Chemical Structure : EPIC-0726
货号: PC-25655Not For Human Use, Lab Use Only.
EPIC-0726 is a selective PROTAC degrader of polymerase I and transcript release factor (PTRF/Cavin1) with DC50 of 5.12 uM in U87-MG cells, Dmax=90.07%.
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EPIC-0726 is a selective PROTAC degrader of polymerase I and transcript release factor (PTRF/Cavin1) with DC50 of 5.12 uM in U87-MG cells, Dmax=90.07%.
EPIC-0726 induces PTRF degradation in pancreatic (PANC-1), hepatocellular (HepG2), lung (A459), and breast (MDA-MB-231) cancer cell lines with DC50 of 10.95 μM, 3.59 μM, 6.00 μM, and 6.60 μM, respectively.
Pharmacological UPS inhibition via MG132 abolished EPIC-0726-mediated degradation.
EPIC-0726 exhibits anti-proliferative efficacy in N37 and HYF cells with IC50 of 18.84 and 16.24 μM, respectively.
EPIC-0726 reduced CAV1 protein levels in a concentration-dependent manner, aligning with the established mechanism whereby PTRF downregulation induces CAV1 degradation.
EPIC-0726 (30 mg/kg, oral) inhibited GBM growth and synergized with TMZ.
| 分子量 | 733.92 | |
| 分子式 | C41H51N9O4 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Biao Hong, et al. Neuro Oncol. 2025 Oct 27:noaf253.
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