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FLLL32

Name: FLLL32
Brand: Selleck Chemicals
SKU: S7259
Rating: 5 (9 reviews)

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.

CAS No. 1226895-15-3

Selleck's FLLL32 has been cited by 9 Publications

2 Customer Reviews

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JAK Signaling Pathway Map

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.

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	464.55
Formula	C₂₈H₃₂O₆
CAS No.	1226895-15-3
Storage	3 years	-20°C	powder
Storage	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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