Pemigatinib
Based on 22 publication(s) in Google Scholar
Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 1513857-77-6
- Formula: C24H27F2N5O4
- Molecular Weight:487.50
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Storage: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) Pemigatinib
More- Nature. 2022 Aug;608(7923):609-617. [Abstract]
- Cancer Res. 2025 Jun 24. [Abstract]
- Adv Sci (Weinh). 2024 Nov 28:e2407519. [Abstract]
- Cell Death Dis. 2025 Apr 4;16(1):251. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Mar 24;123(12):e2506886123. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2317756121. [Abstract]
- NPJ Precis Oncol. 2021 Jul 16;5(1):66. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- J Chem Inf Model. 2024 Mar 25;64(6):2058-2067. [Abstract]
- Commun Biol. 2025 Aug 8;8(1):1185. [Abstract]
- Int J Mol Sci. 2026 Jun 9;27(12):5217. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Luminescence. 2024 Jun;39(6):e4813. [Abstract]
- Separations. 2023 Apr 10, 10(4), 247.
- BMJ Open Ophthalmol. 2026 Jan 12;11(1):e002307. [Abstract]
- Biochem Biophys Res Commun. 2024 Jan 8:691:149314. [Abstract]
- Anticancer Drugs. 2023 Oct 1;34(9):1035-1045. [Abstract]
- Technical University of Dresden. 2025.
- University of Auckland. 2025.
- SSRN. 2025 Jul 4.
- Preprints. 2024 Mar 20.
- Research Square Preprint. 2024 Jan 31.
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Cell Proliferation/Viability Assay
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In Vivo Imaging
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WB
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RT-PCR
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2D/3D Cell Culture and Differentiation
Biological Activity
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FGFR1 0.4 nM (IC50) |
FGFR2 0.5 nM (IC50) |
FGFR3 1.2 nM (IC50) |
FGFR4 30 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A204 | IC50 |
18.4 nM
Compound: 1
|
Antiproliferation activity against human A204 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human A204 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
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[PMID: 38718625] |
| AN3-CA | GI50 |
0.132 μM
Compound: 3
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Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| BaF3 | GI50 |
>5 μM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
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[PMID: 35436119] |
| BaF3 | GI50 |
>5 μM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
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[PMID: 35436119] |
| BaF3 | GI50 |
0.005 μM
Compound: 3
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Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
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[PMID: 35436119] |
| BaF3 | GI50 |
2.073 μM
Compound: 3
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Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
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[PMID: 35436119] |
| BaF3 | GI50 |
4.495 μM
Compound: 3
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Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
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[PMID: 35436119] |
| J82 | GI50 |
4.286 μM
Compound: 3
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Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
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[PMID: 35436119] |
| KMS-11 | GI50 |
0.232 μM
Compound: 3
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Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
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[PMID: 35436119] |
| MDA-MB-453 | IC50 |
73.7 nM
Compound: 1
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Antiproliferation activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant incubated for 72 hrs by CCK8 assay
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[PMID: 38718625] |
| RT-112 | IC50 |
>1150 nM
Compound: Pemigatinib
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Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
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[PMID: 38267212] |
| RT-112 | IC50 |
174 nM
Compound: Pemigatinib
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Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
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[PMID: 38267212] |
| RT-112 | IC50 |
1880 nM
Compound: Pemigatinib
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Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
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[PMID: 38267212] |
| RT-112 | IC50 |
23.7 nM
Compound: 1
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Antiproliferation activity against human RT-112 cells harboring FGFR3-TACC3 incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human RT-112 cells harboring FGFR3-TACC3 incubated for 72 hrs by CCK8 assay
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[PMID: 38718625] |
| RT-112 | IC50 |
3.3 nM
Compound: Pemigatinib
|
Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
|
[PMID: 38267212] |
| RT-112 | IC50 |
6 nM
Compound: Pemigatinib
|
Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
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[PMID: 38267212] |
| Sf9 | IC50 |
0.4 nM
Compound: 2
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Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and m
Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and m
|
[PMID: 36356320] |
| Sf9 | IC50 |
1.7 nM
Compound: 2
|
Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition a
Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition a
|
[PMID: 36356320] |
| SNU-16 | IC50 |
3.9 nM
Compound: Pemigatinib
|
Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
|
[PMID: 38267212] |
| SNU-16 | IC50 |
5.9 nM
Compound: 1
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Antiproliferation activity against human SNU-16 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
Antiproliferation activity against human SNU-16 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
|
[PMID: 38718625] |
Cells expressing the FGFR2-CLIP1 fusion is sensitive to Pemigatinib (INCB054828; IC50 value 10.16 nM), while cells with added N549H mutation is resistant to Pemigatinib (IC50 value of 1527.57 nM)[3].
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. 1513857-77-6
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Appearance Solid
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Molecular Weight 487.50
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Formula C24H27F2N5O4
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Color White to light yellow
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SMILES
CCN(C(N(C(C(F)=C(OC)C=C1OC)=C1F)C2)=O)C(C2=CN3)=C4C3=NC(CN5CCOCC5)=C4
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Synonyms
INCB054828
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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Journal Impact Factor
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Most Recent
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Nature
2022 Aug;608(7923):609-617. PMID: 35948633
Pemigatinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Aug;608(7923):609-617. [Abstract]
Half-maximum inhibitory concentration (IC50) value quantifications of 2D-grown NMuMG cells expressing GFP or the indicated Fgfr2 variants and treated with AZD4547 or Pemigatinib for 4 days. Data are the mean of 5 independent experiments (GFP, Fgfr2FL, Fgfr2ΔE18) or 1 experiment (other Fgfr2 variants).
Pemigatinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Aug;608(7923):609-617. [Abstract]
Dose-response curves of indicated human cancer cell lines treated with Pemigatinib (0.01-105 nM) for 4 days.
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Cancer Res
The C-terminal Kinase Domain-Binding and Suppression Motif Prevents Constitutive Activation of FGFR2. [Abstract]2025 Jun 24. PMID: 40554806
Pemigatinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 24. [Abstract]
Growth rate (GR)-corrected dose–response curves of NMuMG cells expressing indicated Fgfr2 variants and treated for 4 days with Pemigatinib (10-4-100 μM). Data are represented as mean ± SEM of n = 5 replicas per group.
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Adv Sci (Weinh)
Synthetic Retinoid Sulfarotene Selectively Inhibits Tumor-Repopulating Cells of Intrahepatic Cholangiocarcinoma via Disrupting Cytoskeleton by P-Selectin/PSGL1 N-Glycosylation Blockage. [Abstract]2024 Nov 28:e2407519. PMID: 39605300 -
Cell Death Dis
Growth factor receptor plasticity drives therapeutic persistence of metastatic breast cancer. [Abstract]2025 Apr 4;16(1):251. PMID: 40185706
Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251. [Abstract]
T07 cells (5 × 105) were injected into the tail vein of approximately 6-week-old female BALB/c mice, and after 3 days mice were randomized prior to dosing of Pemigatinib at (25 mg/kg; oral gavage). BLI of vehicle vs pemigatinib-treated mice on days 10 and 14. The results showed that Pemigatinib significantly reduced pulmonary tumor burden in these mice.
Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251. [Abstract]
4T07 cells were treated with Pemigatinib (Pemi, 10 nM) for the indicated amounts of time. Cells were lysed and analyzed by immunoblot for expression of PDGFR (α and β), ERK1/2 (phospho and total), and tubulin.
Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251. [Abstract]
4T07 cells were treated with Pemigatinib (10 nM) for 24 h and cells were analyzed by RT-PCR for expression of PDGFRa and PDGFRb.
Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251. [Abstract]
4T07 cells (2000 cells) were seeded under 3D culture conditions for 3 days at which point the cultures were left untreated (top row) or treated with Pemigatinib (50 nM; bottom row) for 96 h. Following drug treatment, cultures were allowed to recover in the absence or presence of PDGF-bb (100 ng/µL). Representative brightfield images are shown at the indicated days and treatment conditions.
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Proc Natl Acad Sci U S A
The conserved fibroblast growth factor receptor-based signaling is required for dendrite regeneration. [Abstract]2026 Mar 24;123(12):e2506886123. PMID: 41849383 -
Proc Natl Acad Sci U S A
Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2. [Abstract]2024 Feb 6;121(6):e2317756121. PMID: 38300868 -
NPJ Precis Oncol
Comprehensive functional evaluation of variants of fibroblast growth factor receptor genes in cancer. [Abstract]2021 Jul 16;5(1):66. PMID: 34272467 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
J Chem Inf Model
Probe Substrate Dependencies in CYP3A4 Allosteric Inhibition: A Novel Molecular Mechanism Involving F-F' Loop Perturbations. [Abstract]2024 Mar 25;64(6):2058-2067. PMID: 38457234 -
Commun Biol
Exploiting collateral sensitivity in the evolution of resistance to tyrosine kinase inhibitors in soft tissue sarcomas. [Abstract]2025 Aug 8;8(1):1185. PMID: 40781553 -
Int J Mol Sci
Inhibition of Fibroblast Growth Factor Receptor 3 Signaling by Ponatinib Reduces Growth and Cytokine Production of Multiple Myeloma Cells. [Abstract]2026 Jun 9;27(12):5217. PMID: 42352940 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Luminescence
A green and highly sensitive microwell spectrofluorimetric method with high throughput for the determination of pemigatinib based on dual fluorescence enhancement by photoinduced electron transfer blocking and micellization: Application to the analysis of tablets, content uniformity testing, and human plasma. [Abstract]2024 Jun;39(6):e4813. PMID: 38922756 -
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BMJ Open Ophthalmol
Impact of anticancer drugs on human Tenon's fibroblast proliferation: implications for glaucoma surgery. [Abstract]2026 Jan 12;11(1):e002307. PMID: 41526033 -
Biochem Biophys Res Commun
Pemigatinib, a selective FGFR inhibitor overcomes ABCB1-mediated multidrug resistance in cancer cells. [Abstract]2024 Jan 8:691:149314. PMID: 38039831 -
Anticancer Drugs
Derazantinib, a fibroblast growth factor receptor inhibitor, inhibits colony-stimulating factor receptor-1 in macrophages and tumor cells and in combination with a murine programmed cell death ligand-1-antibody activates the immune environment of murine syngeneic tumor models. [Abstract]2023 Oct 1;34(9):1035-1045. PMID: 36729099 -
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Solvent & Solubility
DMSO : 25 mg/mL (51.28 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, 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: 2.08 mg/mL (4.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Arudra K, et al. Calcinosis cutis dermatologic toxicity associated with fibroblast growth factor receptor inhibitor for the treatment of Wilms tumor. J Cutan Pathol. 2018 Oct;45(10):786-790. [Content Brief]
[2]. Roskoski R Jr, et al. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567. [Content Brief]
[3]. Krook MA, et al. Tumor heterogeneity and acquired drug resistance in FGFR2-fusion-positive cholangiocarcinoma through rapid research autopsy. Cold Spring Harb Mol Case Stud. 2019 Aug 1;5(4). [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, 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 | 2.0513 mL | 10.2564 mL | 20.5128 mL | 51.2821 mL |
| 5 mM | 0.4103 mL | 2.0513 mL | 4.1026 mL | 10.2564 mL | |
| 10 mM | 0.2051 mL | 1.0256 mL | 2.0513 mL | 5.1282 mL | |
| 15 mM | 0.1368 mL | 0.6838 mL | 1.3675 mL | 3.4188 mL | |
| 20 mM | 0.1026 mL | 0.5128 mL | 1.0256 mL | 2.5641 mL | |
| 25 mM | 0.0821 mL | 0.4103 mL | 0.8205 mL | 2.0513 mL | |
| 30 mM | 0.0684 mL | 0.3419 mL | 0.6838 mL | 1.7094 mL | |
| 40 mM | 0.0513 mL | 0.2564 mL | 0.5128 mL | 1.2821 mL | |
| 50 mM | 0.0410 mL | 0.2051 mL | 0.4103 mL | 1.0256 mL |