Prexasertib dimesylate
Based on 36 publication(s) in Google Scholar
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
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- Reinheit: 98.90%
- CAS. Nr.: 1234015-58-7
- Formel: C20H27N7O8S2
- Molecular Weight:557.60
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Prexasertib dimesylate
More- Nat Commun. 2019 Aug 2;10(1):3485. [Abstract]
- Sci Adv. 2026 Jun 26;12(26):eadz3351. [Abstract]
- Cancer Lett. 2026 Feb 4;642:218300.
- Cancer Lett. 2026 Apr 1:642:218300. [Abstract]
- Cell Death Dis. 2026 Mar 26;17(1):375. [Abstract]
- Thorax. 2022 Mar;77(3):247-258. [Abstract]
- Oncogene. 2026 Jun 10. [Abstract]
- Oncogene. 2022 Nov;41(46):5020-5031. [Abstract]
- Cell Rep. 2025 Apr 17;44(5):115605. [Abstract]
- Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
- Oncogenesis. 2025 Mar 1;14(1):4. [Abstract]
- Cell Biol Toxicol. 2023 Jun;39(3):795-811. [Abstract]
- Mol Cancer Ther. 2025 Jun 4;24(6):920-930. [Abstract]
- Cells. 2024 Apr 19;13(8):710. [Abstract]
- Int Immunopharmacol. 2025 Dec 31:171:116126. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- Int Immunopharmacol. 2025 Mar 26:150:114278. [Abstract]
- Mol Cancer Res. 2019 Oct;17(10):2102-2114. [Abstract]
- Cancers (Basel). 2021 Aug 20;13(16):4200. [Abstract]
- Cancers. 2020 Aug 26;12(9):2426. [Abstract]
- Cancers. 2020 Jun 29;12(7):1726. [Abstract]
- Neurooncol Adv. 2024 Nov 19;6(1):vdae187. [Abstract]
- Sci Rep. 2025 Nov 27. [Abstract]
- Sci Rep. 2021 Feb 4;11(1):3176. [Abstract]
- Cell Signal. 2025 Jul:131:111709. [Abstract]
- bioRxiv. 2025 Dec 25.
- bioRxiv. 2025 April 17.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Research Square Preprint. 2024 Nov 06.
- Universität Hamburg. 2022 Aug.
- Utrecht University. 2023 Feb.
- bioRxiv. January 04, 2022.
- Patent. US20210353605A1.
- bioRxiv. September 10, 2021.
- Research Square Preprint. 2021 May.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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WB
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Flow Cytometry
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In Vivo Efficacy Study
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Apoptosis Analysis
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RT-PCR
Biologische Aktivität
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Chk1 0.9 nM (Ki) |
Chk1 <1 nM (IC50) |
Chk2 8 nM (IC50) |
Prexasertib dimesylate (LY2606368 dimesylate) inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). Prexasertib dimesylate requires CDC25A and CDK2 to cause DNA damage[1].
Prexasertib dimesylate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1].
Prexasertib dimesylate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1].
Prexasertib dimesylate (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells[1].
Prexasertib dimesylate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib dimesylate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:33, 100 nM
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Incubation Time:For 7 hours
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Result:Had an IC50 of 37 nM and resulted in the G2-M population received DNA damage during S-phase but continued to progress through the cell cycle into an early mitosis.
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Cell Line:HT-29 cells
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Concentration:8, 16, 31, 63, 125, 250 nM
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Incubation Time:Pre-treated for 15 minutes
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Result:Inhibited CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) (IC50 of less than 31 nM) in HT-29 cells.
Prexasertib dimesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
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Dosage:1, 3.3, or 10 mg/kg
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Administration:SC; twice daily for 3 days, rest 4 days; for three cycles
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Result:Caused statistically significant tumor growth inhibition (up to 72.3%).
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Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
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Dosage:15 mg/kg (Pharmacokinetic Analysis)
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Administration:SC (200 μL)
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Result:CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures.
Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.
Chemical Information
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CAS. Nr. 1234015-58-7
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Appearance Solid
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Molecular Weight 557.60
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Formel C20H27N7O8S2
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Color Light yellow to yellow
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SMILES
N#CC1=NC=C(NC2=NNC(C3=C(OC)C=CC=C3OCCCN)=C2)N=C1.CS(=O)(O)=O.CS(=O)(O)=O
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Synonyms
LY2606368 dimesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (36)
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Journal Impact Factor
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Most Recent
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Nat Commun
MYC paralog-dependent apoptotic priming orchestrates a spectrum of vulnerabilities in small cell lung cancer. [Abstract]2019 Aug 2;10(1):3485. PMID: 31375684
Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 2;10(1):3485. [Abstract]
Viability of mock control and Myc-activated CRISPRa cells upon treatment with 40 nM prexasertib for 96 h (n = 3).
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Sci Adv
Patient-derived organoids across cancers reveal conserved tumor heterogeneity and actionable therapeutic vulnerabilities. [Abstract]2026 Jun 26;12(26):eadz3351. PMID: 42361179 -
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Cancer Lett
2026 Apr 1:642:218300. PMID: 41651400 -
Cell Death Dis
2026 Mar 26;17(1):375. PMID: 41888112 -
Thorax
Potential for inhibition of checkpoint kinases 1/2 in pulmonary fibrosis and secondary pulmonary hypertension. [Abstract]2022 Mar;77(3):247-258. PMID: 34226205 -
Oncogene
DNA replication stress and translational repression converge to drive CDK1- and caspase-dependent apoptosis in Ewing sarcoma. [Abstract]2026 Jun 10. PMID: 42270776 -
Oncogene
Distinct roles of treatment schemes and BRCA2 on the restoration of homologous recombination DNA repair and PARP inhibitor resistance in ovarian cancer. [Abstract]2022 Nov;41(46):5020-5031. PMID: 36224341 -
Cell Rep
The low-dose CHK1 inhibitor prexasertib triggers VDAC1 dephosphorylation to activate mtDNA-STING signaling and synergize immunotherapy. [Abstract]2025 Apr 17;44(5):115605. PMID: 40249707 -
Br J Cancer
Interferon regulatory factor 1 (IRF-1) downregulates Checkpoint kinase 1 (CHK1) through miR-195 to upregulate apoptosis and PD-L1 expression in Hepatocellular carcinoma (HCC) cells. [Abstract]2021 Jul;125(1):101-111. PMID: 33772151
Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Full length and cleaved PARP protein expressions are determined by western blot in Hepa1-6 cells and Huh-7 cells induced by prexasertib with dose of 1 µM and 5 nM for 24 h, respectively.
Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Representative image of FACS analysis of late apoptotic Hepa1-6 cell rate treated by DMSO or prexasertib with dose of 1 µM for 24 h are shown.
Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Tumour growth curves (Mean ± SEM) of murine HCC model treated by vehicle (n = 8) or prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8) are shown.
Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days). Representative images of TUNEL assay for cellular apoptosis (green staining) in tumours are shown.
Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8). PD-L1 mRNA expression is determined by qPCR in tumours treated by prexasertib or vehicle.
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Oncogenesis
STAG2 expression imparts distinct therapeutic vulnerabilities in muscle-invasive bladder cancer cells. [Abstract]2025 Mar 1;14(1):4. PMID: 40025053 -
Cell Biol Toxicol
Exploring the ATR-CHK1 pathway in the response of doxorubicin-induced DNA damages in acute lymphoblastic leukemia cells. [Abstract]2023 Jun;39(3):795-811. PMID: 34519926 -
Mol Cancer Ther
Targeting Monounsaturated Fatty Acid Metabolism for Radiosensitization of KRAS Mutant 3D Lung Cancer Models. [Abstract]2025 Jun 4;24(6):920-930. PMID: 39834305 -
Cells
Genomic Engineering of Oral Keratinocytes to Establish In Vitro Oral Potentially Malignant Disease Models as a Platform for Treatment Investigation. [Abstract]2024 Apr 19;13(8):710. PMID: 38667326 -
Int Immunopharmacol
CHK1 inhibition by prexasertib sensitizes cisplatin-resistant malignant tumor cells via checkpoint abrogation and STAT1-driven PD-L1 upregulation. [Abstract]2025 Dec 31:171:116126. PMID: 41477994 -
Eur J Pharmacol
VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]2025 Sep 15:1003:177942. PMID: 40651787 -
Int Immunopharmacol
Prexasertib exerts a synergistic effect on the antitumor activity of Lenvatinib through ALOX15-mediated ferroptosis in hepatocellular carcinoma. [Abstract]2025 Mar 26:150:114278. PMID: 39954659 -
Mol Cancer Res
Pharmacologic Ascorbate Primes Pancreatic Cancer Cells for Death by Rewiring Cellular Energetics and Inducing DNA Damage. [Abstract]2019 Oct;17(10):2102-2114. PMID: 31337671 -
Cancers (Basel)
Novel Insights into the Molecular Regulation of Ribonucleotide Reductase in Adrenocortical Carcinoma Treatment. [Abstract]2021 Aug 20;13(16):4200. PMID: 34439352 -
Cancers
Systems Biology Approach Identifies Prognostic Signatures of Poor Overall Survival and Guides the Prioritization of Novel BET-CHK1 Combination Therapy for Osteosarcoma. [Abstract]2020 Aug 26;12(9):2426. PMID: 32859084 -
Cancers
Cotargeting CHK1 and PI3K Synergistically Suppresses Tumor Growth of Oral Cavity Squamous Cell Carcinoma in Patient-Derived Xenografts. [Abstract]2020 Jun 29;12(7):1726. PMID: 32610557 -
Neurooncol Adv
Ion channel modulator DPI-201-106 significantly enhances antitumor activity of DNA damage response inhibitors in glioblastoma. [Abstract]2024 Nov 19;6(1):vdae187. PMID: 39659830 -
Sci Rep
Synergistic inhibition of CHK1 and MUS81 to combat replication stress resistance in high-risk neuroblastoma. [Abstract]2025 Nov 27. PMID: 41310217 -
Sci Rep
The mitotic checkpoint is a targetable vulnerability of carboplatin-resistant triple negative breast cancers. [Abstract]2021 Feb 4;11(1):3176. PMID: 33542435 -
Cell Signal
2025 Jul:131:111709. PMID: 40037423 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (179.34 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 3.5 mg/mL (6.28 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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: ≥ 3.5 mg/mL (6.28 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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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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 (stored under nitrogen)
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.
Reinheit & Dokumentation
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Data Sheet (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-1 [Content Brief]
[2]. Yin Y, et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483. [Content Brief]
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 (stored under nitrogen). 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 | 1.7934 mL | 8.9670 mL | 17.9340 mL | 44.8350 mL |
| 5 mM | 0.3587 mL | 1.7934 mL | 3.5868 mL | 8.9670 mL | |
| 10 mM | 0.1793 mL | 0.8967 mL | 1.7934 mL | 4.4835 mL | |
| 15 mM | 0.1196 mL | 0.5978 mL | 1.1956 mL | 2.9890 mL | |
| 20 mM | 0.0897 mL | 0.4484 mL | 0.8967 mL | 2.2418 mL | |
| 25 mM | 0.0717 mL | 0.3587 mL | 0.7174 mL | 1.7934 mL | |
| 30 mM | 0.0598 mL | 0.2989 mL | 0.5978 mL | 1.4945 mL | |
| 40 mM | 0.0448 mL | 0.2242 mL | 0.4484 mL | 1.1209 mL | |
| 50 mM | 0.0359 mL | 0.1793 mL | 0.3587 mL | 0.8967 mL | |
| 60 mM | 0.0299 mL | 0.1495 mL | 0.2989 mL | 0.7473 mL | |
| 80 mM | 0.0224 mL | 0.1121 mL | 0.2242 mL | 0.5604 mL | |
| 100 mM | 0.0179 mL | 0.0897 mL | 0.1793 mL | 0.4484 mL |
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