MK-4827

• CAT Number: I000230
• CAS Number: 1038915-60-4
• Molecular Formula: C₁₉H₂₀N₄O
• Molecular Weight: 320.39
• Purity: ≥95%
• Synonyms: 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide
• Target: Epigenetics
• Solubility: DMSO: ≥ 34 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 3.8 nM/2.1 nM( PARP1/2) [1]
• 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 (also known as Niraparib)（Cat No.:I000230）is a potent, selective inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair. By inhibiting PARP, MK-4827 induces synthetic lethality in cancer cells with deficiencies in homologous recombination repair mechanisms, such as those with BRCA1/2 mutations. This makes it particularly effective in treating ovarian, breast, and other cancers with such genetic vulnerabilities. MK-4827 has shown promise in both preclinical and clinical studies, making it a valuable tool in oncology research and a potential therapeutic option for targeted cancer treatment.

Reference

[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.