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Chemical Structure| 1226895-15-3 Chemical Structure| 1226895-15-3

Structure of FLLL32
CAS No.: 1226895-15-3

Chemical Structure| 1226895-15-3

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

Synonyms: JAK2 Inhibitor X

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Product Details of FLLL32

CAS No. :1226895-15-3
Formula : C28H32O6
M.W : 464.55
SMILES Code : O=C(C1(C(/C=C/C2=CC=C(OC)C(OC)=C2)=O)CCCCC1)/C=C/C3=CC=C(OC)C(OC)=C3
Synonyms :
JAK2 Inhibitor X
MDL No. :MFCD27976793
InChI Key :NQDROBVIYYEMDQ-WFYKWJGLSA-N
Pubchem ID :68019246

Safety of FLLL32

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of FLLL32

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • JAK2

    JAK2, IC50:<5 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
PBMCs 5 μM 24 hours FLLL32 did not affect the viability and function of PBMCs. PMC2902420
MDA-MB-453 breast cancer cells 20 μM Inhibited IL-6-induced STAT3 phosphorylation PMC2936338
MDA-MB-453 breast cancer cells 10 µM 2 hours pretreatment, 30 minutes IFNα or IL-6 stimulation Inhibited IFNα and IL-6 induced STAT3 phosphorylation PMC2843552
HEP3B liver cancer cells 2.5-10 μM 24 hours Inhibited STAT3 phosphorylation, decreased STAT3 downstream target genes, and increased cleavage of caspase-3 and PARP PMC2936338
SNU449 liver cancer cells 2.5-10 μM 24 hours Inhibited STAT3 phosphorylation, decreased STAT3 downstream target genes, and increased cleavage of caspase-3 and PARP PMC2936338
U266 multiple myeloma cells 2.5-10 μM 24 hours Inhibited STAT3 phosphorylation, decreased STAT3 downstream target genes, and increased cleavage of caspase-3 and PARP PMC2936338
U87 glioblastoma cells 2.5-10 μM 24 hours Inhibited STAT3 phosphorylation, decreased STAT3 downstream target genes, and increased cleavage of caspase-3 and PARP PMC2936338
HCT-116 colorectal cancer cells 2.5-10 μM 24 hours Inhibited STAT3 phosphorylation, decreased STAT3 downstream target genes, and increased cleavage of caspase-3 and PARP PMC2936338
SW480 colorectal cancer cells 2.5-10 μM 24 hours Inhibited STAT3 phosphorylation, decreased STAT3 downstream target genes, and increased cleavage of caspase-3 and PARP PMC2936338
PANC-1 pancreatic cancer cells 2.5 and 5 µM 24 hours Inhibited STAT3 phosphorylation, reduced STAT3 DNA-binding activity, induced caspase-3 cleavage PMC2843552
MDA-MB-231 breast cancer cells 2.5 and 5 µM 24 hours Inhibited STAT3 phosphorylation, reduced STAT3 DNA-binding activity, induced caspase-3 cleavage PMC2843552
SG 16 μM 24 hours FLLL32 treatment only reduced the viability of SG cells by approximately 20%. PMC8584525
SCC-9 0, 1, 2, 4, 8, 16 μM 24 hours FLLL32 significantly inhibited the viability of SCC-9 cells, with approximately 90% reduction in cell viability after 24 h treatment with 16 μM. PMC8584525
HSC-3 0, 1, 2, 4, 8, 16 μM 24 hours FLLL32 significantly inhibited the viability of HSC-3 cells, with approximately 90% reduction in cell viability after 24 h treatment with 16 μM. PMC8584525
CD44+/CD24+ pancreatic cancer cells 5 µM 24 hours Inhibited STAT3 phosphorylation, reduced cell viability and tumorsphere formation PMC5118001
ALDH+ pancreatic cancer cells 5 µM 24 hours Inhibited STAT3 phosphorylation, reduced cell viability and tumorsphere formation PMC5118001
MPNST cell lines 200 nM 4 days FLLL32 decreased cell survival in 5/5 tested cell lines PMC3923530
Hs294T 1.9-2.8 μM (IC 50) 48 hours FLLL32 induced apoptosis in Hs294T cells and inhibited STAT3 phosphorylation. PMC2902420
A375 1.3 μM (IC 50) 48 hours FLLL32 induced apoptosis in A375 cells and inhibited STAT3 phosphorylation. PMC2902420
Pancreatic stellate cells (PSC) 6 μM 48 hours FLLL32 treatment of PSC inhibited STAT3 phosphorylation, reduced IL-6 production, and decreased cell viability PMC3785672
TE13 5 μM 48 hours Inhibit JAK2/STAT3 signaling pathway and detect IL-6 secretion PMC4946714
TE1 5 μM 48 hours Inhibit JAK2/STAT3 signaling pathway and detect IL-6 secretion PMC4946714
Eca109 5 μM 48 hours Inhibit JAK2/STAT3 signaling pathway and detect IL-6 secretion PMC4946714
Peripheral blood mononuclear cells (PBMC) 6 μM 7 days FLLL32 abrogated PSC supernatant or IL-6/GM-CSF-induced MDSC differentiation, indicating this process is STAT3-dependent PMC3785672
T84 intestinal epithelial cells 50 µM 72 hours To evaluate the effect of FLLL32 on inflammation-induced paracellular permeability. FLLL32 pretreatment ameliorated IL-6-induced reduction in TEER at 24, 48, and 72 hours, indicating superior barrier protection compared to curcumin in vitro. PMC5476581
Normal human Schwann cells 0.5 μM Did not affect viability of normal human Schwann cells PMC3923530

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice MPNST xenograft model Intraperitoneal injection 200 mg/kg Daily for 23 days FLLL32 significantly delayed MPNST xenograft formation PMC3923530
Mice Neurofibroma model Not specified 200 mg/kg/day Once daily for 60 days FLLL32 inhibited STAT3-Y705 phosphorylation, reduced neurofibroma volume and macrophage numbers, and suppressed cell proliferation. PMC6461477
CD-1 mice Necrotizing enterocolitis (NEC) model Oral gavage 25 mg/kg Once daily for 6 days (P9 to P14) To assess the protective effects of FLLL32 on intestinal inflammation and injury in the NEC model. FLLL32 pretreatment reduced intestinal injury scores, NEC incidence, improved intestinal permeability, and decreased proinflammatory cytokines (TNF-α, IL-6, IL-1β, and GRO-α) levels. PMC5476581
NOD/SCID mice MDA-MB-231 breast cancer xenografts Intraperitoneal 50 mg/kg Daily for 18 days Suppressed tumor growth PMC2936338
Nude mice MDA-MB-231 breast cancer xenograft model Intraperitoneal injection 50 mg/kg Once daily for 19 days Inhibited tumor growth, reduced tumor volume PMC2843552
MRL/lpr mice Diffuse proliferative lupus nephritis (DPLN) model Intraperitoneal injection 50 mg/kg Once daily for 4 weeks FLLL32 combined with methylprednisolone therapy significantly inhibited STAT3 activation, improved acute kidney damage, reduced interstitial infiltration of inflammatory cells, and decreased AKI incidence in MRL/lpr mice. PMC11136473

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.53mL

4.31mL

2.15mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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