MK-4827 hydrochloride
Data Sheet
For research use only. Not for human use.
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| CAS No. | 1038915-64-8 | Cat. No. | BCP18442 |
| Name | MK-4827 hydrochloride | ||
| Synonyms | MK 4827 hydrochloride;MK4827 hydrochloride; | ||
| SMILES | |||
| Chemical Name | |||
| Formula | C19H21ClN4O | M. Wt | 356.85 |
| Purity | 98% | Storage | Store at 4-8°C |
| Description | 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. 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. 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. | ||
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