RBN-2397 是一种有效的、选择性的、具有口服活性的跨物种 NAD+ 竞争性 PARP7 抑制剂，IC50 小于 3 nM。它选择性结合 PARP7 ，Kd为0.001 μM，可恢复干扰素 I 型信号转导，有用于晚期或转移性实体肿瘤的研究潜力。

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

Inhibition of PARP7 with RBN-2397 can potently inhibit the growth of cancer cells and restore interferon signaling, effectively releasing the brake cancer uses to hide from the immune system and suppress both innate and adaptive immune mechanisms.RBN-2397 inhibits cells proliferation(IC50 value of 20 nM in NCI-H1373 lung cancer cells), 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,and inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM[2].

RBN-2397 oral administration induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice.RBN-2397 oral administration 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.The half-life (t1/2) of RBN-2397 in vivo is 325 mins[2].

2381037-82-5

C20H23F6N7O3

523.43

DMSO:247 mg/mL (471.89mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years