FLLL32

Alias:
Cat No.:V0324 Purity: ≥98%
FLLL32, a synthetic curcumin analog, is a novel and potent Janus kinases-JAK2/STAT3 inhibitor with potential antitumor activity.
FLLL32 Chemical Structure CAS No.: 1226895-15-3
Product category: JAK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

FLLL32, a synthetic curcumin analog, is a novel and potent Janus kinases-JAK2/STAT3 inhibitor with potential antitumor activity. It inhibits JAK2 with IC50 of<5 μM. FLLL-32 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In human melanoma cell lines and primary melanoma cultures, FLLL32 selectively decreases STAT3 phosphorylation at Tyr705 (pSTAT3) and promotes apoptosis at micromolar amounts[1].
ln Vivo
In 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 Protocol
Dissolved in DMSO; 50 mg daily; i.p. injection
MDA-MB-231 xenografted mice
References
[1]. Bill MA, et al. The small molecule curcumin analog FLLL32 induces apoptosis in melanoma cells via STAT3inhibition and retains the cellular response to cytokines with anti-tumor activity. Mol Cancer. 2010 Jun 25;9:165.
[2]. Lin L, et al. Novel STAT3 phosphorylation inhibitors exhibit potent growth-suppressive activity in pancreaticand breast cancer cells. Cancer Res. 2010 Mar 15;70(6):2445-54.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H32O6
Molecular Weight
464.55
CAS #
1226895-15-3
SMILES
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

Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1526 mL 10.7631 mL 21.5262 mL
5 mM 0.4305 mL 2.1526 mL 4.3052 mL
10 mM 0.2153 mL 1.0763 mL 2.1526 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • FLLL32

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


    FLLL32

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

  • FLLL32



    FLLL32

    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.

  • FLLL32

    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.

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