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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
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.
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].
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ln Vivo |
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Animal Protocol |
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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. |
Molecular Formula |
C28H32O6
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Molecular Weight |
464.55
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CAS # |
1226895-15-3
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Related CAS # |
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
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.
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. td> |
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. td> |
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. td> |