Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
mTOR Autophagy
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ln Vitro |
Compound 5e, mTOR inhibitor-8 (0.1-10 μM; 24 and 48 hours) inhibits A549 cell growth in a dose-dependent manner[1]. Autophagy is induced by mTOR inhibitor-8 in a mTOR-dependent way. Autophagy is induced in a time-dependent manner by mTOR inhibitor-8 (10 μM; 3-24 hours). There is an increase in LC3B-II levels[1]. Two crucial mTOR substrates, ribosomal protein S6 kinase (RPS6KB1) and eukaryotic translation initiation factor 4E-binding protein 1 (EIF4EBP1), are phosphorylated less when treated with mTOR inhibitor-8 (10 μM; 3–24 hours)[1].
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ln Vivo |
In vivo tumor development is significantly inhibited by mTOR inhibitor-8 (25 and 50 μM; 6 days) without negatively impacting normal chick chorioallantoic membrane angiogenesis.
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Cell Assay |
Cell Viability Assay[1]
Cell Types: A549 cells Tested Concentrations: 0.1, 1, 5, 10 μM Incubation Duration: 24 and 48 hrs (hours) Experimental Results: Suppressed the growth of A549 cells with an IC50 of 2.6±0.11 μM. Western Blot Analysis[1] Cell Types: A549 cells Tested Concentrations: 10 μM Incubation Duration: 3, 6, 12 and 24 hrs (hours) Experimental Results: The levels of phosphorylation of RPS6KB1 and EIF4EBP1 were Dramatically diminished after treatment. |
Animal Protocol |
Animal/Disease Models: Fertile chicken eggs (7-9 days old)[1]
Doses: 25 and 50 μM Route of Administration: 6 days Experimental Results: Significant xenograft tumor remission was observed in eggs compared with the DMSO-treated eggs. |
References |
[1]. ZhaoMin Lin, et al. Discovery of new fluorescent thiazole-pyrazoline derivatives as autophagy inducers by inhibiting mTOR activity in A549 human lung cancer cells. Cell Death Dis. 2020 Jul 20;11(7):551.
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Molecular Formula |
C24H19CLN4OS
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Molecular Weight |
446.95
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CAS # |
2489196-70-3
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SMILES |
C1C=C(OC)C=CC=1C1N(C2=NC(=CS2)C2=CC=NC=C2)N=C(C2C=CC(Cl)=CC=2)C1
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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 : 25 mg/mL (55.93 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.65 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (4.65 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 20.8 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2374 mL | 11.1869 mL | 22.3739 mL | |
5 mM | 0.4475 mL | 2.2374 mL | 4.4748 mL | |
10 mM | 0.2237 mL | 1.1187 mL | 2.2374 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.