5'-Fluoroindirubinoxime

Names

[ Name ]:
5'-Fluoroindirubinoxime

[Synonym ]:
MFCD18086923

Biological Activity

[Description]:

5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

[Target]

15 nM (FLT3)[1].

[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].

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₁₀FN₃O₂

[ Molecular Weight ]:
295.26800

[ Exact Mass ]:
295.07600

[ PSA ]:
77.21000

[ LogP ]:
3.01600

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

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