MK-4827 tosylate

• CAT Number: I000232
• CAS Number: 1038915-73-9
• Molecular Formula: C19H20N4O C7H8O3S
• Molecular Weight: 492.6
• Purity: ≥95%
• Target: PARP
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 3.8 nM/2.1 nM( PARP1/2) [1]
• IUPAC Name: 4-methylbenzenesulfonic acid;2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide
• 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: 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

MK-4827 tosylate (Cat.No:I000232) is a potent and selective inhibitor of poly(ADP-ribose) polymerase (PARP). It works by blocking the enzymatic activity of PARP, which plays a crucial role in DNA repair. MK-4827 tosylate has shown promise in preclinical and clinical studies as a potential anticancer agent, particularly in cancers with defects in DNA repair pathways.

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.