VX-984|1476074-39-1|(M9831)-陌孚医药/Medlife

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VX-984 (Synonyms: M9831)

目录号: PL04978 纯度: ≥99%

CAS No. :1476074-39-1

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中文名称	VX-984
英文名称	VX-984
英文别名	0C33IBK195;(S)-N-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl-4',6'-d2)amino)propan-2-yl)quinoline-4-carboxamide;SB19729;4-Quinolinecarboxamide, N-methyl-8-((1S)-1-methyl-2-((2'-methyl(4,5'-bipyrimidin)-6-yl-4',6'-d2)amino)ethyl)-;N-Methyl-8-((2S)-1-((6-(2-methyl(2H2)pyrimidin-5-yl)pyrimidin-4-yl)amino)propan-2-yl)quinoline-4-carboxamide;VX-984 free base;VX984;NSC792969;VX-984;M9831
Cas No.	1476074-39-1
分子式	C₂₃H₂₃N₇O
分子量	415.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

VX-984 是一种口服有效、选择性的、可透过血脑屏障的 DNA-PK 抑制剂。VX-984 有效抑制 NHEJ (非同源性末端接合)，增加DSBs (DNA 双链断裂)。VX-984 可用于胶质母细胞瘤 (GBM) 和非小细胞肺癌 (NSCLC) 的研究。

生物活性

VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research[1][2][3].

性状

Solid

体外研究(In Vitro)

VX-984 (0-500 nM, 30 min) inhibits radiation-induced DNA-PKcs phosphorylation in U251 and NSC11 cells.
VX-984 (0-500 nM) enhances the radiosensitivity of U251 and NSC11 cells in a concentration-dependent manner.
VX-984 inhibits the repair of radiation-induced DNA double-strand breaks (DSBs).
VX-984 (0-1 μM) increases alternate pathways of DSB repair, including HR (homologous recombination) and mutagenic NHEJ (mNHEJ). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

VX-984 (0-100 mg/kg, Oral gavage, daily) inhibits radiation-induced DNA-PKcs phosphorylation in orthotopic brain tumor xenografts.
VX-984 (0-50 mg/kg, Oral gavage, twice a day for 2 days) enhances the radiosensitivity of brain tumor xenografts. 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]. Timme CR, et al. The DNA-PK Inhibitor VX-984 Enhances the Radiosensitivity of Glioblastoma Cells Grown In Vitro and as Orthotopic Xenografts. Mol Cancer Ther. 2018 Jun;17(6):1207-1216.
[2]. Khan AJ, et al. VX-984 is a selective inhibitor of non-homologous end joining, with possible preferential activity in transformed cells. Oncotarget. 2018 May 25;9(40):25833-25841.

溶解度数据	In Vitro: DMSO : 10 mg/mL (24.07 mM; Need ultrasonic)配制储备液

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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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