Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.
Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.
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DOI：
10.1002/pbc.23319
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发表时间：
2012-08
影响因子：
3.2
通讯作者：
Houghton PJ
中科院分区：
文献类型：
--
作者：
Smith MA;Gorlick R;Kolb EA;Lock R;Carol H;Maris JM;Keir ST;Morton CL;Reynolds CP;Kang MH;Arts J;Bashir T;Janicot M;Kurmasheva RT;Houghton PJ
JNJ-26854165最初是作为一种P53激活剂而开发的，能够诱导癌细胞株的凋亡。在体外，JNJ-26854165具有细胞毒活性。ALL细胞组的IC50中位数(0.85微米)显著低于其余细胞系。在体内，JNJ-26854165在37个实体肿瘤中的18个和可评估的7个异种移植中的5个中，EFS的分布与对照组相比有显着差异。目的37例实体瘤移植瘤中有4例有反应，7例全部移植瘤中有2例完全缓解或完全缓解。在带有突变型和野生型P53的异种移植中都观察到了反应。
JNJ-26854165 was originally developed as an activator of p53 capable of inducing apoptosis in cancer cell lines. In vitro, JNJ-26854165 demonstrated cytotoxic activity. The ALL cell line panel had a significantly lower median IC50 (0.85 µM) than the remaining cell lines. In vivo JNJ-26854165 induced significant differences in EFS distribution compared to control in 18 of 37 solid tumors and in 5 of 7 of the evaluable ALL xenografts. Objective responses were observed in 4 of 37 solid tumor xenografts, and 2 of 7 ALL xenografts achieved PR or CR. Responses were noted in xenografts with both mutant and wild-type p53.