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50mg | ||
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Other Sizes |
Targets |
Kd: 10.2 nM (leukemia inhibitory factor receptor)[1]
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ln Vitro |
In a dose-dependent way, EC359 (0-100 nM; 3 days) treatment decreases cell viability in BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells[1]. Caspasese-3/7 activity and Annexin V-positive cells in MDA-MB-231 and BT-549 cells are markedly increased by EC359 (20 nM, 25 nM; 72 hours). TNBC cells undergo apoptosis when exposed to EC359, which inhibits invasion significantly[1]. Many known STAT3 target genes, including STAT1, TGFB1, JUNB, MCL-1, and others, have markedly decreased expression when exposed to EC359 (100 nM; 12 hours; BT549 cells)[1]. Significantly lessening STAT3 activation by LIF, OSM, and CNTF, EC359 (100 nM; 1 hour; MDA-MB-231 and BT-549 cells) therapy also does so. AKT, mTOR, S6, and ERK1/2 phosphorylation in MDA-MB231 and BT-549 cells is significantly reduced by EC359 therapy. Phosphorylation of proapoptotic p38MAPK in BT549 cells is likewise increased by EC359 treatment[1].
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ln Vivo |
Treatment with EC359 (5 mg/kg; subcutaneous injection; three days a week; for 25 days; female athymic nude mice) dramatically slowed the growth of the tumor. The mice's body weights in the EC359-treated groups do not vary, indicating that EC359 is not very toxic[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: BT-549, SUM-159, MDA-MB-231, MDA-MB-468, and HCC1806 cells Tested Concentrations: 0 nM, 1.5 nM, 12.5 nM, 25 nM, 50 nM, 100 nM Incubation Duration: 3 days Experimental Results: decreased cell viability in a dose-dependent manner. Apoptosis Analysis[1] Cell Types: MDA-MB-231 and BT-549 cells Tested Concentrations: 20 nM, 25 nM Incubation Duration: 72 hrs (hours) Experimental Results: Promoted apoptosis of TNBC cells. RT-PCR[1] Cell Types: BT549 cells Tested Concentrations: 100 nM Incubation Duration: 12 hrs (hours) Experimental Results: decreased the expression of several known STAT3 target genes. Western Blot Analysis [1] Cell Types: MDA-MB-231 and BT-549 cells Tested Concentrations: 100 nM Incubation Duration: 1 hour Experimental Results: Substantially decreased the LIF activation of STAT3, decreased the STAT3 activation by OSM and CNTF, diminished the phosphorylation of AKT, mTOR, S6, and ERK1/2 in both BT-549 and MDA-MB-231 cells and increased the phosphorylation of proapoptotic p38MAPK in BT549 cells. |
Animal Protocol |
Animal/Disease Models: 8weeks old female athymic nude mice with MDA-MB-231 cells[1]
Doses: 5 mg/kg Route of Administration: subcutaneous (sc)injection; 3 days per week; for 25 days Experimental Results: Dramatically diminished the tumor progression. |
References |
[1]. Viswanadhapalli S, et al. EC359: A First-in-Class Small-Molecule Inhibitor for Targeting Oncogenic LIFR Signaling in Triple-Negative Breast Cancer. Mol Cancer Ther. 2019 Aug;18(8):1341-1354.
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Molecular Formula |
C36H38F2O2
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Molecular Weight |
540.68
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CAS # |
2012591-09-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC(C#C)([C@]1(CC[C@@H]2[C@H]3CCC4=CC(CCC4=C3[C@H](C3C=CC(C4C(C)=CC(C)=CC=4C)=CC=3)C[C@]21C)=O)O)F
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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 |
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) |
DMSO : 125 mg/mL (231.19 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.85 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 20.8 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: ≥ 2.08 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8495 mL | 9.2476 mL | 18.4952 mL | |
5 mM | 0.3699 mL | 1.8495 mL | 3.6990 mL | |
10 mM | 0.1850 mL | 0.9248 mL | 1.8495 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.