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MK-4827 tosylate CAS: 1038915-73-9

Category: Inhibitors
Product Name: MK-4827 tosylate
Cat No: I000232
CAS No: 1038915-73-9
Synonyms: (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carbimidic acid compound with 4-methylbenzenesulfonic acid (1:1)
Molecular Formula: C19H20N4O • C7H8O3S
Molecular Weight: 492.6
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
InChIKey: LCPFHXWLJMNKNC-PFEQFJNWSA-N
Solubility: 10 mM in DMSO
Target: PARP
IC50: 3.8 nM/2.1 nM( PARP1/2) [1]
Storage: Store at -20°C
CAS 1038915-73-9,MK-4827 tosylate
  • Description

MK-4827(Niraparib) tosylate 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].

  • Spec


Assay:≥98%
Appearance:A crystalline solid

  • References


[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.


price inquiry for CAS:1038915-73-9, Product:MK-4827 tosylate