1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

AZD-2461 

Cat. No.: HY-13536 Purity: 98.12%
Handling Instructions

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

For research use only. We do not sell to patients.

AZD-2461 Chemical Structure

AZD-2461 Chemical Structure

CAS No. : 1174043-16-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 190 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 290 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

PARP2

2 nM (IC50)

PARP1

5 nM (IC50)

PARP3

200 nM (IC50)

In Vitro

AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively. AZD-2461 (500 nM) shows inhibitory activity against DNA single-strand break repair in human A459 cells. AZD-2461 cuases resistance and high P-gp expression levels in BRCA2-deficient mouse breast cancer line KB2P3.4[1]. AZD-2461 is cytotoxic to BT-20 cells (5-50 μM), increases the proportions of S- and G2-phase BT-20 cells (5-20 μM), and weakly affects the progression of cell cycle in SKBr-3 cells (5-20 μM)[2].

In Vivo

AZD-2461 (10 mg/kg, p.o.) enhances the antitumor activity of temozolomide in a mouse colorectal xenograft and exhibits low effect on mouse bone marrow cells. However, the increased bone marrow tolerability of AZD-2461 is not seen in rat models[1]. AZD-2461 (0.5% v/w HPMC, p.o.) increases the survival of mice bearing KB1P tumors after short-term treatment, and long-term treatment is well tolerated, but can not lead to tumor eradication[3].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.5289 mL 12.6445 mL 25.2889 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 mL
10 mM 0.2529 mL 1.2644 mL 2.5289 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

AZD-2461 is dissolved in DMSO.

BT-20 and SKBr-3 human primary breast cancer cell lines are used in the assay. SKBr-3 cells are cultivated in DMEM medium with 10% FCS and BT-20 in RPMI medium under an atmosphere containing 5% CO2. Twenty four hours after plating (at 60-70% confluence), the cells are treated with the PARP-1 inhibitors NU1025, AZD-2461, iniparib, olaparib, and rucaparib at concentrations ranging from 50 to 200 μM, 5 to 50 μM, 5 to 50 μM, 1 to 10 μM, and 0.3 to 10 μM, respectively, for durations indicated in figures 1-7[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

AZD-2461 is diluted in 0.5% w/v hydroxypropyl methylcellulose in deionized water to a concentration of 10 mg/mL.

Starting from 2 weeks after transplantation into mice, tumor size is monitored at least 3 times a week. All treatments are started when tumors reach a size of approximately 200 mm3. Olaparib (50 mg/kg intraperitoneally) and AZD-2461 (100 mg/kg per os) are given for 28 consecutive days, unless otherwise indicated. If tumors do not shrink below 50% of the initial volume, treatment is continued for another 28 days; otherwise, a new treatment cycle of 28 days is started when the relapsing tumor reaches a size of 100% of the original volume. AZD-2461 is diluted in 0.5% w/v hydroxypropyl methylcellulose in deionized water to a concentration of 10 mg/mL[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

395.43

Formula

C₂₂H₂₂FN₃O₃

CAS No.

1174043-16-3

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.12%

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AZD-2461
Cat. No.:
HY-13536
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