|5'-氟-3-(肟基)-[2,3'-双吲哚亚基]-2'-酮|CsnPharm

CAS No.: 861214-33-7

5'-Fluoroindirubinoxime/5'-氟二异丁酮肟 Catalog No. CSN22654

Synonyms: 5'-FIO;PD 082106;5’-FIO

5'-Fluoroindirubinoxime is an inhibitor of FMS-like receptor tyrosine kinase-3 (FLT3) with IC50 of 15 nM.

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实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3868 mL
- 16.9338 mL
- 33.8675 mL
- 5 mM
- 0.6774 mL
- 3.3868 mL
- 6.7735 mL
- 10 mM
- 0.3387 mL
- 1.6934 mL
- 3.3868 mL

技术信息

CAS号

861214-33-7

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H10FN3O2

运输

蓝冰

分子量

295.27

别名

5'-FIO;PD 082106;5’-FIO;5′-Fluoroindirubinoxime

溶解度

DMSO	80.0 mg/mL (270.9 mM) warming

动物实验配方

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5'-Fluoroindirubinoxime/5'-氟二异丁酮肟 Catalog No. CSN22654

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