MedChemExpress LLC (MCE)

MedChemExpress - Model RBN-2397 - 2381037-82-5

RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors[1][2].

RBN-2397

MCE China：RBN-2397

Brand：MedChemExpress (MCE)

Cat. No.HY-136174

CAS：2381037-82-5

Purity：99.86%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping：Room temperature in continental US; may vary elsewhere.

Description：RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.

In Vitro：RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells? proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells[2].RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells[2].RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM[2].

In Vivo：RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice[2].RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg[2].The half-life (t1/2) of RBN-2397 in vivo is 325 mins[2].

IC50 & Target：PARP-7 3 nM (IC50) PARP-7 1 nM (Kd)

References：

[1]. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency

[2]. Melissa Vasbinder, et al. RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways.

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