Description: |
5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM[1]. |
Target: |
15 nM (FLT3)[1]. |
In Vivo: |
5'-Fluoroindirubinoxime (5’-FIO, 10 μmol/L/100 μL (~2.95 mg/mL) every other day beginning on day 6, S.C..) exhibits significant anti-tumor activity in rats[2]. Animal Model: Rat tumor model based RK3E-ras cells[2]. Dosage: S.C.. Administration: 10 μmol/L/100 μL (~2.95 mg/mL) every other day beginning on day 6. Result: Effectively inhibited tumor growth. |
In Vitro: |
5'-Fluoroindirubinoxime (5’-FIO, compound 13) exhibits IC50 values of 1.53 μM and 1.27 μM for VEGFR2 and Aurora A, respectively[1]. 5'-Fluoroindirubinoxime (5’-FIO) exhibits IC50 values of 12.2 μM, 2.1 μM, 3.4 μM and 5.1 μM in A549, SNU-638, HT-1080 and RK3E-ras cancer cells, respectively. 5'-Fluoroindirubinoxime (5’-FIO) induces the apoptosis in RK3E-ras cells[2]. |
References: |
[1]. Choi SJ, et al. 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, et al. Antitumor activity of novel indirubin derivatives in rat tumor model. Clin Cancer Res. 2007 Jan 1;13(1):253-9. |