9-ING-41|1034895-42-5|(Elraglusib)-陌孚医药/Medlife

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9-ING-41 (Synonyms: Elraglusib)

目录号: PL02160 纯度: ≥98%

CAS No. :1034895-42-5

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中文名称	9-ING-41
英文名称	9-ING-41
英文别名	ND1SOF0DLU;BDBM50267716;SB19735;3-(5-Fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo[4,5-f]indol-7-yl)pyrrole-2,5-dione;1H-Pyrrole-2,5-dione, 3-(5-fluoro-3-benzofuranyl)-4-(5-methyl-5H-1,3-dioxolo(4,5-F)indol-7-yl)-;4-(5-methyl-5H-[1,3]dioxolo[4,5-f]-indol-7-yl)-3-(5-fluoro-1-benzofuran-3-yl)-1 h-pyrrole-2,5-dione;3-(5-Fluoro-benzofuran-3-yl)-4-(5-methyl-5H-(1,3)dioxolo(4,5-F)indol-7-yl)-pyrrole-2,5-dione;9-ING-41;elraglusib;3-(5-fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo[4,5-f]indol-7-yl)-1H-pyrrole-2,5-dione;3-(5-fluoro-1-benzofuran-3-yl)-4-(5-methyl-[1,3]dioxolo[4,5-f]indol-7-yl)pyrrole-2,5-dione;Elraglusib [USAN];GTPL11412;s9602;WHO 11553;compound 26 [PMID: 19338355];E73486
Cas No.	1034895-42-5
分子式	C₂₂H₁₃FN₂O₅
分子量	404.35
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

9-ING-41 是一种基于马来酰亚胺的 ATP 竞争性和选择性的糖原合酶激酶-3β (GSK-3β) 抑制剂，IC₅₀ 为 0.71 μM。9-ING-41 显著导致癌细胞的细胞周期停滞，自噬和凋亡。9-ING-41 具有抗癌活性，并具有增强化疗药物抗肿瘤作用的潜力。

生物活性

9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC 50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.

性状

Solid

IC50 & Target[1][2]

GSK-3β 0.71 μM (IC50)

体外研究(In Vitro)

9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis.
9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells.
9-ING-41 (10?μM; for 72?hours) increases the expression of LC3, an autophagy marker.
9-ING-41 (compound 26; 5 μM; for 6, 12, 24, 36 h) results in a pronounced decrease in NFκB-mediated expression of XIAP, the most potent antiapoptotic protein, leading to subsequent apoptosis in BXPC3 pancreatic cancer cells.
9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM.
9-ING-41 (10?μM; for 72?hours) causes cell cycle blockage at G2/M after 24?hours. 9-ING-41 treatment induces apoptotic cell death in bladder cancer cells.
9-ING-41 (25?μM; for 96?hours) significantly decreases expression of Cdk1 and Cyclin B1 pr

体内研究(In Vivo)

9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity in a mouse model of MCL. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NSG (NOD.Cg-PrkdcIl2rg/Sz

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]. Irina N Gaisina, et al. From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. J Me
[2]. Wu X, et al. Targeting glycogen synthase kinase 3 for therapeutic benefit in lymphoma. Blood. 2019 Jul 25;134(4):363-373.

溶解度数据	In Vitro: DMSO : 50 mg/mL (123.66 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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