RBN-2397

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Chemical Structure| 2381037-82-5 同义名 : Atamparib
CAS号 : 2381037-82-5
货号 : A1329221
分子式 : C20H23F6N7O3
纯度 : 99%+
分子量 : 523.432
MDL号 : MFCD32701939
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 190 mg/mL(362.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 PARP7, which is induced by cancer relevant stress (e.g., aryl hydrocarbon receptor ligands such as chemicals found in cigarette smoke and kynurenine), acts as a tumor cell brake in cytosolic nucleic acid sensing and the Type I interferon (IFN) response. RBN-2397 is a potent, selective and orally active NAD+ competitive inhibitor of PARP7 with IC50 <3 nM and KD <1 nM. RBN-2397 blocked proliferation in NCI-H1373 lung cancer cells with a GI50 of 20 nM. Further, RBN-2397 (0.4-1000 nM; 24 hr) restored cytosolic nucleic acid sensing and induced Type I IFNs in NCI-H1373 lung cancer cells in a dose-dependent manner. In vivo, RBN-2397 induced tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses[2].
作用机制 RBN-2397 interacts with adenosine sub-pocket and nicotinamide sub-pocket of PARP7[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.55mL

1.91mL

0.96mL

19.10mL

3.82mL

1.91mL
参考文献

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

[2]RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways