AZD-2461

AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.

Product Specifications

CAS Number

[1174043-16-3]

UNSPSC

12352005

Hazard Statement

H302

Target

PARP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/azd-2461.html

Purity

99.79

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C1NN=C(CC2=CC=C(F)C(C(N3CCC(OC)CC3)=O)=C2)C4=C1C=CC=C4

Molecular Formula

C22H22FN3O3

Molecular Weight

395.43

Precautions

H302

References & Citations

[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.