Venadaparib|1681017-83-3|(IDX-1197)-陌孚医药/Medlife

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Venadaparib (Synonyms: IDX-1197)

目录号: PL08912 纯度: ≥98%

CAS No. :1681017-83-3

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中文名称	Venadaparib
英文名称	Venadaparib
英文别名	Venadaparib;PUP792O0IW;Venadaparib [INN];GTPL11184;example 26 [WO2015037939A1];C1(CC1)NCC1CN(C1)C(=O)C=1C=C(CC2=NNC(C3=CC=CC=C23)=O)C=CC1F;1(2H)-Phthalazinone, 4-((3-((3-((cyclopropylamino)methyl)-1-azetidinyl)carbonyl)-4-fluorophenyl)methyl)-;4-((3-((3-((Cyclopropylamino)methyl)-1-azetidinyl)carbonyl)-4-fluorophenyl)methyl)-1(2H)-phthalazinone;4-(3-(3-((cyclopropylamino)methyl)azetidine-1-carbonyl)-4-fluorobenzyl)-phthal;AT31387;4-(3-(3-((cyclopropylamino)methyl)azetidine-1-carbonyl)-4-fluorobenzyl)-phthalazin-1(2H)-one;4-(3-(3
Cas No.	1681017-83-3
分子式	C₂₃H₂₃FN₄O₂
分子量	406.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Venadaparib (IDX-1197) 是一种有效、选择性和具有口服活性的 PARP 抑制剂，对 PARP1 和 PARP2 的 IC₅₀ 分别为 1.4 nM 和 1.0 nM。Venadaparib 对 PARP-5 不敏感。Venadaparib 可防止 DNA 单链断裂 (SSB) 的修复，可用于实体瘤研究。

生物活性

Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC 50 s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research.

性状

Solid

IC50 & Target[1][2]

PARP1 1.4 nM (IC50) PARP2 1 nM (IC50

体外研究(In Vitro)

In DNA damage-induced Hela cells, Venadaparib (IDX-1197) significantly inhibits PARP1-mediated PAR expression (EC50 of 0.5 nM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In the germline BRCA1-mutated ovarian cancer PDX model, oral administration of Venadaparib (IDX-1197) exhibits significant PAR inhibition (>90%) in tumor tissues until 24 hr post dose. Venadaparib also dose-dependently led to potent tumor growth inhibition compared to Olaparib treatment group. 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]. Myongjae Lee, et al. Abstract A106: Development of IDX-1197, a novel, selective, and highly potent PARP inhibitor. American Association for Cancer Research, 2018.
[2]. Yong Man Kim, et al. First-in-human dose-finding study of venadaparib (IDX-1197), a potent and selective PARP inhibitor, in patients with advanced solid tumors. Journal of Clinical Oncology. 39, no. 15_suppl (May 20, 2021) 3107-3107.

溶解度数据	In Vitro: DMSO : 100 mg/mL (246.03 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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