FLLL32

Catalog No.S7259

For research use only.

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.

FLLL32 Chemical Structure

CAS No. 1226895-15-3

Selleck's FLLL32 has been cited by 9 Publications

2 Customer Reviews

Purity & Quality Control

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Biological Activity

Description FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
Targets
JAK2 [1]
<5 μM
In vitro

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. [1] 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. [2]

In vivo In MDA-MB-231 xenografted mice, FLLL32 (50 mg/kg, i.p.) significantly reduces tumor burdens. [1] In mouse xenografts with OS-33 osteosarcoma cells, FLLL32 (50 mg/kg, i.p.) also inhibits tumor growth by targeting STAT3. [3]

Protocol (from reference)

Kinase Assay:[1]
  • JAK2 and other human kinase activity assays:

    JAK2 kinase activity was assessed with the HTScan JAK2 Kinase Assay Kit per manufacturer's protocol. The possible effects of FLLL32 on the other 10 purified human protein kinases were determined by using a Kinase Profiler Assay.

Cell Research:[1]
  • Cell lines: MDA-MB-231 cell line
  • Concentrations: ~5 μM
  • Incubation Time: 72 hours
  • Method: 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.
Animal Research:[1]
  • Animal Models: MDA-MB-231 xenografted mice
  • Dosages: 50 mg/kg, daily
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 464.55
Formula

C28H32O6

CAS No. 1226895-15-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=C(C=C1)C=CC(=O)C2(CCCCC2)C(=O)C=CC3=CC(=C(C=C3)OC)OC)OC

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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