A PARP1 and PARP2 inhibitor
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KU-0058948

Item No. 42098

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[4-fluoro-3-[(hexahydro-1H-1,4-diazepin-1-yl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
CAS Number
763111-49-5
Molecular Formula
C21H21FN4O2
Formula Weight
380.4
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10mg/ml
SMILES
FC(C(C(N1CCNCCC1)=O)=C2)=CC=C2CC3=NNC(C4=C3C=CC=C4)=O
InChi Code
InChI=1S/C21H21FN4O2/c22-18-7-6-14(12-17(18)21(28)26-10-3-8-23-9-11-26)13-19-15-4-1-2-5-16(15)20(27)25-24-19/h1-2,4-7,12,23H,3,8-11,13H2,(H,25,27)
InChi Key
HGEPGGJUGUMFHT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $43

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    5 mg

    $194

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    10 mg

    $344

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    25 mg

    $752

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    Cayman Chemical
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    Product Description

    KU-0058948 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.4 and 1.5 nM, respectively).1 It is selective for PARP1 over PARP3, PARP4, and tankyrase (IC50s = 40, 1,200, and >10,000 nM, respectively). It also selectively inhibits the survival of mouse embryonic stem cells lacking Brca1 or Brca2 over mouse embryonic stem cells expressing wild-type Brca1 or Brca2. KU-0058948 (1 µM) induces apoptosis in P39 and MUTZ-3 acute myeloid leukemia (AML) cells.2 It decreases the survival of P39 and MUTZ-3 cells but not a variety of other AML and non-AML cells, including ME-1, U937, HL-60, and K562 cells. KU-0058948 (5 nM) potentiates cytotoxicity induced by MS-275 (Item No. 13284) in patient-derived AML cells. It reduces survival of HCT116 cells deficient in phosphatase and tensin homolog (PTEN) but not those expressing wild-type PTEN or containing a PTEN construct (HCT116+/neo).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Farmer, H., McCabe, N., Lord, C.J., et al. Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy. Nature 434(7035), 917-921 (2005).

    2. Gaymes, T.J., Shall, S., Macpherson, L.J., et al. Inhibitors of poly ADP-ribose polymerase (PARP) induce apoptosis of myeloid leukemic cells: Potential for therapy of myeloid leukemia and myelodysplastic syndromes. Haematologica 94(5), 638-646 (2009).

    3. Mendes-Pereira, A.M., Martin, S.A., Brough, R., et al. Synthetic lethal targeting of PTEN mutant cells with PARP inhibitors. EMBO Mol. Med. 1(6-7), 315-322 (2009).