AES-350
Based on 1 Customer Validation
AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.30%
- No. CAS: 847249-57-4
- Fòrmula: C18H20N2O3
- Peso molecular:312.36
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC6 24.4 nM (IC50) |
HDAC3 187 nM (IC50) |
HDAC11 245 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.58 μM
Compound: 51; AES-350
|
Inhibition of HDAC6 in human HeLa cells incubated for 15 mins by ELISA
Inhibition of HDAC6 in human HeLa cells incubated for 15 mins by ELISA
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[PMID: 31938464] |
| HeLa | IC50 |
2.53 μM
Compound: 51; AES-350
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
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[PMID: 31938464] |
| MDA-MB-231 | IC50 |
>25 μM
Compound: 51; AES-350
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
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[PMID: 31938464] |
| MDA-MB-468 | IC50 |
>50 μM
Compound: 51; AES-350
|
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
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[PMID: 31938464] |
| MOLM-13 | IC50 |
6 μM
Compound: 51; AES-350
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Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
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[PMID: 31938464] |
| MV4-11 | IC50 |
0.576 μM
Compound: 51; AES-350
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Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay
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[PMID: 31938464] |
| MV4-11 | IC50 |
0.58 μM
Compound: AES-350
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Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
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[PMID: 32615502] |
| MV4-11 | IC50 |
576 nM
Compound: AES-350
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Cytotoxicity against human MV4-11 cells
Cytotoxicity against human MV4-11 cells
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[PMID: 32615502] |
| Sf9 | IC50 |
>1 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 17 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
>1 μM
Compound: 51; AES-350
|
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
>1 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
>1 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
>1 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
>1 μM
Compound: 51; AES-350
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Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
0.0244 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
0.187 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
0.245 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC8 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC8 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
0.605 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
| Sf9 | IC50 |
0.899 μM
Compound: 51; AES-350
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Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
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[PMID: 31938464] |
In Vitro
In contrast, AES-350 has submicromolar activity (IC50=0.58±0.13 μM) against MV4-11 cells than to that of vorinostat (IC50=0.31±0.061 μM). AES-350 is more ligand efficient and exemplifies a large therapeutic index (IC50>30 μM in noncancerous MRC-9 cells). AES-350 is also shown to be effective in AML-3 (acute myeloid leukemia) cells (IC50=0.73 ± 0.12 μM)[1].AES-350 (0.25-4 μM; 18 hours) induces MV4-11 cells apoptosis in a dose-dependent manner. The late apoptosis ratios are 8.74%, 11.7%,16.08%, 30.97%, and 38.48%, respectively at 0.25 μM-4 μM[1].An ELISA is performed using HeLa cervical cancer cell lysates, and HeLa cells highly express HDAC6 and are sensitive to AES-350. Correspondingly, ELISA assays depicted a dose-dependent increase in HDAC6 inhibition (IC50=0.58±0.13 μM), Western blot analysis shows that AES-350 (0.1-10 μM) induces a dose-dependent increase in acetylated α-tubulin (Ac-α-tubulin), a substrate of HDAC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MV4-11 cells
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Concentration:0.25 μM; 0.5 μM; 1.00 μM; 2.00 μM; 4.00 μM
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Incubation Time:18 hours
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Result:Revealed a clear dosedependent increase in the percentage of cells entering late-stage apoptosis, similar to SAHA.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 847249-57-4
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Appearance Solid
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Peso molecular 312.36
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Fòrmula C18H20N2O3
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Color Off-white to light yellow
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SMILES
O=C(NO)C1=CC=C(NC(C2=CC=C(C(C)(C)C)C=C2)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (320.14 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (8.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Protocolo
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (544 KB)
- English - EN (544 KB)
- Français - FR (544 KB)
- Deutsch - DE (544 KB)
- Norwegian - NO (544 KB)
- Español - ES (544 KB)
- Swedish - SV (544 KB)
- Italian - IT (544 KB)
- Korean - KR (544 KB)
- Portuguese - PT (544 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2014 mL | 16.0072 mL | 32.0143 mL | 80.0359 mL |
| 5 mM | 0.6403 mL | 3.2014 mL | 6.4029 mL | 16.0072 mL | |
| 10 mM | 0.3201 mL | 1.6007 mL | 3.2014 mL | 8.0036 mL | |
| 15 mM | 0.2134 mL | 1.0671 mL | 2.1343 mL | 5.3357 mL | |
| 20 mM | 0.1601 mL | 0.8004 mL | 1.6007 mL | 4.0018 mL | |
| 25 mM | 0.1281 mL | 0.6403 mL | 1.2806 mL | 3.2014 mL | |
| 30 mM | 0.1067 mL | 0.5336 mL | 1.0671 mL | 2.6679 mL | |
| 40 mM | 0.0800 mL | 0.4002 mL | 0.8004 mL | 2.0009 mL | |
| 50 mM | 0.0640 mL | 0.3201 mL | 0.6403 mL | 1.6007 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3339 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0004 mL | |
| 100 mM | 0.0320 mL | 0.1601 mL | 0.3201 mL | 0.8004 mL |
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