MK-4827


CAS No. : 1038915-60-4

MK-4827,1038915-60-4
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000230
Synonyms:2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide
Molecular Formula:C₁₉H₂₀N₄O
Molecular Weight:320.39
Target:PARP
IC50:3.8 nM/2.1 nM( PARP1/2) [1]
Price:Get quote
We would like to match the lowest price on market if possible.

Your information is safe with us.

refresh
Cat No:I000230
Cas No:1038915-60-4
Product-Name:MK-4827
InChI:InChI=1S/C19H20N4O/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/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1
InChIKey:PCHKPVIQAHNQLW-CQSZACIVSA-N
SMILES:C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N

MK-4827(Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.
IC50 value: 3.8 nM/2.1 nM( PARP1/2) [1]
Target: PARP1/2
in vitro: MK-4827 displays excellent PARP 1 and 2 inhibition with IC(50) = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibits PARP activity with EC(50) = 4 nM and inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range [1].
in vivo: MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer [1]. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. The enhancement of radiation response is observed in clinically relevant radiation-dose fractionation schedules. The therapeutic window during which time MK-4827 interacts with radiation lasts for several hours. These biological attributes make translation of this therapeutic combination treatment feasible for translation to the treatment of a variety of human cancers [2].


[1]. Jones P, 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. 2009 Nov 26;52(22):7170-85.
[2]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

Related Products
  • CAS No. :934162-61-5
    Product Name:

    A-966492

    Cat No: I005541 View details
  • CAS No. :459868-92-9
    Product Name:

    AG-014699 phosphate

    Cat No: I003606 View details
  • CAS No. :912444-00-9
    Product Name:

    Veliparib

    Cat No: I005438 View details
  • CAS No. :1038915-75-1
    Product Name:

    MK-4827 Racemate

    Cat No: I011725 View details