Temuterkib
Based on 35 publication(s) in Google Scholar
Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.93%
- CAS No.: 1951483-29-6
- Formule: C22H27N7O2S
- Masse moléculaire:453.56
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Temuterkib
More- Signal Transduct Target Ther. 2020 Sep 30;5(1):197. [Abstract]
- Immunity. 2026 May 13:S1074-7613(26)00171-8. [Abstract]
- Autophagy. 2025 Mar;21(3):565-582. [Abstract]
- Mol Cell. 2019 Jan 3;73(1):7-21.e7. [Abstract]
- Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]
- Cell Rep Med. 2026 Mar 26:102704. [Abstract]
- Cell Death Dis. 2022 Dec 27;13(12):1075. [Abstract]
- Phytomedicine. 2025 Dec 30:150:157747. [Abstract]
- Diabetes. 2023 Nov 1;72(11):1534-1546. [Abstract]
- Mol Med. 2025 May 29;31(1):211. [Abstract]
- EMBO Mol Med. 2023 Mar 8;15(3):e16235. [Abstract]
- Stem Cell Res Ther. 2024 Oct 8;15(1):350. [Abstract]
- Cell Rep. 2024 Mar 4;43(3):113881. [Abstract]
- J Med Chem. 2026 Apr 9;69(7):7663-7676. [Abstract]
- Front Immunol. 2021 Oct 8;12:709229. [Abstract]
- Biochem Pharmacol. 2025 Jul 12:241:117162. [Abstract]
- Cancer Biol Ther. 2022 Dec 31;23(1):69-82. [Abstract]
- Respir Res. 2021 Apr 1;22(1):97. [Abstract]
- Cancer Sci. 2019 May;110(5):1746-1759. [Abstract]
- Neoplasia. 2021 Jun;23(6):607-623. [Abstract]
- iScience. 2023 Jul 4;26(8):107283. [Abstract]
- Poultry Sci. 2021 May;100(5):101085. [Abstract]
- Front Biosci (Landmark Ed). 2024 Apr 23;29(4):160. [Abstract]
- J Biol Chem. 2024 Apr;300(4):107208. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2026 May 29. [Abstract]
- Cancer Res Commun. 2024 Sep 1;4(9):2454-2462. [Abstract]
- J Funct Foods. 45 (2018) 110-117.
- J Microbiol. 2020 Apr;58(4):320-329. [Abstract]
- Pathol Res Pract. 2022 Oct:238:154104. [Abstract]
- Arch Med Res. 2020 Feb;51(2):124-134. [Abstract]
- Cancer Med. 2020 Jun;9(11):3875-3884. [Abstract]
- J Food Biochem. 2020 Sep;44(9):e13352. [Abstract]
- Int J Ophthalmol. 2020 Jul 18;13(7):1039-1045. [Abstract]
- Drexel University. 2025.
- Int J Biol Sci. 2022 Jan 16;18(4):1363-1380. [Abstract]
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WB
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Bio/Physico-chemical Assay
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WB
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IF
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IP
Activité biologique
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ERK1 5 nM (IC50) |
ERK2 5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-MEL-2 | IC50 |
1 μM
Compound: LY3214996
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Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of MK2206 by MTT assay
Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of MK2206 by MTT assay
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[PMID: 36961300] |
| SK-MEL-2 | IC50 |
1 μM
Compound: LY3214996
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Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of Rapamycin by MTT assay
Synergistic cytotoxicity against human SK-MEL-2 cells expressing NRAS mutant assessed as cell growth inhibition measured for 48 hrs in presence of Rapamycin by MTT assay
|
[PMID: 36961300] |
Temuterkib is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to Temuterkib[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1951483-29-6
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Appearance Solid
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Masse moléculaire 453.56
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Formule C22H27N7O2S
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Color White to yellow
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SMILES
O=C(C(C=C(C1=NC(NC2=CC=NN2C)=NC=C1)S3)=C3C4(C)C)N4CCN5CCOCC5
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Synonyms
LY3214996
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (35)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
The cross-talk between methylation and phosphorylation in lymphoid-specific helicase drives cancer stem-like properties. [Abstract]2020 Sep 30;5(1):197. PMID: 32994405
Temuterkib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 30;5(1):197. [Abstract]
Endogenous and exogenous LSH were respectively immunoprecipitated from A549 and 293T cells after treatment with the MAPK1/2 inhibitor Temuterkib for the indicated time, and then IB assay was carried out to detect the phosphorylated LSH with anti-phosphoserine antibody.
Temuterkib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 30;5(1):197. [Abstract]
IP followed by IB assay in PC9 cell lines stably expressing LSH after treatment with the MAPK1/2 inhibitor Temuterkib for the indicated time.
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Immunity
Modulation of the mevalonate pathway by TCR engagement regulates T follicular helper cell generation in homeostasis and autoimmunity. [Abstract]2026 May 13:S1074-7613(26)00171-8. PMID: 42134327 -
Autophagy
USP13 facilitates a ferroptosis-to-autophagy switch by activation of the NFE2L2/NRF2-SQSTM1/p62-KEAP1 axis dependent on the KRAS signaling pathway. [Abstract]2025 Mar;21(3):565-582. PMID: 39360581
Temuterkib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar;21(3):565-582. [Abstract]
Western blot analysis of sgCtrl, sgUSP13#1 or sgUSP13#2 A549 cell lysates treated with DMSO or Temuterkib (LY3214996, 10 μM, 24 h) and probed with the indicated antibodies.
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Mol Cell
2019 Jan 3;73(1):7-21.e7. PMID: 30472188 -
Theranostics
FGF19/SOCE/NFATc2 signaling circuit facilitates the self-renewal of liver cancer stem cells. [Abstract]2021 Mar 5;11(10):5045-5060. PMID: 33754043
Temuterkib purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]
Cells were pre-treated with DMSO, 3-NC (20 µM), Temuterkib (LY3214996, 2 µM), or 3-NC (20 µM) + Temuterkib (LY3214996, 2 µM) for 2h, respectively; then Ca2+ mobilization in Fura-2-loaded cells respectively upon FGF19 stimulation were measured and expressed as means ± SEM of 12 independent cells each group.
Temuterkib purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]
Subcellular location of NFATc2 after FGF19 treatment: Huh-7 NCSCs were pre-treated with DMSO, BLU9931 (100 nM), 3-NC (20 µM), Temuterkib (LY3214996, 2 µM), 3-NC (20 µM) + Temuterkib (LY3214996, 2 µM), SKF96365 (5 µM), and FK506 (50 nM) for 2h, respectively; then treated with FGF19 (100 ng/ml) for 4h.
Temuterkib purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]
Subcellular location of NFATc2 after FGF19 treatment: Huh-7 NCSCs were pre-treated with DMSO, BLU9931 (100 nM), 3-NC (20 µM), Temuterkib (LY3214996, 2 µM), 3-NC (20 µM) + Temuterkib (LY3214996, 2 µM), SKF96365 (5 µM), and FK506 (50 nM) for 2h, respectively; then treated with FGF19 (100 ng/ml) for 4h.
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Cell Rep Med
Targeting the noncanonical function of metabolic enzyme PHGDH in driving PD-L1 expression and cancer immune evasion. [Abstract]2026 Mar 26:102704. PMID: 41905348 -
Cell Death Dis
4EBP1 senses extracellular glucose deprivation and initiates cell death signaling in lung cancer. [Abstract]2022 Dec 27;13(12):1075. PMID: 36575176 -
Phytomedicine
Unveiling poliumoside: A herbal-derived FAK kinase inhibitor with anti-proliferative and anti-metastatic efficacy. [Abstract]2025 Dec 30:150:157747. PMID: 41485292 -
Diabetes
Chronic Glucocorticoid Exposure Induced a S1PR2-RORγ Axis to Enhance Hepatic Gluconeogenesis in Male Mice. [Abstract]2023 Nov 1;72(11):1534-1546. PMID: 37552863 -
Mol Med
Activation of the MEK1-CHK2 axis in macrophages by Staphylococcus aureus promotes mitophagy, resulting in a reduction in bactericidal efficacy. [Abstract]2025 May 29;31(1):211. PMID: 40437411 -
EMBO Mol Med
Thioparib inhibits homologous recombination repair, activates the type I IFN response, and overcomes olaparib resistance. [Abstract]2023 Mar 8;15(3):e16235. PMID: 36652375 -
Stem Cell Res Ther
SMYD1 modulates the proliferation of multipotent cardiac progenitor cells derived from human pluripotent stem cells during myocardial differentiation through GSK3β/β-catenin&ERK signaling. [Abstract]2024 Oct 8;15(1):350. PMID: 39380045 -
Cell Rep
Liver-derived plasminogen mediates muscle stem cell expansion during caloric restriction through the plasminogen receptor Plg-RKT. [Abstract]2024 Mar 4;43(3):113881. PMID: 38442019 -
J Med Chem
Platinum-Paeonol Complexes as ERK Inhibitors To Restrain Melanoma and Relieve Cancer Pain. [Abstract]2026 Apr 9;69(7):7663-7676. PMID: 41873204 -
Front Immunol
IL-27 Mediates Pro-Inflammatory Effects via the ERK Signaling Pathway During Preterm Labor. [Abstract]2021 Oct 8;12:709229. PMID: 34691022 -
Biochem Pharmacol
Glimepiride overcomes acquired resistance to EGFR TKIs in lung cancer via the AMPK/ERK/MMP7 signaling pathway. [Abstract]2025 Jul 12:241:117162. PMID: 40659128 -
Cancer Biol Ther
Repeated treatments of Capan-1 cells with PARP1 and Chk1 inhibitors promote drug resistance, migration and invasion. [Abstract]2022 Dec 31;23(1):69-82. PMID: 35000525 -
Respir Res
CREB-dependent LPA-induced signaling initiates a pro-fibrotic feedback loop between small airway basal cells and fibroblasts. [Abstract]2021 Apr 1;22(1):97. PMID: 33794877 -
Cancer Sci
Antitumor activity of Raddeanin A is mediated by Jun amino-terminal kinase activation and signal transducer and activator of transcription 3 inhibition in human osteosarcoma. [Abstract]2019 May;110(5):1746-1759. PMID: 30907478
Temuterkib purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2019 May;110(5):1746-1759. [Abstract]
Cells are treated with RA in the presence or absence of the Erk1/2 inhibitor LY3214996, phospho-Erk1/2, Erk1/2, phospho-JNK, JNK, phospho-c-Jun, c-Jun, total and cleaved PARP, phospho-STAT3S727, and STAT3 are analyzed.
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Neoplasia
STAMBP promotes lung adenocarcinoma metastasis by regulating the EGFR/MAPK signaling pathway. [Abstract]2021 Jun;23(6):607-623. PMID: 34102455 -
iScience
A defective mechanosensing pathway affects fibroblast-to-myofibroblast transition in the old male mouse heart. [Abstract]2023 Jul 4;26(8):107283. PMID: 37520701 -
Poultry Sci
SC75741 antagonizes vesicular stomatitis virus, duck Tembusu virus, and duck plague virus infection in duck cells through promoting innate immune responses. [Abstract]2021 May;100(5):101085. PMID: 33799115 -
Front Biosci (Landmark Ed)
Activation of the MEK/ERK Pathway Mediates the Inhibitory Effects of Silvestrol on Nasopharyngeal Carcinoma Cells via RAP1A, HK2, and GADD45A. [Abstract]2024 Apr 23;29(4):160. PMID: 38682208 -
J Biol Chem
Upregulation of CYR61 by TGF-β and YAP signaling exerts a counter-suppression of hepatocellular carcinoma. [Abstract]2024 Apr;300(4):107208. PMID: 38521502 -
Naunyn Schmiedebergs Arch Pharmacol
Label-free cell phenotypic profiling of sphingosine-1-phosphate receptor 1 and discovery of its agonist from natural products. [Abstract]2026 May 29. PMID: 42209736 -
Cancer Res Commun
2024 Sep 1;4(9):2454-2462. PMID: 39212544 -
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J Microbiol
Autophagy of bovine mammary epithelial cell induced by intracellular Staphylococcus aureus. [Abstract]2020 Apr;58(4):320-329. PMID: 32103442 -
Pathol Res Pract
Effect of NMB-regulated ERK1/2 and p65 signaling pathway on proliferation and apoptosis of cervical cancer. [Abstract]2022 Oct:238:154104. PMID: 36095918 -
Arch Med Res
Infiltrating Macrophages Induced Stem-cell-like Features Through PI3K/AKT/GSK3β Signaling to Promote Neurofibroma Growth. [Abstract]2020 Feb;51(2):124-134. PMID: 32111496 -
Cancer Med
Metformin revert insulin-induced oxaliplatin resistance by activating mitochondrial apoptosis pathway in human colon cancer HCT116 cells. [Abstract]2020 Jun;9(11):3875-3884. PMID: 32248666 -
J Food Biochem
A novel di-peptide Met-Glu from collagen hydrolysates inhibits platelet aggregation and thrombus formation via regulation of Gq-mediated signaling. [Abstract]2020 Sep;44(9):e13352. PMID: 32662128 -
Int J Ophthalmol
Blocking VEGF signaling augments interleukin-8 secretion via MEK/ERK/1/2 axis in human retinal pigment epithelial cells. [Abstract]2020 Jul 18;13(7):1039-1045. PMID: 32685389 -
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Int J Biol Sci
Cancer-associated adipocytes promote the invasion and metastasis in breast cancer through LIF/CXCLs positive feedback loop. [Abstract]2022 Jan 16;18(4):1363-1380. PMID: 35280694
Solvant et solubilité
DMSO : 16.67 mg/mL (36.75 mM; ultrasonic and warming and heat to 60°C; 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Instruction de manipulation (2659 KB)
Références
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2048 mL | 11.0239 mL | 22.0478 mL | 55.1195 mL |
| 5 mM | 0.4410 mL | 2.2048 mL | 4.4096 mL | 11.0239 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2048 mL | 5.5119 mL | |
| 15 mM | 0.1470 mL | 0.7349 mL | 1.4699 mL | 3.6746 mL | |
| 20 mM | 0.1102 mL | 0.5512 mL | 1.1024 mL | 2.7560 mL | |
| 25 mM | 0.0882 mL | 0.4410 mL | 0.8819 mL | 2.2048 mL | |
| 30 mM | 0.0735 mL | 0.3675 mL | 0.7349 mL | 1.8373 mL |