AZD-2461 (AZD2461)是PARP抑制剂,作用于PARP1/2的IC50值约为5 nM和2 nM,是转运蛋白P-糖蛋白的不良底物,可用于研究奥拉帕尼耐药的肿瘤,具有抗肿瘤活性。
参考文献
[1] Jaspers JE, Kersbergen A, Boon U, et al. Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 2013 Jan;3(1):68-81. doi: 10.1158/2159-8290.CD-12-0049(IF:26.37).
[2] Węsierska-Gądek J, Mauritz M, Mitulovic G, 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. doi: 10.1002/jcb.25229(IF:3.448).
[3] Oplustil O'Connor L, Rulten SL, Cranston AN, 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. doi: 10.1158/0008-5472.CAN-15-3240(IF:8.378).
-25~-15℃保存,有效期3年。