AVN-944|297730-17-7|(VX-944)-陌孚医药/Medlife

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AVN-944 (Synonyms: VX-944)

目录号: PL03477 纯度: ≥99%

CAS No. :297730-17-7

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中文名称	AVN-944
中文别名	[(1S)-1-[3-[[[[3-甲氧基-4-(5-恶唑基)苯基]氨基]羰基]氨基]苯基]乙基]氨基甲酸 (1R)-1-(氰基甲基)丙基酯;AVN-944
英文名称	AVN-944
英文别名	[(2R)-1-cyanobutan-2-yl] N-[(1S)-1-[3-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoylamino]phenyl]ethyl]carbamate;AVN 944;AVN-944
Cas No.	297730-17-7
分子式	C₂₅H₂₇N₅O₅
分子量	477.51
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

AVN-944 (VX-944) 是一种口服有效、选择性、非竞争性和特异性的 IMPDH (肌苷一磷酸脱氢酶)抑制剂。AVN-944 是从头合成鸟嘌呤核苷酸的必要限速酶。AVN-944 也是一种沙粒病毒 RNA 合成 (arenavirus RNA synthesis) 抑制剂，可阻断沙粒病毒感染。AVN-944 具有广泛的抗癌活性，可用于多发性骨髓瘤 (MM) 和急性髓系白血病 (AML) 的研究。

生物活性

AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research.

性状

Solid

体外研究(In Vitro)

AVN-944 (0-1 μM, 48 h) inhibits growth of human multiple myeloma (MM) cell lines in a dose-dependent manner.
AVN-944 (800?nM, 0-72?h) induces apoptosis in MM cell lines via a caspase-independent, Bax/AIF/Endo G pathway.
AVN-944 (0-200 nM) enhances the cytotoxicity of Doxorubicin (HY-15142A) and Melphalan (HY-17575).
AVN-944 inhibits the proliferation of the human MV-4-11 and murine Ba/F3-Flt3-ITD-dependent cell lines with IC50 values of 26 and 30 nM, respectively.
AVN-944 (0-32 μM, 48?h) shows good activity against arenavirus infection at low doses (7.5?μM) with less cytotoxicity.
AVN-944 (0-6.4 μM, 48 h) does not reduce the viability of peripheral blood mononuclear cells (PBMNCs). has not independently confirmed the accuracy of these methods.

体内研究(In Vivo)

AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Balb/c mice (leukem

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]. Zimmermann AG, et al. Inosine-5-monophosphate dehydrogenase: regulation of expression and role in cellular proliferation and T lymphocyte activation. Prog Nucleic Acid Res Mol Biol. 1998;61:181-209.
[2]. Huang M, et al. Guanine nucleotide depletion inhibits pre-ribosomal RNA synthesis and causes nucleolar disruption. Leuk Res. 2008 Jan;32(1):131-41.

溶解度数据	In Vitro: DMSO : 100 mg/mL (209.42 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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