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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
PARP1; PARP2; PARP3
Available Sizes
Frequently Asked Questions
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