product name FLLL32
Description: FLLL32, a novel curcumin analogue, is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. In multiple human melanoma cell lines, after a 24 hour treatment with FLLL32, the STAT3 phosphorylation at Tyr705 but not at Tyr727 was inhibited. In the experiment with multiple human melanoma cell line, no appreciable alteration in the phosphorylation of Jak2, even when the concentration of FLLL32 was 8 μM, was observed. This meant that FLLL32 likely directly acted against the STAT3 protein. FLLL32 at concentrations ranged from 2-4 μM for only 4 hours reduced pSTAT3 and induce cell death.
References: Cancer Res. 2010;70(6):2445-54; Mol Cancer. 2010;9:217; Invest New Drugs. 2012 Jun;30(3):916-26.
464.55
Formula
C28H32O6
CAS No.
1226895-15-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 92 mg/mL (198.0 mM)
Water: <1 mg/mL
Ethanol: 25 mg/mL warmed (53.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In MDA-MB-231 breast and PANC-1 pancreatic cancer cells, FLLL32 downregulates STAT3 phosphorylation and DNA-binding activity. In MDA-MB-231 cells, FLLL32 inhibit the formation of colonies and cell invasion. In human multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cell lines, FLLL32 also leads to the inhibition of cell proliferation and the induction of caspase-3 and PARP cleavages. Kinase Assay: JAK2 kinase activity was assessed with the HTScan JAK2 Kinase Assay Kit per manufacturers protocol. The possible effects of FLLL32 on the other 10 purified human protein kinases were determined by using a Kinase Profiler Assay. Cell Assay: Cells are seeded in 96-well plates (3,000 per well) in triplicate and then treated with 0.5 to 5 μM of FLLL31 or FLLL32 or with 0.5 to 30 μM of curcumin for 72 h. MTT (25 μL) is added to each sample and incubated for 3.5 h. Then, 100 μL of N,N-dimethylformamide solubilization solution are added to each well. The absorbance at 450 nm is read the following day. IC50 are determined using Sigma Plot 9.0 software. |
|---|---|
| In Vivo | In MDA-MB-231 xenografted mice, FLLL32 (50 mg/kg, i.p.) significantly reduces tumor burdens. In mouse xenografts with OS-33 osteosarcoma cells, FLLL32 (50 mg/kg, i.p.) also inhibits tumor growth by targeting STAT3. |
| Animal model | MDA-MB-231 xenografted mice |
| Formulation & Dosage | Dissolved in DMSO; 50 mg daily; i.p. injection |
| References | Cancer Res. 2010 Mar 15;70(6):2445-54; Mol Cancer. 2010 Aug 16;9:217; Invest New Drugs. 2012 Jun;30(3):916-26. |
