Vimentin-IN-1|2319587-80-7|-陌孚医药/Medlife

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Vimentin-IN-1

目录号: PL10719 纯度: ≥99%

CAS No. :2319587-80-7

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中文名称	Vimentin-IN-1
中文别名	化合物 ANTICANCER AGENT 82
英文名称	Vimentin-IN-1
英文别名	Anticancer agent 82;HY-151424;MS-26462;F84652;CS-0611676;VIMENTIN-IN-1;2319587-80-7;SCHEMBL23595654;Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]-
Cas No.	2319587-80-7
分子式	C₁₉H₁₈Cl₂N₄O
分子量	389.28
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Vimentin-IN-1 是 FiVe1 衍生物，是一种口服有效的选择性抗癌剂。FiVe1 能够结合 III 型中间丝蛋白 vimentin (VIM)，诱导 Ser56 过度磷酸化，导致有丝分裂的选择性中断和转化表达 VIM 的间充质癌细胞的多核化。Vimentin-IN-1 比 FiVe1 表现出更好的口服利用度和药代动力学特征。
生物活性	Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1.
性状	Solid
IC50 & Target[1][2]	vimentin (VIM)
体外研究(In Vitro)	Vimentin-IN-1 (compound 4e) (0-10 mM; 72 h) inhibits a marked improvement in potency with an IC50 value of 44 nM against HT-1080 fibrosarcoma, better than than FiVe1 (IC50=1.6 μM, HT-1080). Vimentin-IN-1 (0.1 μM; 24 h) induces phosphorylation of VIM at Ser56. Vimentin-IN-1 (100 μM; sampled at 0, 5, 15, 30, 45, and 60 min) exhibits poor stability with 0.0% remaining after 60 min of incubation in mouse liver microsome. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Vimentin-IN-1 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1. Pharmacokinetic properties of Vimentin-IN-1 in mice Route Dose (mg/kg)
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
参考文献	[1]. Martínez-Pe?a F, et al. Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers. Eur J Med Chem. 2022 Nov 15;242:114638.

溶解度数据	In Vitro: DMSO : 25 mg/mL (64.22 mM; Need ultrasonic)配制储备液

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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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