AZD 2461

Pricing Availability   Qty
Cat.No. 6060 - AZD 2461 | C22H22FN3O3 | CAS No. 1174043-16-3
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 395.43. Batch specific molecular weights may vary from batch to batch due to solvent 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References

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

Oplustil O'Connor et al (2016) 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. 76 6084 PMID: 27550455

Jaspers et al (2013) Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 3 68 PMID: 23103855


If you know of a relevant reference for AZD 2461, please let us know.

View Related Products by Product Action

View all Poly(ADP-Ribose) Polymerase Inhibitors

Keywords: AZD 2461, AZD 2461 supplier, AZD2461, potent, PARP, inhibitors, inhibits, poly, (ADP-ribose), polymerases, orally, bioavailable, chemotherapeutics, Poly(ADP-ribose), Polymerase, 6060, Tocris Bioscience

Citations for AZD 2461

Citations are publications that use Tocris products.

Currently there are no citations for AZD 2461. Do you know of a great paper that uses AZD 2461 from Tocris? Please let us know.

Reviews for AZD 2461

There are currently no reviews for this product. Be the first to review AZD 2461 and earn rewards!

Have you used AZD 2461?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.