HDACs/mTOR Inhibitor 1
Based on 1 publication(s) in Google Scholar
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies.
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- Pureza : 98.10%
- No. CAS: 2271413-06-8
- Fòrmula: C28H38N8O5
- Peso molecular:566.65
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) HDACs/mTOR Inhibitor 1
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC1 0.19 nM (IC50) |
HDAC6 1.8 nM (IC50) |
mTOR 1.2 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
17.2 nM
Compound: 12l
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Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 30629434] |
| MM1.S | IC50 |
7.3 nM
Compound: 12l
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Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay
Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay
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[PMID: 30629434] |
| MV4-11 | IC50 |
4.05 nM
Compound: 12l
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Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
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[PMID: 30629434] |
| OCI-AML2 | IC50 |
9.01 nM
Compound: 12l
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Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay
Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay
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[PMID: 30629434] |
| OCI-AML-3 | IC50 |
9.98 nM
Compound: 12l
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Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay
Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay
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[PMID: 30629434] |
| Raji | IC50 |
1.9 nM
Compound: 12l
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Antiproliferative activity against human Raji cells after 72 hrs by MTT assay
Antiproliferative activity against human Raji cells after 72 hrs by MTT assay
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[PMID: 30629434] |
| Sf9 | IC50 |
0.58 nM
Compound: 12l
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Inhibition of recombinant full length N-terminal FLAG-tagged human HDAC10 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
Inhibition of recombinant full length N-terminal FLAG-tagged human HDAC10 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
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[PMID: 30629434] |
| Sf9 | IC50 |
>1000 nM
Compound: 12l
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Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay
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[PMID: 30629434] |
In Vitro
HDACs/mTOR Inhibitor 1 (Compound 12l) inhibits leukemia cells proliferation with IC50s of 4.05, 9.01, 9.98 μM for MV4-11, OCI-AML2, OCI-AML3 cells[1].
HDACs/mTOR Inhibitor 1 (0-10 μM, 6 h or 24 h) downregulates p-ERK and increases Ac-H3 in MV4-11 cells[1].
HDACs/mTOR Inhibitor 1 (10 to 1000 nM, 48 h) reduces S-phase cells and increases the percentage of cells in G0/G1 phase in MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:6 h or 24 h
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Result:Downregulated p-ERK (24 h) and increased of the Ac-H3 (6 h) in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 xenograft NOD/SCID mouse model[1]
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Dosage:10 mg/kg
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Administration:Intravenous injection (i.v.), every two days (Q2D)×6
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Result:The TGI (tumor growth inhibitory rate) was 53.1%.
Chemical Information
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No. CAS 2271413-06-8
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Appearance Solid
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Peso molecular 566.65
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Fòrmula C28H38N8O5
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Color White to off-white
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SMILES
O=C(NO)CCCCCCN1C2=NC(C3=CC=C(NC(N4C[C@@H](C)OCC4)=O)C=C3)=NC(N5CCOCC5)=C2C=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Pharmacol
CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]2020 Nov 11:11:580407. PMID: 33343350
Solvente y solubilidad
In Vitro:
DMSO : 32.5 mg/mL (57.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (3.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7648 mL | 8.8238 mL | 17.6476 mL | 44.1189 mL |
| 5 mM | 0.3530 mL | 1.7648 mL | 3.5295 mL | 8.8238 mL | |
| 10 mM | 0.1765 mL | 0.8824 mL | 1.7648 mL | 4.4119 mL | |
| 15 mM | 0.1177 mL | 0.5883 mL | 1.1765 mL | 2.9413 mL | |
| 20 mM | 0.0882 mL | 0.4412 mL | 0.8824 mL | 2.2059 mL | |
| 25 mM | 0.0706 mL | 0.3530 mL | 0.7059 mL | 1.7648 mL | |
| 30 mM | 0.0588 mL | 0.2941 mL | 0.5883 mL | 1.4706 mL | |
| 40 mM | 0.0441 mL | 0.2206 mL | 0.4412 mL | 1.1030 mL | |
| 50 mM | 0.0353 mL | 0.1765 mL | 0.3530 mL | 0.8824 mL |
HDACs/mTOR Inhibitor 1 Related Classifications
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