AZD2461 is indeed a novel poly (ADP-ribose) polymerase (PARP) inhibitor that has been investigated for its potential to overcome resistance mechanisms associated with other PARP inhibitors, such as Olaparib. One of the key resistance mechanisms to Olaparib is mediated by P-glycoprotein (Pgp), an efflux pump that can reduce intracellular concentrations of the drug, thereby diminishing its efficacy.
Cat.No
DC1037
Name
AZD2461
Chemical Properties
CAS
1174043-16-3
Formula
C22H22FN3O3
MW
395.4268
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
[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.
[3]. Jaspers JE, et al. Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 2013 Jan;3(1):68-81.
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