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    InvivoChem Cat #: V0310
    CAS #: 1174043-16-3Purity ≥98%

    Description: AZD-2461 is a novel, selective and potent inhibitor of Poly (ADP-ribose) polymerase (PARP) with potential anticancer activity. In inhibits PARP1/2/3 with IC50 values of 5 nM, 2 nM and 200 nM, respectively. It is a poor substrate of P-glycoprotein and was developed as a 2nd-generation compound of olaparib.

    References:  2016 Oct 15;76(20):6084-6094; Br J Pharmacol. 2009 Jul;157(5):854-62.

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    Molecular Weight (MW)395.43
    CAS No.1174043-16-3 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mM
    Water: <1 mg/mL
    Ethanol: <1 mg/mL

    AZD 2461; AZD-2461; AZD2461; 4-(4-fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one


    InChi Code: InChI=1S/C22H22FN3O3/c1-29-15-8-10-26(11-9-15)22(28)18-12-14(6-7-19(18)23)13-20-16-4-2-3-5-17(16)21(27)25-24-20/h2-7,12,15H,8-11,13H2,1H3,(H,25,27)

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

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    In Vitro

    In vitro activity: AZD-2461 is a novel and 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. 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).

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

    Cell Assay: 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

    In VivoAZD-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. 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.
    Animal modelMice
    Formulation & DosageDissolved in 0.5% w/v hydroxypropyl methylcellulose in deionized water to a concentration of 10 mg/mL; 100 mg/kg per os
    References 2016 Oct 15;76(20):6084-6094;  2013 Jan;3(1):68-81. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.


    AZD2461 has comparable effects on DNA single-strand break repair and efficacy as olaparib in vitro.


    AZD2461 inhibits PARP3 to a lesser extent than olaparib, resulting in a lack of inhibition of nonhomologous end-joining repair in cancer cells. Cancer Res. 2016 Oct 15;76(20):6084-6094. Epub 2016 Aug 22.



    AZD2461 overcomes P-gp–associated resistance to olaparib. Cancer Res. 2016 Oct 15;76(20):6084-6094. Epub 2016 Aug 22.



    PARP3 levels are significantly higher in mouse but not rat or human bone marrow cells and, consistent with this, is a lack of differential bone marrow toxicity between AZD2461 and olaparib in rats. Cancer Res. 2016 Oct 15;76(20):6084-6094. Epub 2016 Aug 22.


    AZD2461 is as effective as olaparib in potentiating the antitumor efficacy of temozolomide and shows lower impact on mouse bone marrow cells. Cancer Res. 2016 Oct 15;76(20):6084-6094. Epub 2016 Aug 22.



    Comparison between the catalytic domains of PARP1 and PARP3. Sequence alignment of a portion of the catalytic domains of PARPs 1–3. Residues forming the “HYE triad” within the catalytic core (green arrows) and a PARP3-specific deletion (gray box) are shown. Cancer Res. 2016 Oct 15;76(20):6084-6094. Epub 2016 Aug 22.


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