MK-4827

CAS No. 1038915-60-4

MK-4827( Niraparib | MK 4827 | MK4827 )

Catalog No. M10194 CAS No. 1038915-60-4

MK-4827 (Niraparib, MK4827) is a highly potent PARP inhibitor with IC50 of 3.8 nM/2.1 nM for PARP1/PARP2.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    MK-4827
  • Note
    Research use only, not for human use.
  • Brief Description
    MK-4827 (Niraparib, MK4827) is a highly potent PARP inhibitor with IC50 of 3.8 nM/2.1 nM for PARP1/PARP2.
  • Description
    MK-4827 (Niraparib, MK4827) is a highly potent PARP inhibitor with IC50 of 3.8 nM/2.1 nM for PARP1/PARP2; inhibits PARP activity with EC50=4 nM in a whole cell assay, and inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10?100 nM range; well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.Ovarian Cancer Approved(In Vitro):Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.(In Vivo):Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily.
  • In Vitro
    Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.
  • In Vivo
    Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily. Animal Model:Female nude mice (Ncr Nu/Nu) with solitary tumor xenografts Dosage:25 mg/kg or 50 mg/kg Administration:Gavage, 25 mg/kg twice a day with 6 h between doses or 50 mg/kg once daily for 21 consecutive days Result:Enhanced radiation response.
  • Synonyms
    Niraparib | MK 4827 | MK4827
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP1|PARP2|PARP3|TANK-1|V-PARP
  • Research Area
    Cancer
  • Indication
    Ovarian Cancer

Chemical Information

  • CAS Number
    1038915-60-4
  • Formula Weight
    320.3883
  • Molecular Formula
    C19H20N4O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 32 mg/mL
  • SMILES
    C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
  • Chemical Name
    2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Jones P, et al. J Med Chem. 2009 Nov 26;52(22):7170-85. 2. Bridges KA, et al. Oncotarget. 2014 Jul 15;5(13):5076-86. 3. Mirza MR, et al. N Engl J Med. 2016 Dec 1;375(22):2154-2164.
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