STUDIES ON ANTITUMOR DRUGS Ⅵ.EXPERIMENTAL THERAPY AND TOXICITY OF p-BIS (2-CHLOROETHYL)AMINO-O-METHOXYL PHENYLALANINE(3P)

synthesized in our Institute,is a new derivative of sarcolysin.In this work we have investigated the therapeutic effect and toxicity of the drug in animals.The results obtained were as follows: 1.Intraperitoneal injection of 3P at the dosage of 5 mg/kg produced a marked inhibitory effect on sarcoma 180,but no effect on spindle cell sarcoma.When the dosage was raised to 10 mg/kg,the drug significantly inhibited the growth of spindle cell sarcoma (both the solid and ascitic forms),Ehrlich ascites carcinoma in mice and Guerin carcinoma,Walker carcinoma and Yoshida sarcoma in rats.Daily doses of 10 mg/kg introduced into the stomach of mice had also therapeutic action on sarcoma 180.At the above-mentioned dosages the drug lacked antitumor activity on AK sarcoma,solid forms of Ehrlich carcinoma and lymphatic leukemia. 2.In mice,the acute and subacute LD₅₀ after intraperitoneal injections of 3P were found to be 39 and 14 mg/kg respectively. 3.In rabbits,intravenous injections of 3P at the daily dosage of 1 mg/kg for 10 days could slightly decrease the white cell counts,but R.B.C.,Hb,EKG,body weight and urinalysis re- mained normal. 4.Two monkeys were given 3P by stomach tube at the dosages of 25(2.7 mg/kg)and 50 mg(5.3 mg/kg)every four days,and the total doses reached 300 and 850 mg,no signi- ficant alterations of blood cell counts,respiration,blood pressure,EKG,body weight,urine and stool routine examinations were observed.