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RBN-2397

CAS No. : 2381037-82-5

MCE 站：RBN-2397

产品活性：RBN-2397 是一种强效的，跨物种的，且具有口服活性的 NAD⁺ 竞争性 PARP7 抑制剂，IC₅₀ 值小于 3 nM。RBN-2397 有选择性地结合 PARP7 (K_d=0.001 μM) 并可以恢复干扰素 I 型信号转导。RBN-2397 有潜力用于研究晚期或转移性实体肿瘤。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

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.
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.
RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC₅₀ value of 1 nM.

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.
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.
The half-life (t_1/2) of RBN-2397 in vivo is 325 mins.

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