FLLL32

Name: FLLL32
Brand: Selleck Chemicals
SKU: S7259
Rating: 5 (4 reviews)

For research use only. Not for use in humans.

Catalog No.S7259

4 publications

Molecular Weight(MW): 464.55

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.

Selleck's FLLL32 has been cited by 4 publications

Biochem Biophys Res Commun, 2019, 514(3):639-644

PubMed: 31076105 ( click the link to review the publication )

Exp Ther Med, 2017, 14(4):3926-3934

PubMed: 29043002 ( click the link to review the publication )

Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011

PubMed: 28742207 ( click the link to review the publication )

Cancer Sci, 2016, 107(7):944-54

PubMed: 27088889 ( click the link to review the publication )

2 Customer Reviews

Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.

Cancer Sci, 2016, 107(7):944-54. . FLLL32 purchased from Selleck.

Flow cytometry detection of cell proliferation.

Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011. FLLL32 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.

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

Kinase Assay:^[1]	- Collapse 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]	- Collapse 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. (Only for Reference)
Animal Research:^[1]	- Collapse Animal Models: MDA-MB-231 xenografted mice Formulation: DMSO Dosages: 50 mg/kg, daily Administration: i.p. (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	92 mg/mL (198.04 mM)
	Ethanol	25 mg/mL warmed (53.81 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download FLLL32 SDF

Molecular Weight	464.55
Formula	C₂₈H₃₂O₆
CAS No.	1226895-15-3
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	COC1=CC=C(/C=C/C(=O)C2(CCCCC2)C(=O)\C=C\C3=CC(=C(OC)C=C3)OC)C=C1OC

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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.

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JAK Signaling Pathway Map

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FLLL32