MK-4827 hydrochloride

• CAT Number: I000231
• CAS Number: 1038915-64-8
• Molecular Formula: C19H21ClN4O
• Molecular Weight: 356.85
• Purity: ≥95%
• Synonyms: 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;hydrochloride
• Target: PARP
• Solubility: 10 mM in DMSO
• Storage: Store at -20℃
• IC50: 3.8 nM/2.1 nM( PARP1/2) [1]
• InChI: InChI=1S/C19H20N4O.ClH/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);1H/t14-;/m1./s1
• InChIKey: YXYDNYFWAFBCAN-PFEQFJNWSA-N
• SMILES: C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N.Cl

MK-4827 hydrochloride（Cat No.:I000231）is a selective inhibitor of the enzyme poly(ADP-ribose) polymerase (PARP), primarily targeting PARP1 and PARP2. This compound is designed to enhance the efficacy of cancer therapies by exploiting the DNA repair deficiencies in tumors, particularly those with BRCA1 and BRCA2 mutations. By inhibiting PARP, MK-4827 disrupts the repair of single-strand DNA breaks, leading to the accumulation of DNA damage and ultimately inducing apoptosis in cancer cells. It has shown promise in clinical trials for various cancers, making it a potential therapeutic option in personalized cancer treatment strategies.

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.