AZD 2461

Name: AZD 2461
Brand: Tocris Bioscience
SKU: 6060

Tocris Bioscience, part of Bio-Techne | Catalog # 6060

Citations (3)

COA / SDS

Potent PARP inhibitor; orally bioavailable

Key Product Details

Description:	Potent PARP inhibitor; orally bioavailable
Chemical Name:	4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
Purity:	≥98% (HPLC)
Molecular Weight:	395.43

View Full Technical Details for AZD 2461

Technical Data
Citations

Biological Activity for AZD 2461

AZD 2461 is a potent PARP inhibitor (IC₅₀ values are 2, 5 and 200 nM for PARP2, PARP1 and PARP3, respectively). Exhibits anticancer effects in BRCA1 mutant, but not wild-type breast cancer cell lines in vitro. Inhibits growth of olaparib-resistant mammary tumors in a mouse model and is a poor substrate for the P-gp transporter. Orally bioavailable.

Compound Libraries for AZD 2461

AZD 2461 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for AZD 2461

M. Wt	395.43
Formula	C₂₂H₂₂FN₃O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1174043-16-3
PubChem ID	44199317
InChi Key	HYNBNUYQTQIHJK-UHFFFAOYSA-N
Smiles	COC1CCN(C(C2=C(C=CC(CC3=NNC(C4=CC=CC=C34)=O)=C2)F)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for AZD 2461

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	39.54	100
	ethanol	39.54	100

Preparing Stock Solutions for AZD 2461

The following data is based on the product molecular weight 395.43.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.53 mL	12.64 mL	25.29 mL
5 mM	0.51 mL	2.53 mL	5.06 mL
10 mM	0.25 mL	1.26 mL	2.53 mL
50 mM	0.05 mL	0.25 mL	0.51 mL

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References for AZD 2461

References are publications that support the biological activity of the product.

Jaspers Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 2013 PMID: 23103855
Oplustil O'Connor 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 PMID: 27550455