Niraparib-d5

Niraparib-d5 (MK-4827-d5) is the deuterium labeled Niraparib. Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

MK-4827-d5

12352005

Apoptosis; Isotope-Labeled Compounds; PARP

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Others

Cancer

O=C(N)C1=CC=CC2=C(N(N=C12)C3=CC=C(C=C3)[C@H]4C([2H])(NC([2H])(CC4)[2H])[2H])[2H]

C19H15D5N4O

325.42

[1]Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375 (22) :2154-2164.|[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.|[3]Bridges KA, et al. Niraparib (MK-4827), a novel poly (ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5 (13) :5076-86.|[4]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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-W759435/

Isotope-Labeled Compounds

No Development Reported