5'-Fluoroindirubinoxime

Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.[Pubmed:20153646]

Bioorg Med Chem Lett. 2010 Mar 15;20(6):2033-7.

Indirubin derivatives were identified as potent FLT3 tyrosine kinase inhibitors with anti-proliferative activity at acute myeloid leukemic cell lines, RS4;11 and MV4;11 which express FLT3-WT and FLT3-ITD mutation, respectively. Among several 5 and 5'-substituted indirubin derivatives, 5-fluoro analog, 13 exhibited potent inhibitory activity at FLT3 (IC(50)=15 nM) with more than 100-fold selectivity versus 6 other kinases and potent anti-proliferative effect for MV4;11 cells (IC(50)=72 nM) with 30-fold selectivity versus RS4;11 cells. Cell cycle analysis indicated that compound 13 induced cell cycle arrest at G(0)/G(1) phase in MV4;11 cells.

Inhibition of Toxoplasma gondii by indirubin and tryptanthrin analogs.[Pubmed:18824607]

Antimicrob Agents Chemother. 2008 Dec;52(12):4466-9.

New drugs are needed for treatment of Toxoplasma gondii infections. We tested derivatives of principles found in Isatis indigotica for in vitro efficacy against T. gondii infection. Indirubin-3'-oxime analogs showed modest micromolar activity, while tryptanthrin derivatives displayed 50% inhibitory doses in the low nanomolar range. Tryptanthrins have potential as anti-Toxoplasma infection therapeutics.

Antitumor activity of novel indirubin derivatives in rat tumor model.[Pubmed:17200363]

Clin Cancer Res. 2007 Jan 1;13(1):253-9.

PURPOSE: The novel indirubin derivatives 5'-nitro-indirubinoxime, 5'-fluoro-indirubinoxime, and 5'-trimethylacetamino-indirubinoxime were designed and tested for antitumor activity both in vitro and in vivo using rat tumor model. EXPERIMENTAL DESIGN: Three-week-old male Sprague-Dawley rats were inoculated s.c. on the left flank with 10(7) RK3E-ras rat kidney epithelial cells harboring k-ras gene. Alternatively, 5 x 10(6) RK3E-ras cells were injected into the oral mucosa. Indirubin derivative treatment began on the 3rd or 6th day after oral or s.c. cell injection, respectively. Indirubin derivatives were directly injected into the tumor every other day for a total of five times. Animals were monitored daily and tumor volume was measured by caliper. RESULTS: 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. CONCLUSIONS: Our data showed that 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. These findings provide the potential value of indirubin derivatives as novel candidates for antitumor agents.

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

5'-Fluoroindirubinoxime,861214-33-7,Natural Products,FLT3, buy 5'-Fluoroindirubinoxime , 5'-Fluoroindirubinoxime supplier , purchase 5'-Fluoroindirubinoxime , 5'-Fluoroindirubinoxime cost , 5'-Fluoroindirubinoxime manufacturer , order 5'-Fluoroindirubinoxime , high purity 5'-Fluoroindirubinoxime