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Niraparib
- MK 4827
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C19H20N4O
- MW: 320.39
Description
Niraparib is a potent, selective and orally available PARP 1/2 inhibitor with IC50 values of 3.8 and 2.1 nM, respectively. Moreover, in a whole cell assay, Niraparib inhibited PARP activity with an EC50 value of 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 (CC50 value of 10−100 nM). Niraparib was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.
More Information
| Parent CAS No. | 1038915-60-4 |
|---|---|
| Chemical Name | (S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide |
| SMILES | C1(N2C=C3C=CC=C(C(N)=O)C3=N2)C=CC([C@H]2CNCCC2)=CC=1 |&1:16,r| |
| MFCD | N.A. |
| 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 |
| CID | 24958200 |
| Short Description | PARP inhibitor |
References
- P Jones 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.
- P Jones et al. Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination. J Med Chem. 2015 Apr 23;58(8):3302-14.
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