A PARP inhibitor
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AZD 2461

Item No. 16876

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[4-fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
CAS Number
1174043-16-3
Molecular Formula
C22H22FN3O3
Formula Weight
395.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mLDMSO: 2 mg/mLDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mLEthanol: 0.5 mg/mL
λmax
277 nm
SMILES
O=C1C2=CC=CC=C2C(CC3=CC(C(N4CCC(OC)CC4)=O)=C(F)C=C3)=NN1
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)
InChi Key
HYNBNUYQTQIHJK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $49

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    5 mg

    $202

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    10 mg

    $376

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    25 mg

    $702

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    Cayman Chemical
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    Product Description

    AZD 2461 is a PARP inhibitor (IC50 = 5 nM) with low affinity for the P-glycoprotein drug efflux transporter.1 It was developed to overcome the resistance encountered with olaparib (Item No. 10621) that is presumed to be mediated in part by P-glycoprotein-mediated drug efflux.1 When tested on the olaparib-resistant KB1P tumor T6-28, which has an 80-fold increased Mdr1b expression, AZD 2461 did not affect P-glycoprotein.1 Furthermore, it can induce a loss of p53 binding protein 1 expression in mice with KB1P tumors at 100 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jaspers, J.E., Kersbergen, A., Boon, U., et al. Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 3(1), 68-81 (2013).