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同义名 : | Atamparib |
CAS号 : | 2381037-82-5 | |
货号 : | A1329221 | |
分子式 : | C20H23F6N7O3 | |
纯度 : | 99%+ | |
分子量 : | 523.43 | |
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 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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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 | |||
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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 |
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[1]RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency |