MK-4827

• CAT Number: I000230
• CAS Number: 1038915-60-4
• Molecular Formula: C₁₉H₂₀N₄O
• Molecular Weight: 320.39
• Purity: ≥95%
• Target: PARP
• Solubility: DMSO: ≥ 34 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 3.8 nM/2.1 nM( PARP1/2) [1]
• IUPAC Name: 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide
• 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(Cat.No:I000230) is a potent and selective inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes. PARP enzymes are involved in DNA repair, and inhibition of these enzymes can lead to increased sensitivity to DNA-damaging agents, such as chemotherapy and radiation. MK-4827 has shown promise in the treatment of various types of cancer, including ovarian and breast cancer, and is currently undergoing clinical trials for these indications. It is administered orally and is generally well-tolerated, but may cause side effects such as fatigue, nausea, vomiting, and anemia.

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.