JNJ 26854165 (JNJ26854165, Serdemetan),又称谢尔德梅坦,是一种可口服HDM2泛素连接酶拮抗剂,通过抑制HDM2-目的蛋白复合体与蛋白酶体的相互作用,抑制目的蛋白降解,具有抗肿瘤活性。JNJ 26854165可以诱导p53野生型细胞的早期凋亡。
参考文献
1.Kojima K, Burks JK, Arts J, Andreeff M.The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias.Mol Cancer Ther. 2010 Sep;9(9):2545-57.
2.T. Stühmer et al. A first-in-class HDM2-inhibitor (JNJ-26854165) in phase I development shows potent activity against multiple myeloma (MM) cells in vitro and ex vivo Journal of Clinical Oncology, 2008 ASCO Annual Meeting Proceedings (Post-Meeting Edition ).Vol 26, No 15S (May 20 Supplement), 2008: 14694.
3.Chargari C, et al.Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts.Cancer Lett. 2011 Dec 22;312(2):209-18.
4.Smith MA, et al. Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.Pediatr Blood Cancer. 2012 Aug;59(2):329-32.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。