MK-4827 [1038915-60-4]

Catalog number: HY-10619_10mM
Brand: MedChem Express
Packing: 10 mM
Other sizes: 5 mg
10 mg
50 mg
100 mg
Price: € 107.00
Expected delivery time: 10 days

Product specifications for - MK-4827 [1038915-60-4]

Product group: Chemicals
Category: Inhibitors / activators
CAS No.: 1038915-60-4
Purity: >98%
Molecular Formula: C19H20N4O
Molecular weight: 320.3883
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: MK-4827(Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2, >330-fold selective against PARP3, V-PARP and Tank1. IC50 value: 3.8 nM/2.1 nM( PARP1/2) [1] Target: PARP1/2 in vitro: MK-4827 displays excellent PARP 1 and 2 inhibition with IC(50) = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibits PARP activity with EC(50) = 4 nM and inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range [1]. in vivo: MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer [1]. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. The enhancement of radiation response is observed in clinically relevant radiation-dose fractionation schedules. The therapeutic window during which time MK-4827 interacts with radiation lasts for several hours. These biological attributes make translation of this therapeutic combination treatment feasible for translation to the treatment of a variety of human cancers [2].
Safety information: 
Additional information: 
Synonyms: HY-10619; Niraparib; MK 4827; MK4827
Dna2 inhibitors for cancer treatment ', Binghui Shen, . Patent. US 20170226063 A1. Read more
Iodinated benzimidazole PARP radiotracer for evaluating PARP1/2 expression in vitro and in vivo', RC Anderson. Nucl Med Biol. 2016 Dec;43(12):752-758. Read more
Synthetic lethality in malignant pleural mesothelioma with PARP1 inhibition', Srinivasan G. Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867. Read more