RBN-2397

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RBN-2397 是一种有效的跨物种、口服活性的 PARP7 NAD+ 竞争性抑制剂 (IC50<3 nM)。 RBN-2397 选择性结合 PARP7 (Kd=0.001 μM) 并恢复 IFN 信号传导。

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 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 (t1/2) of RBN-2397 in vivo is 325 mins.

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. Cell Proliferation Assay Cell Line:NCI-H1373 lung cancer cells Concentration:0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM Incubation Time:24 hours Result:Blocked cell proliferation. Western Blot Analysis Cell Line:NCI-H1373 lung cancer cells Concentration:0.4 nM-1 μM Incubation Time:24 hours Result:Increasedp-STAT1 protein expression.

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 (t1/2) of RBN-2397 in vivo is 325 mins. Animal Model:CB17 SCID mice withNCI-H1373 xenografts Dosage:3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg Administration:Oral administration; once daily; 24-32 days Result:Decreased tumor volume and exerted anti-tumor effects.

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Cell Cycle/DNA Damage

PARP

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2381037-82-5

523.43

C??H??F?N?O?

>98% (HPLC)

DMSO : 250 mg/mL (477.62 mM; Need ultrasonic)

O=C1C(C(F)(F)F)=C(N[C@@H](C)COCCC(N2CCN(C3=NC=C(C(F)(F)F)C=N3)CC2)=O)C=NN1

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(-20℃)

With Ice Pack

≥ 2 years