MK-4827 tosylate

• CAT Number: I000232
• CAS Number: 1038915-73-9
• Molecular Formula: C19H20N4O C7H8O3S
• Molecular Weight: 492.60
• Purity: ≥95%
• Synonyms: MK-4827 tosylate; (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carbimidic acid compound with 4-methylbenzenesulfonic acid (1:1)
• Target: PARP
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 3.8 nM/2.1 nM( PARP1/2)
• IUPAC Name: 4-methylbenzenesulfonic acid;2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide
• InChI: InChI=1S/C19H20N4O.C7H8O3S/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;1-6-2-4-7(5-3-6)11(8,9)10/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);2-5H,1H3,(H,8,9,10)/t14-;/m1./s1
• InChIKey: LCPFHXWLJMNKNC-PFEQFJNWSA-N
• SMILES: CC1=CC=C(C=C1)S(=O)(=O)O.C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N

MK-4827 tosylate（Cat No.:I000232）is a potent 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 DNA repair deficiencies, such as those with BRCA1 or BRCA2 mutations, leading to cell death. This compound is under investigation for its potential in treating various cancers, including ovarian, breast, and prostate cancers. MK-4827 tosylate is an essential tool in oncology research, offering promise in enhancing the efficacy of DNA-damaging chemotherapies and radiation treatments.

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.