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FLLL32 JAK inhibitor

Cat.No.S7259

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

Chemical Structure

Molecular Weight: 464.55

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S725901 DMSO]92 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 99.79%
99.79

Chemical Information, Storage & Stability

Molecular Weight 464.55 Formula

C28H32O6

 Storage (From the date of receipt)
CAS No. 1226895-15-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C(C=C1)C=CC(=O)C2(CCCCC2)C(=O)C=CC3=CC(=C(C=C3)OC)OC)OC

Solubility

In vitro
Batch:

DMSO : 92 mg/mL ( (198.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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, this compound inhibits the formation of colonies and cell invasion. [1] In human multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cell lines, it also leads to the inhibition of cell proliferation and the induction of caspase-3 and PARP cleavages. [2]
Kinase Assay
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 this compound on the other 10 purified human protein kinases were determined by using a Kinase Profiler Assay.
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, this compound (50 mg/kg, i.p.) also inhibits tumor growth by targeting STAT3. [3]
References

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