KU-60019
Based on 28 publication(s) in Google Scholar
KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.43%
- No. CAS: 925701-46-8
- Fòrmula: C30H33N3O5S
- Peso molecular:547.67
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) KU-60019
More- Cell Stem Cell. 2026 Mar 5;33(3):470-486.e14. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Biomater. 2021 Jun:127:276-286. [Abstract]
- Acta Pharmacol Sin. 2021 Apr;42(4):648-654. [Abstract]
- Cell Rep. 2020 Jan 14;30(2):497-509.e4. [Abstract]
- Breast Cancer Res. 2025 May 26;27(1):92. [Abstract]
- EMBO Rep. 2024 Mar;25(3):1469-1489. [Abstract]
- Oncogenesis. 2020 Feb 3;9(2):8. [Abstract]
- Int J Mol Sci. 2024 Nov 11;25(22):12108. [Abstract]
- Int J Mol Sci. 2024 Jun 25;25(13):6947. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Am J Pathol. 2026 Jun 10:S0002-9440(26)00163-X. [Abstract]
- World J Stem Cells. 2026 Jan 26;18(1):112278. [Abstract]
- Sci Rep. 2023 Jan 17;13(1):882. [Abstract]
- Cancers (Basel). 2023 Sep 6;15(18):4442. [Abstract]
- Neoplasia. 2018 Mar 28;20(5):478-488. [Abstract]
- Cell Signal. 2025 Jul:131:111709. [Abstract]
- iScience. 2025 Sep 4;28(10):113508. [Abstract]
- iScience. 2020 Aug 21;23(8):101431. [Abstract]
- FASEB J. 2022 Jul;36(7):e22379. [Abstract]
- University of North Carolina at Chapel Hill. 2026.
- University of Califomia San Francisco. 2026.
- Res Sq. 2025 Nov 19:rs.3.rs-7682325. [Abstract]
- bioRxiv. 2025 Aug 21.
- Authorea. 2025 Aug 22.
- University of Gothenburg. 2023 Jun 27.
- Technische Universitat Darmstadt. 2022 Aug.
- Oxid Med Cell Longev. 2022 Jun 24;2022:4201287. [Abstract]
Customer Validation & Images
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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WB
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WB
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Cell Proliferation/Viability Assay
Actividad biológica
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ATM 6.3 nM (IC50) |
DNA-PKcs 1.7 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | IC50 |
0.149 μM
Compound: 2; KU-60019
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Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis
Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis
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[PMID: 27259031] |
| HT-29 | IC50 |
8.5 μM
Compound: 2; KU-60019
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Inhibition of ATR in human HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis
Inhibition of ATR in human HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis
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[PMID: 27259031] |
| MCF7 | IC50 |
11.9 μM
Compound: 2; KU-60019
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Antiproliferative activity against human MCF7 cells measured after 2 days by SRB assay
Antiproliferative activity against human MCF7 cells measured after 2 days by SRB assay
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[PMID: 35231830] |
| MCF7 | IC50 |
2.8 μM
Compound: 2; KU-60019
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Antiproliferative activity against human MCF7 cells measured after 6 days by SRB assay
Antiproliferative activity against human MCF7 cells measured after 6 days by SRB assay
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[PMID: 35231830] |
| SW480 | IC50 |
13.3 μM
Compound: 2; KU-60019
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Antiproliferative activity against human SW480 cells measured after 3 days by SRB assay
Antiproliferative activity against human SW480 cells measured after 3 days by SRB assay
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[PMID: 35231830] |
| SW480 | IC50 |
3.3 μM
Compound: 2; KU-60019
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Antiproliferative activity against human SW480 cells measured after 9 days by SRB assay
Antiproliferative activity against human SW480 cells measured after 9 days by SRB assay
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[PMID: 35231830] |
KU-60019 is an improved analogue of KU-55933. KU-55933 has an IC50 of 13 nM and Ki of 2.2 nM in vitro and is highly specific for the ATM kinase using a panel of 60 protein kinases. KU-60019 is an improved inhibitor of the ATM kinase with an IC50 of 6.3 nM, approximately half that of KU-55933. The IC50 values for DNA-PKcs and ATR are 1.7 and >10 μM, respectively, almost 270-and 1600-fold higher than for ATM. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. In human U87 glioma cells, KU-55933 completely inhibits phosphorylation of p53 (S15) at 10 μM but not at 3 μM, whereas γ-H2AX levels are only partly reduced with 10 μM 1 h after irradiation. By comparison, 3 μM KU-60019 completely inhibits p53 phosphorylation and partial inhibits at 1 μM[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 925701-46-8
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Appearance Solid
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Peso molecular 547.67
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Fòrmula C30H33N3O5S
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Color Light yellow to khaki
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SMILES
C[C@@H]1O[C@@H](CN(CC(NC2=CC3=C(C=C2)SC4=C(C3)C=CC=C4C5=CC(C=C(O5)N6CCOCC6)=O)=O)C1)C
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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 (28)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
Minimizing far-extending chromatin perturbation in genome editing preserves stem cell identity. [Abstract]2026 Mar 5;33(3):470-486.e14. PMID: 41742419 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Acta Biomater
Ataxia telangiectasia mutated inhibitor-loaded copper sulfide nanoparticles for low-temperature photothermal therapy of hepatocellular carcinoma. [Abstract]2021 Jun:127:276-286. PMID: 33812073 -
Acta Pharmacol Sin
Targeting DNA-PK overcomes acquired resistance to third-generation EGFR-TKI osimertinib in non-small-cell lung cancer. [Abstract]2021 Apr;42(4):648-654. PMID: 33414509 -
Cell Rep
2020 Jan 14;30(2):497-509.e4. PMID: 31940492 -
Breast Cancer Res
NOTCH1 inhibition enhances immunogenicity and sensitizes triple-negative breast cancer to immune checkpoint inhibitors. [Abstract]2025 May 26;27(1):92. PMID: 40420289
KU-60019 purchased from MedChemExpress. Usage Cited in: Breast Cancer Res. 2025 May 26;27(1):92. [Abstract]
Senescence was detected by SA-β-Gal staining after MDA-MB-231 cells were treated with shNOTCH1 plasmid or KU60019 (3 μM, 48 h).
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EMBO Rep
Tumor acidosis-induced DNA damage response and tetraploidy enhance sensitivity to ATM and ATR inhibitors. [Abstract]2024 Mar;25(3):1469-1489. PMID: 38366255
KU-60019 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2024 Mar;25(3):1469-1489. [Abstract]
Cell viability assays were performed in HCT116 and HT-29 cancer cells cultured at pH 7.4 or 6.5 and treated with the indicated doses of ATMi KU60019 for 72 h.
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Oncogenesis
SCFβ-TrCP-mediated degradation of TOP2β promotes cancer cell survival in response to chemotherapeutic drugs targeting topoisomerase II. [Abstract]2020 Feb 3;9(2):8. PMID: 32015321
KU-60019 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2020 Feb 3;9(2):8. [Abstract]
KU60019 (5 μM, 3 h) abolished VM-26-induced TOP2β degradation in SK-BR3 and MDA-MB-231 cells.
KU-60019 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2020 Feb 3;9(2):8. [Abstract]
The half-life of TOP2β protein was significantly extended in the presence of KU60019 (5 μM, 1 h).
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Int J Mol Sci
2024 Nov 11;25(22):12108. PMID: 39596176 -
Int J Mol Sci
2024 Jun 25;25(13):6947. PMID: 39000057 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Am J Pathol
Low-Dose Radiotherapy Attenuates Pulmonary Granulomas Involving Ataxia-Telangiectasia Mutated-Dependent Modulation of the Interferon-β Response: A Host-Directed Therapeutic Strategy for Tuberculosis. [Abstract]2026 Jun 10:S0002-9440(26)00163-X. PMID: 42270072 -
World J Stem Cells
Hypoxia facilitates triple-negative breast cancer stem cells enrichment and stemness maintenance through oxidized ataxia telangiectasia mutated-induced one-carbon metabolism. [Abstract]2026 Jan 26;18(1):112278. PMID: 41608656 -
Sci Rep
ATM inhibitor KU60019 synergistically sensitizes lung cancer cells to topoisomerase II poisons by multiple mechanisms. [Abstract]2023 Jan 17;13(1):882. PMID: 36650267 -
Cancers (Basel)
In Vitro and In Silico Investigation of BCI Anticancer Properties and Its Potential for Chemotherapy-Combined Treatments. [Abstract]2023 Sep 6;15(18):4442. PMID: 37760412 -
Neoplasia
Combined Inhibition of ATR and WEE1 as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer. [Abstract]2018 Mar 28;20(5):478-488. PMID: 29605721
KU-60019 purchased from MedChemExpress. Usage Cited in: Neoplasia. 2018 Mar 28;20(5):478-488. [Abstract]
MDA-MB-231 and Hs578t cells were treated with 0.05–50 µM of AZD1775 in combination with 0.1–10 µM of ATRi, ATMi (KU-60019) or DNA-PKi for 72 h. Cell viability was detected by CCK-8 assay (n = 3, means).
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Cell Signal
2025 Jul:131:111709. PMID: 40037423 -
iScience
Nucleolar stress facilitates islet β cell senescence via hijacking the DNA damage response pathways. [Abstract]2025 Sep 4;28(10):113508. PMID: 41031371 -
iScience
BxPC-3-Derived Small Extracellular Vesicles Induce FOXP3+ Treg through ATM-AMPK-Sirtuins-Mediated FOXOs Nuclear Translocations. [Abstract]2020 Aug 21;23(8):101431. PMID: 32798974 -
FASEB J
Downregulation of miR-1270 mediates endothelial progenitor cell function in preeclampsia: Role for ATM in the Src/VE-cadherin axis. [Abstract]2022 Jul;36(7):e22379. PMID: 35648632 -
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Res Sq
Small Molecule Activators of the Mitochondrial Protease ClpP Induce Senescence in Triple-Negative Breast Cancer Cells and Sensitize Cells to the Bcl-2 Inhibitor Venetoclax. [Abstract]2025 Nov 19:rs.3.rs-7682325. PMID: 41333384 -
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Oxid Med Cell Longev
Inhibition of PLK3 Attenuates Tubular Epithelial Cell Apoptosis after Renal Ischemia-Reperfusion Injury by Blocking the ATM/P53-Mediated DNA Damage Response. [Abstract]2022 Jun 24;2022:4201287. PMID: 35783188
Solvente y solubilidad
DMSO : 100 mg/mL (182.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 10 mg/mL (18.26 mM; Need ultrasonic)
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 (4.56 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 (4.56 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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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
Cell growth is determined by AlamarBlue. U1242 cells are serially diluted, allowed to attach for 6 h and then exposed to KU-60019 at 3 μM. At days 1, 3 and 5 after seeding, AlamarBlue is added to the medium to the recommended final concentration. Plates are incubated for 1 h at 37°C and fluorescence determined on a FluoroCount plate reader (excitation 530 nm, emission 590 nm) and values taken as a measure of cell growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Cells (3×107) are implanted into male Fox Chase Severe Combined Immunodeficiency (SCID) mice. Administration of Doxycycline is started when tumors reach 100 mm3 in volume and is performed every 48 hours up to removal of the animal from the experiment. Forty-eight hours after PTEN induction, animals are administered KU-60019 (100 mg/kg) for 5 consecutive days and measured until they reach a target 400 mm3 volume. Measurements of tumor volume and body weight took place every 3 days using calipers.
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 (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Golding SE, et al. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902. [Content Brief]
[2]. McCabe N, et al. Mechanistic Rationale to Target PTEN-Deficient Tumor Cells with Inhibitors of the DNA Damage Response Kinase ATM. Cancer Res. 2015 Jun 1;75(11):2159-65. [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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 1.8259 mL | 9.1296 mL | 18.2592 mL | 45.6479 mL |
| 5 mM | 0.3652 mL | 1.8259 mL | 3.6518 mL | 9.1296 mL | |
| 10 mM | 0.1826 mL | 0.9130 mL | 1.8259 mL | 4.5648 mL | |
| 15 mM | 0.1217 mL | 0.6086 mL | 1.2173 mL | 3.0432 mL | |
| DMSO | 20 mM | 0.0913 mL | 0.4565 mL | 0.9130 mL | 2.2824 mL |
| 25 mM | 0.0730 mL | 0.3652 mL | 0.7304 mL | 1.8259 mL | |
| 30 mM | 0.0609 mL | 0.3043 mL | 0.6086 mL | 1.5216 mL | |
| 40 mM | 0.0456 mL | 0.2282 mL | 0.4565 mL | 1.1412 mL | |
| 50 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.9130 mL | |
| 60 mM | 0.0304 mL | 0.1522 mL | 0.3043 mL | 0.7608 mL | |
| 80 mM | 0.0228 mL | 0.1141 mL | 0.2282 mL | 0.5706 mL | |
| 100 mM | 0.0183 mL | 0.0913 mL | 0.1826 mL | 0.4565 mL |
KU-60019 Related Classifications
HY-12061 Related Classifications
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