ARV-771
Based on 29 publication(s) in Google Scholar
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
(Pink: BET ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.82%
- No. CAS: 1949837-12-0
- Fòrmula: C49H60ClN9O7S2
- Peso molecular:986.64
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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 Citing Use of MedChemExpress (MCE) ARV-771
More- Cell. 2024 Jan 4;187(1):166-183.e25. [Abstract]
- Mol Cell. 2024 Apr 4;84(7):1304-1320.e16. [Abstract]
- Mol Cell. 2021 Apr 1;81(7):1411-1424.e7. [Abstract]
- Mol Cell. 2019 Aug 22;75(4):849-858.e8. [Abstract]
- Nat Commun. 2024 Jul 2;15(1):5379. [Abstract]
- Nat Chem Biol. 2023 Mar;19(3):323-333. [Abstract]
- Nat Chem Biol. 2021 Nov;17(11):1157-1167. [Abstract]
- Nat Chem Biol. 2020 Nov;16(11):1199-1207. [Abstract]
- J Adv Res. 2025 Jul 4:S2090-1232(25)00504-1. [Abstract]
- J Control Release. 2021 Feb 10;330:1244-1249. [Abstract]
- Clin Cancer Res. 2019 Jun 1;25(11):3404-3416. [Abstract]
- Nat Struct Mol Biol. 2024 Feb;31(2):323-335. [Abstract]
- Cell Rep. 2021 Jan 5;34(1):108532. [Abstract]
- J Med Chem. 2020 Jul 9;63(13):7186-7210. [Abstract]
- JCI Insight. 2022 May 23;7(10):e151353. [Abstract]
- Biochem Pharmacol. 2025 Jul 12:241:117159. [Abstract]
- Philos Trans R Soc Lond B Biol Sci. 2025 Jan 23;380(1918):20230342. [Abstract]
- Bioorg Chem. 2022 Feb:119:105505. [Abstract]
- Structure. 2024 Dec 5;32(12):2352-2363.e8. [Abstract]
- Drug Metab Dispos. 2025 May;53(5):100066. [Abstract]
- ACS Chem Biol. 2019 Oct 18;14(10):2215-2223. [Abstract]
- Curr Issues Mol Biol. 2026 Jan 10;48(1):71. [Abstract]
- bioRxiv. 2025 April 16.
- bioRxiv. 2023 Apr 21.
- Patent. US20230124700A1.
- Patent. US20220288051A1.
- Methods Mol Biol. 2021:2365:151-171. [Abstract]
- Research Square Preprint. 2020 Dec.
- Martin-Luther-Universität Halle-Wittenberg. 2020 Dec.
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WB
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Others
Ver todos los productos específicos de isoformas PROTACs
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Actividad biológica
|
BRD2(1) 34 nM (Kd) |
BRD2(2) 4.7 nM (Kd) |
BRD3(1) 8.3 nM (Kd) |
BRD3(2) 7.6 nM (Kd) |
BRD4(1) 9.6 nM (Kd) |
BRD4(2) 7.6 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.64 μM
Compound: ARV-771
|
Antiproliferative activity against human normal (non-senescent) A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human normal (non-senescent) A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38635879] |
| A549 | IC50 |
603 nM
Compound: ARV-771
|
Antiproliferative activity against human senescent A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human senescent A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38635879] |
| CWR22R | EC50 |
44 nM
Compound: 22; ARV-771
|
Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-Glo cell viability assay
Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-Glo cell viability assay
|
[PMID: 34881891] |
| EOL1 | IC50 |
1.5 nM
Compound: ARV-771; 34
|
Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth
Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth
|
[PMID: 36202064] |
| HeLa | IC50 |
183 nM
Compound: 35; ARV-771
|
Antiproliferative activity against human HeLa cells
Antiproliferative activity against human HeLa cells
|
[PMID: 35763424] |
| HeLa | IC50 |
183 nM
Compound: ARV-771
|
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38160619] |
| HFF-1 | IC50 |
1.1 μM
Compound: ARV-771
|
Antiproliferative activity against human HFF-1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HFF-1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38160619] |
| HK-2 | IC50 |
0.16 μM
Compound: ARV-771
|
Antiproliferative activity against human HK-2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HK-2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38160619] |
| HL-60 | IC50 |
1.5 nM
Compound: ARV-771; 34
|
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth
|
[PMID: 36202064] |
| MCF7 | IC50 |
120.4 nM
Compound: ARV-771
|
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 38160619] |
| MOLM-13 | IC50 |
7.45 nM
Compound: ARV-771
|
Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay
Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay
|
[PMID: 30019901] |
| MV4-11 | IC50 |
0.43 nM
Compound: ARV-771
|
Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay
Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay
|
[PMID: 30019901] |
| NIH3T3 | IC50 |
0.21 μM
Compound: ARV-771
|
Antiproliferative activity against mouse 3T3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse 3T3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38160619] |
| OVCAR-8 | IC50 |
215 nM
Compound: ARV-771
|
Antiproliferative activity against human OVCAR-8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human OVCAR-8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38160619] |
| RS4-11 | IC50 |
2.4 nM
Compound: ARV-771
|
Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay
Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay
|
[PMID: 30019901] |
| T47D | IC50 |
13 nM
Compound: ARV-771
|
Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
[PMID: 38160619] |
| VCaP | DC50 |
<5 nM
Compound: 101; ARV-771
|
Degradation of BRD4 in human VCaP cells after 16 hrs by Western blot analysis
Degradation of BRD4 in human VCaP cells after 16 hrs by Western blot analysis
|
[PMID: 30542529] |
| VCaP | DC50 |
<5 nM
Compound: 47; ARV-771
|
Protac activity against VHL/BRD3 in human VCaP cells assessed as induction of BRD3 protein degradation by reverse phase protein array analysis
Protac activity against VHL/BRD3 in human VCaP cells assessed as induction of BRD3 protein degradation by reverse phase protein array analysis
|
[PMID: 31035238] |
| Z-138 | IC50 |
142 nM
Compound: 101; ARV-771
|
Induction of apoptosis in human ibrutinib-resistant Z138 cells after 48 hrs by Annexin-V/propidium iodide staining based assay
Induction of apoptosis in human ibrutinib-resistant Z138 cells after 48 hrs by Annexin-V/propidium iodide staining based assay
|
[PMID: 30542529] |
ARV-771, a small-molecule pan-BET PROTAC degrader, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 potently degrades BRD2/3/4 in 22Rv1 cells with a DC50 less than 5 nM. c-MYC protein is a downstream effector of BET proteins. Treatment with ARV-771 results in depletion of c-MYC with an IC50 of less than 1 nM. ARV-771 shows strong antiproliferative effect on 22Rv1, VCaP, and LnCaP95 cell lines. ARV-771 treatment has a pronounced effect on cell morphology consistent with apoptosis. FL-AR and AR-V7 mRNA are down-regulated upon treatment with 10 nM ARV-771 in VCaP cells. ARV-771 has an antiandrogenic effect on a number of AR-regulated genes in VCaP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1949837-12-0
-
Appearance Solid
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Peso molecular 986.64
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Fòrmula C49H60ClN9O7S2
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Color White to light yellow
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SMILES
CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@H](C4=NN=C(N42)C)CC(NCCOCCCOCC(N[C@H](C(N5C[C@@H](C[C@H]5C(N[C@@H](C)C6=CC=C(C=C6)C7=C(C)N=CS7)=O)O)=O)C(C)(C)C)=O)=O
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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 (29)
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Journal Impact Factor
-
Most Recent
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Cell
A TCF4-dependent gene regulatory network confers resistance to immunotherapy in melanoma. [Abstract]2024 Jan 4;187(1):166-183.e25. PMID: 38181739 -
Mol Cell
Cullin-RING ligases employ geometrically optimized catalytic partners for substrate targeting. [Abstract]2024 Apr 4;84(7):1304-1320.e16. PMID: 38382526
ARV-771 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2024 Apr 4;84(7):1304-1320.e16. [Abstract]
ARV-771 (500 nM; 6 h). Representative western blots comparing protein levels upon treatment with PROTACs in control or UBE2R1/UBE2R2 DKO HEK293T cells. Notice that ectopic expression of either UBE2R1 (lanes 9-12) or UBE2R2 (lanes 13-16) completely restored BRD4 degradation with ARV-771.
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Mol Cell
TRIP12 promotes small-molecule-induced degradation through K29/K48-branched ubiquitin chains. [Abstract]2021 Apr 1;81(7):1411-1424.e7. PMID: 33567268 -
Mol Cell
Plasticity of the Cullin-RING Ligase Repertoire Shapes Sensitivity to Ligand-Induced Protein Degradation. [Abstract]2019 Aug 22;75(4):849-858.e8. PMID: 31442425 -
Nat Commun
2024 Jul 2;15(1):5379. PMID: 38956052 -
Nat Chem Biol
2023 Mar;19(3):323-333. PMID: 36329119
ARV-771 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Mar;19(3):323-333. [Abstract]
Heatmap depicting mean log2 fold-enrichment of VHL mutations normalized to maximum log2 fold-changes vs. DMSO across ARV-771 (500 nM; 7 days) treated for 7 days. n = 2 independent measurements.
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Nat Chem Biol
2021 Nov;17(11):1157-1167. PMID: 34675414 -
Nat Chem Biol
2020 Nov;16(11):1199-1207. PMID: 32747809 -
J Adv Res
2025 Jul 4:S2090-1232(25)00504-1. PMID: 40617410 -
J Control Release
Enhanced protein degradation by intracellular delivery of pre-fused PROTACs using lipid-like nanoparticles. [Abstract]2021 Feb 10;330:1244-1249. PMID: 33234362 -
Clin Cancer Res
2019 Jun 1;25(11):3404-3416. PMID: 30796033 -
Nat Struct Mol Biol
2024 Feb;31(2):323-335. PMID: 38177676 -
Cell Rep
Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins. [Abstract]2021 Jan 5;34(1):108532. PMID: 33406420 -
J Med Chem
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. [Abstract]2020 Jul 9;63(13):7186-7210. PMID: 32453591 -
JCI Insight
2022 May 23;7(10):e151353. PMID: 35439169 -
Biochem Pharmacol
Discovery of a potent BRD4 PROTAC and evaluation of its bioactivity in breast cancer cell lines. [Abstract]2025 Jul 12:241:117159. PMID: 40659131 -
Philos Trans R Soc Lond B Biol Sci
2025 Jan 23;380(1918):20230342. PMID: 39842482 -
Bioorg Chem
2022 Feb:119:105505. PMID: 34838332 -
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062 -
Drug Metab Dispos
Applications of contemporary tools to measure plasma protein binding of targeted protein degraders. [Abstract]2025 May;53(5):100066. PMID: 40286535 -
ACS Chem Biol
Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway. [Abstract]2019 Oct 18;14(10):2215-2223. PMID: 31553577 -
Curr Issues Mol Biol
Role of the Super-Enhancer Component Bromodomain Protein 4 in the Radiation Response of Human Head and Neck Squamous Cell Carcinoma Cells. [Abstract]2026 Jan 10;48(1):71. PMID: 41614901 -
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Methods Mol Biol
Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells. [Abstract]2021:2365:151-171. PMID: 34432243 -
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Solvente y solubilidad
DMSO : ≥ 50 mg/mL (50.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 (2.53 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 (2.53 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.
Please enter the basic information of animal experiments:
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-
-
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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.
Protocolo
ARV-771 is dissolved in DMSO. 22Rv1 cells (5,000 cells per well) are dosed with ARV-771 serially diluted 1:3 for a 10-point dose curve for 72 h. CellTiter-Glo Luminescent Cell Viability Assay is added, and the plate is read on a luminometer. Data are analyzed and plotted using GraphPad Prism software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Mice bearing tumors are treated with ARV-771 (5, 10, 30, 50 mg/kg) for up to 3 wk, depending on the experiment. Mice are sacrificed 8 h after the final dose. Plasma and tissues are harvested and flash frozen for further analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 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 | 1.0135 mL | 5.0677 mL | 10.1354 mL | 25.3385 mL |
| 5 mM | 0.2027 mL | 1.0135 mL | 2.0271 mL | 5.0677 mL | |
| 10 mM | 0.1014 mL | 0.5068 mL | 1.0135 mL | 2.5339 mL | |
| 15 mM | 0.0676 mL | 0.3378 mL | 0.6757 mL | 1.6892 mL | |
| 20 mM | 0.0507 mL | 0.2534 mL | 0.5068 mL | 1.2669 mL | |
| 25 mM | 0.0405 mL | 0.2027 mL | 0.4054 mL | 1.0135 mL | |
| 30 mM | 0.0338 mL | 0.1689 mL | 0.3378 mL | 0.8446 mL | |
| 40 mM | 0.0253 mL | 0.1267 mL | 0.2534 mL | 0.6335 mL | |
| 50 mM | 0.0203 mL | 0.1014 mL | 0.2027 mL | 0.5068 mL |