0576-88813233
产品描述:
AZD2461是一种新型PARP抑制剂,作用于Pgp比Olaparib亲和力低。Phase 1。
靶点:
PARP
体外研究:
AZD2461作用于Pgp比Olaparib亲和力低。
体内研究:
AZD2461作用于抗Olaparib的KB1P肿瘤T6-28,提高Mdr1b表达80倍,不抑制Pgp。AZD2461短期处理携带KB1P肿瘤的小鼠,诱导53BP1表达损失。AZD2461长期处理,具有良好的耐受性,平均无复发生存期延长一倍。
[1]. Oplustil O'Connor L, et al. The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models. Cancer Res. 2016 Oct 15;76(20):6084-6094. Epub 2016 Aug 22.
[2]. Węsierska-Gądek J, et al. Differential Potential of Pharmacological PARP Inhibitors for Inhibiting Cell Proliferation and Inducing Apoptosis in Human Breast Cancer Cells. J Cell Biochem. 2015 Dec;116(12):2824-39.
版权所有 Copyright(C) 2018-2022 台州市科瑞生物技术有限公司