RBN-2397|2381037-82-5|-陌孚医药/Medlife

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RBN-2397

目录号: PL08913 纯度: ≥99%

CAS No. :2381037-82-5

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中文名称	RBN-2397
英文名称	RBN-2397
英文别名	4-[[(2S)-1-[3-Oxo-3-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy]propan-2-yl]amino]-;RBN-2397;Atamparib;B1MW2ME77A;4-[[(2S)-1-[3-oxo-3-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy]propan-2-yl]amino]-5-(trifluoromethyl)-1H-pyridazin-6-one;(S)-5-((1-(3-Oxo-3-(4-(5-(trifluoromethyl)pyrimidin-2-yl)piperazin-1-yl)propoxy)propan-2-yl)amino)-4-(trifluoromethyl)pyridazin-3(2H)-one;RBN2397;Atamparib [INN];Atamparib [USAN];BCP33764;RBN2397;RBN 2397;NSC825956;s8993;WHO 11539;D9764
Cas No.	2381037-82-5
分子式	C₂₀H₂₃F₆N₇O₃
分子量	523.43
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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。

生物活性

RBN-2397 is a potent, accross species and orally active NAD competitive inhibitor of PARP7 (IC 50 <3 nM). RBN-2397 selectively binds to PARP7 (K d =0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.

性状

Solid

IC50 & Target[1][2]

PARP-7 3 nM (IC50) PARP-7 1 nM (Kd)

体外研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency
[2]. Melissa Vasbinder, et al. RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways.

溶解度数据	In Vitro: DMSO : 200 mg/mL (382.10 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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