RBN-2397是一种高效、跨物种且口服活性的 NAD+ 竞争性 PARP7 抑制剂(IC50 < 3 nM)。RBN-2397 选择性结合 PARP7(Kd = 0.001 μM)并恢复 IFN 信号通路,具有研究晚期或转移性实体瘤的潜力。
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产品名称 | PARP ↓ ↑ | PARP1 ↓ ↑ | PARP2 ↓ ↑ | PARP3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PJ34 HCl |
++
PARP, EC50: 20 nM |
99%+ | |||||||||||||||||
Rucaparib phosphate |
++++
PARP, Ki: 1.4 nM |
99%+ | |||||||||||||||||
3-Aminobenzamide |
++
PARP, IC50: <50 nM |
98% | |||||||||||||||||
AZD-2461 | ✔ | 99%+ | |||||||||||||||||
BGP-15 | ✔ | 99%+ | |||||||||||||||||
NU1025 |
+
PARP, IC50: 400 nM |
97% | |||||||||||||||||
Benzamide |
+
PARP, IC50: 3.3 μM |
98% | |||||||||||||||||
Picolinamide |
+
PARP, IC50: 95 μM |
98% | |||||||||||||||||
AG14361 |
+++
PARP1, Ki: <5 nM |
98+% | |||||||||||||||||
Iniparib | ✔ | 98% | |||||||||||||||||
Talazoparib |
++++
PARP1, IC50: 0.57 nM |
99%+ | |||||||||||||||||
NMS-P118 |
++
PARP1, Kd: 0.009 μM |
98+% | |||||||||||||||||
UPF 1069 |
+
PARP1, IC50: 8.0 μM |
++
PARP2, IC50: 0.3 μM |
98% | ||||||||||||||||
A-966492 |
++++
PARP1, EC50: 1 nM PARP1, Ki: 1 nM |
+++
PARP2, Ki: 1.5 nM |
99%+ | ||||||||||||||||
Veliparib |
++
PARP1, Ki: 5.2 nM |
+++
PARP2, Ki: 2.9 nM |
98% | ||||||||||||||||
Niraparib tosylate |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
99%+ | ||||||||||||||||
Stenoparib |
++++
PARP1, IC50: 1 nM |
++++
PARP2, IC50: 1.2 nM |
98% | ||||||||||||||||
Olaparib |
+++
PARP1, IC50: 5 nM |
++++
PARP2, IC50: 1 nM |
98% | ||||||||||||||||
Niraparib |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
98% | ||||||||||||||||
ME0328 |
+
PARP1, IC50: 6.3 μM |
+
PARP3, IC50: 0.89 μM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 2381037-82-5 |
分子式 | C20H23F6N7O3 |
分子量 | 523.432 |
别名 | Atamparib |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
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 |