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FLLL32
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FLLL32图片
CAS NO:1226895-15-3
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)464.55
FormulaC28H32O6
CAS No.1226895-15-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 92 mg/mL (198.0 mM)
Water: <1 mg/mL
Ethanol: 25 mg/mL warmed (53.8 mM)
Solubility (In vivo)

Chemical Name: (2E,2'E)-1,1'-(cyclohexane-1,1-diyl)bis(3-(3,4-dimethoxyphenyl)prop-2-en-1-one)

InChi Key: NQDROBVIYYEMDQ-WFYKWJGLSA-N

InChi Code: InChI=1S/C28H32O6/c1-31-22-12-8-20(18-24(22)33-3)10-14-26(29)28(16-6-5-7-17-28)27(30)15-11-21-9-13-23(32-2)25(19-21)34-4/h8-15,18-19H,5-7,16-17H2,1-4H3/b14-10+,15-11+

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

FLLL-32; FLLL32; FLLL 32

实验参考方法
In Vitro

In vitro activity: 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. 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.


Kinase Assay: 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 Assay: 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.

In VivoIn MDA-MB-231 xenografted mice, FLLL32 (50 mg/kg, i.p.) significantly reduces tumor burdens. In mouse xenografts with OS-33 osteosarcoma cells, FLLL32 (50 mg/kg, i.p.) also inhibits tumor growth by targeting STAT3.
Animal modelMDA-MB-231 xenografted mice
Formulation & DosageDissolved in DMSO; 50 mg daily; i.p. injection
References

Cancer Res. 2010 Mar 15;70(6):2445-54; Mol Cancer. 2010 Aug 16;9:217; Invest New Drugs. 2012 Jun;30(3):916-26.

生物活性


FLLL31 and FLLL32 inhibit STAT3-dependent transcriptional activation.Cancer Res. 2010 Mar 15;70(6):2445-54.



FLLL31 and FLLL32 are potent inhibitors of STAT3 phosphorylation. Cancer Res. 2010 Mar 15;70(6):2445-54.





A. FLLL31 and FLLL32 reduce STAT3’s ability to bind DNA in nuclear extracts isolated from MDA-MB-231 breast cancer and PANC-1 pancreatic cancer cells. B. FLLL31-and FLLL32-mediated decreases in STAT3 DNA binding activity correlate with increases in STAT1 DNA binding activity in MDA-MB-231 cells. Cancer Res. 2010 Mar 15;70(6):2445-54.


A. Comparison of tumor volumes over time in mouse xenografts with MDA-MB-231 breast cancer cells. B. Effect of FLLL32 on vascularity and tumor growth in CAMs. The pictures show blood vessel density around xenografted tumors (t). C. Relative tumor sizes of CAM xenografts. D. Relative CAM blood vessel density. Cancer Res. 2010 Mar 15;70(6):2445-54.