An orally bioavailable PARP1/2 inhibitor
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MK-4827 (tosylate)

Item No. 20842

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-(3S)-3-piperidinylphenyl]-2H-indazole-7-carboxamide, 4-methylbenzenesulfonate
CAS Number
1038915-73-9
Synonyms
  • Niraparib tosylate
Molecular Formula
C19H20N4O • C7H8O3S
Formula Weight
492.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/mlEthanol: 1 mg/ml
λmax
223, 239, 311 nm
SMILES
NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C21)=O.CC5=CC=C(S(O)(=O)=O)C=C5
InChi Code
InChI=1S/C19H20N4O.C7H8O3S/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14;1-6-2-4-7(5-3-6)11(8,9)10/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);2-5H,1H3,(H,8,9,10)/t14-;/m1./s1
InChi Key
LCPFHXWLJMNKNC-PFEQFJNWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $51

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    10 mg

    $92

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    25 mg

    $164

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    50 mg

    $279

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    Cayman Chemical
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    Product Description

    MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively).1 It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro (IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice.1,2 MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.3 Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jones, P., Altmura, S., Boueres, J., et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J. Med. Chem. 52(22), 7170-7185 (2009).

    2. Yuan, Y., Liao, Y.M., Hsueh, C.T., et al. Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARP. J. Hematol. Oncol. 4(16), 1-14 (2011).

    3. Wang, L., Mason, K.A., Ang, K.K., et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs 30(6), 2113-2120 (2012).

    4. Mirza, M.R., Monk, B.J., Herrstedt, J., et al. Niraparib maintenance therapy in platinum-sensitive, recurrent ovarian cancer. N. Engl. J. Med. 375(22), 2154-2164 (2016).