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Medchemexpress LLC RBN-2397 | 2381037-82-5 | >99.8% | 523.43 | 1 ML
Supplier: Medchemexpress LLC HY13617410MM/1ML
RBN-2397 is a potent, orally active, and across-species NAD+ competitive inhibitor of PARP7 (IC50<3 nM). It selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has potential for the study of advanced or metastatic solid tumors. It inhibits cell proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells and shows a restoration of type I IFN response by increasing STAT1 phosphorylation in NCI-H1373 human lung cancer cells. It also inhibits cell MARylation with an EC50 value of 1 nM.
- Induces tumor-specific adaptive immune memory in a CT26 syngeneic model
- Causes complete regressions at a dose of 100 mg/kg
- Exerts dose-dependent effects on tumor growth
- Half-life (t1/2) in vivo is 325 minutes
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