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5'-Fluoroindirubinoxime

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Chemical Structure| 861214-33-7 同义名 : 5'-FIO;PD 082106;5′-Fluoroindirubinoxime;5’-FIO;compound 13
CAS号 : 861214-33-7
货号 : A929501
分子式 : C16H10FN3O2
纯度 : 98%
分子量 : 295.268
MDL号 : MFCD18086923
存储条件:

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 85 mg/mL(287.87 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM. 5'-Fluoroindirubinoxime (5’-FIO, compound 13) exhibits IC50 values of 1.53 μM and 1.27 μM for VEGFR2 and Aurora A, respectively[1]. Indirubin derivatives showed potent antiproliferative activity on various human cancer cells and oncogenic RK3E-ras rat kidney cells, with IC(50) ranging from 1 to 12 mumol/L. Treatment with indirubin derivatives induced the activation of caspase-7 followed by apoptosis in RK3E-ras cells. Indirubin derivatives showed strong antitumor activity in rat solid and oral tumor models. Direct injection of indirubin derivatives every other day for 10 days induced significant inhibition of tumor growth in Sprague-Dawley rats bearing RK3E-ras-induced tumors. Histologically, treatment with indirubin derivatives caused significant inhibition of tumor formation with increased apoptosis and decreased tumor cell proliferation. Novel indirubin derivatives 5'-nitro-indirubinoxime, 5'-fluoro-indirubinoxime, and 5'-trimethylacetamino-indirubinoxime effectively arrested the tumor growth by inhibiting cell proliferation and inducing apoptosis[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.39mL

0.68mL

0.34mL

16.93mL

3.39mL

1.69mL

33.87mL

6.77mL

3.39mL

参考文献

[1]Choi SJ, Moon MJ, Lee SD, Choi SU, Han SY, Kim YC. Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells. Bioorg Med Chem Lett. 2010 Mar 15;20(6):2033-7

[2]Kim SA, Kim YC, Kim SW, Lee SH, Min JJ, Ahn SG, Yoon JH. Antitumor activity of novel indirubin derivatives in rat tumor model. Clin Cancer Res. 2007 Jan 1;13(1):253-9