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| 100mg |
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Purity: ≥98%
PD: MHY1485 is a novel, potent and cell-permeable activator of mTOR (mammalian target of rapamycin) activator and autophagy inhibitor that prevents the fusion of autophagosomes and lysosomes.
| Targets |
mTORC1; mTORC2; mTORC1; Autophagy
|
|---|---|
| ln Vitro |
MHY1485 (10 μM; 4 hours) demonstrates that GCDC-induced autophagic activity is inhibited by upregulating p-mTOR expression and downregulating LC3 and p62 expression in HCC cells[1]. MHY1485 (5 μM; 6 hours) increases the LC3I/LC3I ratio in a dose- and time-dependent manner because it ostensibly inhibits LC3II degradation in rat liver Ac2F cells[2]. MHY1485 (0.5-2 μM; 6 hours) increases the phosphorylation of mTOR at ser2448 and upregulates the level of phosphorylation of 4E-BP1 in a dose-dependently manner in Ac2F cells[2].
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| ln Vivo |
MHY1485 (intraperitoneal injection; 10 mg/kg, 2 days) inhibits the follicle-stimulating hormone (FSH)-induced autophagy signaling. While p-mTOR and p-S6K1 expression levels rise, the expression of LC3 does not differ noticeably from that of the control group[3].
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| Enzyme Assay |
Western blot analysis is used to find changes in the levels of total protein and phosphorylated forms of mTOR and 4E-BP1, which are indicators of mTOR activity. MHY1485 in varying concentrations is applied to Ac2F cells for 1 hour while rapamycin (5 mM) is used as a positive control. Cells are harvested after being washed in cold PBS. RIPA buffer, which contains 50 mM Tris-HCl, 150 mM NaCl, 1% NP-40, 1 mM DTT, 0.1 mM NaF, 1 mM PMSF, and 1 mg/mL each of pepstatin, leupeptin, and aprotinin, is used to make cell lysates. Bicarbonate of acid (BCA) analysis is used to measure protein concentration. SDS-PAGE (sodium dodecyl sulfate-polyacrylamide gel electrophoresis) gels are used to separate proteins in exactly the same amounts. The gels are then electroblotted for 2 hours at 60-75 V to transfer them onto a polyvinylidene difluoride membrane. The membranes are then incubated with primary antibodies after being blocked in a solution of 5% nonfat milk in Tris-buffered saline (TBS) with 0.5% Tween-20. For determining molecular weight, pre-stained protein markers are employed.
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| Cell Assay |
Cells were exposed to the drug at the indicated concentration for 24 hours.
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| Animal Protocol |
4-week-old female ICR mice[3]
10 mg/kg, 2 days Intraperitoneal injection |
| References |
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| Molecular Formula |
C17H21N7O4
|
|---|---|
| Molecular Weight |
387.39314
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| Exact Mass |
387.165
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| Elemental Analysis |
C, 52.71; H, 5.46; N, 25.31; O, 16.52
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| CAS # |
326914-06-1
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| Related CAS # |
326914-06-1
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| PubChem CID |
2834965
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
643.3±65.0 °C at 760 mmHg
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| Melting Point |
259°C
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| Flash Point |
342.9±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.652
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| LogP |
-0.98
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
|
| Heavy Atom Count |
28
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| Complexity |
476
|
| Defined Atom Stereocenter Count |
0
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| SMILES |
O=[N+](C1=CC=C(NC2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=C1)[O-]
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| InChi Key |
MSSXBKQZZINCRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21N7O4/c25-24(26)14-3-1-13(2-4-14)18-15-19-16(22-5-9-27-10-6-22)21-17(20-15)23-7-11-28-12-8-23/h1-4H,5-12H2,(H,18,19,20,21)
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| Chemical Name |
4,6-dimorpholino-N-(4-nitrophenyl)-1,3,5-triazin-2-amine
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| Synonyms |
MHY-1485; MHY 1485; MHY1485
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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: ~33 mg/mL (85.2 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.77 mg/mL (1.99 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 7.7 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: ≥ 0.77 mg/mL (1.99 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 7.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5 mg/mL (12.91 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 1 mg/mL (2.58 mM) in 20% HP-β-CD in Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5814 mL | 12.9069 mL | 25.8138 mL | |
| 5 mM | 0.5163 mL | 2.5814 mL | 5.1628 mL | |
| 10 mM | 0.2581 mL | 1.2907 mL | 2.5814 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.
Failure of the increase of autophagic flux. PLoS One. 2012; 7(8): e43418. |
Inhibition of starvation-induced autophagic flux by MHY1485. |
Activation of mTOR by MHY1485. |
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