A PARP1 inhibitor
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Fluzoparib

Item No. 36671

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[3-[[5,6-dihydro-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
CAS Number
1358715-18-0
Molecular Formula
C22H16F4N6O2
Formula Weight
472.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=C1NN=C(CC2=CC=C(C(C(N3CC4=NC(C(F)(F)F)=NN4CC3)=O)=C2)F)C5=C1C=CC=C5
InChi Code
InChI=1S/C22H16F4N6O2/c23-16-6-5-12(10-17-13-3-1-2-4-14(13)19(33)29-28-17)9-15(16)20(34)31-7-8-32-18(11-31)27-21(30-32)22(24,25)26/h1-6,9H,7-8,10-11H2,(H,29,33)
InChi Key
XJGXCBHXFWBOTN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $219

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    10 mg

    $372

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    25 mg

    $712

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    50 mg

    $986

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    Cayman Chemical
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    Product Description

    Fluzoparib is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; IC50 = 1.46 nM).1 It induces DNA double-strand breaks in wild-type, but not BRCA2-/-, V-C8 cells, as well as BRCA1-/- MDA-MB-436 cells when used at concentrations of 1 and 10 µM. Fluzoparib inhibits the proliferation of BRCA2-/- V-C8 cells (IC50 = 0.053 µM), BRCA1-/- MDA-MB-436, UWB1.289, and MX-1 cells (IC50s = 0.51, 1.57, and 1.57 µM, respectively), and OVCAR-8 cells containing hypermethylated BRCA1 (IC50 = 1.43 µM). In vivo, fluzoparib (1 and 3 mg/kg) reduces tumor formation in an MDA-MB-436 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, L., Yang, C., Xie, C., et al. Pharmacologic characterization of fluzoparib, a novel poly(ADP-ribose) polymerase inhibitor undergoing clinical trials. Cancer Sci. 110(3), 1064-1075 (2019).