Potent PARP1 Degrader (PROTAC™)
SK 575 is a potent PARP1 Degrader (PROTAC®; DC50 ≤ 6.72 nM, >99% PARP1 degradation at 10 nM). It comprises the PARP1/2 inhibitor Olaparib (Cat. No. 7579), joined by a linker to cereblon/cullin 4A ligand Thalidomide (Cat. No. 0652). SK 575 inhibits the growth of various cancer cell lines bearing BRCA1/2 mutations with IC50 values in the nanomolar range. It effectively reduces PARP1 protein levels in mouse SW620 tumor xenograft models. SK 575 dose-dependently potentiates the antitumor activity of Temozolomide (Cat. No. 2706) and Cisplatin (Cat. No. 2251)
in vivo
.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-124631 |
| Réf. fabricant | 18788436 |
| Nom chimique ou matériau | N-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-12-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-12-oxododecanamide |
| CAS | 2523016-96-6 |
| Quantité | 5 mg |
| Cible | PARP |
| Formule moléculaire | C<sub>47</sub>H<sub>53</sub>FN<sub>8</sub>O<sub>8</sub> |
| Pureté | 0.98 |
