S-37无效,其他肿瘤和消瘤芥的疗效相似。另口服和注射给药均有效。 AT-1420对~3H-TdR参入EAC细胞中有明显的抑制作用,抑制率为70％(±8.1)。 测得大鼠腹腔注射一次的LD50为5.4mg/kg,7次给药的LD50为1.25mg/kg/次。测得小鼠腹腔注射一次的LD50为8mg/kg,而7次给药的LD50为1.13mg/kg/次。 上述表明AT-1420有明显的抗动物肿瘤作用,抗瘤谱广,口服和注射给药有效。疗效与消瘤介相似,且用量较小,故AT-1420值得进一步研究,考虑提供临床试用。
AT-1420 is methyl-phenylalanine mustard. Experiments show that there is a significant antitumor activity against rat W-255, 0.155-1 mg/kg/d×7, 81-100% inhibition rate, 0.25-1 mg/kg/d×7, 50-100 % tumor dissipation rate, similar efficacy and elimination of tumor mustard. For mice S-180, hepatocellular carcinoma and reticulocyte sarcoma (L 2 ), there was obvious anti-tumor effect, and they were intraperitoneally administered with 0.6-0.8 mg/kg/d×7-8. The tumor inhibition rate was 48-52% respectively. 28%, 41 ~ 50%, Ehrlich ascites carcinoma (EAC) life extension rate was 177%. As a comparison, the amount of tumor mustard was 2.5-3.5 mg/kg/d, and the inhibition rate for S-37 was 64%. AT-1420 had a good effect on EAC and W-256, but it had no effect on S-37. The efficacy of other tumors and tumor elimination was similar. The other oral and injection are effective. AT-1420 had significant inhibitory effect on ~3H-TdR incorporation into EAC cells with an inhibition rate of 70% (±8.1). The LD50 was determined to be 5.4 mg/kg once for intraperitoneal injection in rats and 1.25 mg/kg/time for 7 doses. The LD50 of the mouse once intraperitoneally injected was measured as 8 mg/kg, and the LD50 of the seven administrations was 1.13 mg/kg/time. The above shows that AT-1420 has a significant anti-tumor effect on animals, has a broad anti-tumor spectrum, and is effective for oral and injection administration. The efficacy is similar to that of elimination of tumors, and the dosage is small. Therefore, AT-1420 is worthy of further study. Consider providing clinical trials.