GW843682X
Based on 7 publication(s) in Google Scholar
GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.89%
- CAS 番号: 660868-91-7
- 分子式: C22H18F3N3O4S
- 分子量:477.46
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 GW843682X
More- Signal Transduct Target Ther. 2026 Jun 23;11(1):244. [Abstract]
- Sci Adv. 2025 Nov 28;11(48):eadz2345. [Abstract]
- Cell Rep. 2021 Jun 8;35(10):109225. [Abstract]
- Sci Rep. 2017 Aug 17;7(1):8629. [Abstract]
- Mol Oncol. 2024 Feb;18(2):386-414. [Abstract]
- Adv Ther (Weinh). 10 September 2022.
- Technical University of Dresden. 2025.
生物活性
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PLK1 2.2 nM (IC50) |
PLK3 9.1 nM (IC50) |
PDGFR1β 160 nM (IC50) |
VEGFR2 360 nM (IC50) |
Aurora A 4800 nM (IC50) |
CDK2/cyclin A 7600 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.41 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| A549 | IC50 |
411 nM
Compound: 2
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Antiproliferative activity against human A549 cells after 3 days by methylene blue stain technique
Antiproliferative activity against human A549 cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
| BT-474 | IC50 |
0.57 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth
Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| HCT-116 | IC50 |
0.7 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| HCT-116 | IC50 |
699 nM
Compound: 2
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Antiproliferative activity against human HCT116 cells after 3 days by methylene blue stain technique
Antiproliferative activity against human HCT116 cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
| HeLa | IC50 |
0.11 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| HN5 | IC50 |
0.68 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human HN5 cells assessed as inhibition of cell growth
Antiproliferative activity against human HN5 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| HN5 | IC50 |
678 nM
Compound: 2
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Antiproliferative activity against human HN5 cells after 3 days by methylene blue stain technique
Antiproliferative activity against human HN5 cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
| MCF7 | IC50 |
0.56 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| MCF7 | IC50 |
558 nM
Compound: 2
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Antiproliferative activity against human MCF7 cells after 3 days by methylene blue stain technique
Antiproliferative activity against human MCF7 cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
| MES-SA | IC50 |
0.21 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against DX5 resistant human MES-SA cells assessed as inhibition of cell growth
Antiproliferative activity against DX5 resistant human MES-SA cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| MES-SA | IC50 |
0.21 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human MES-SA cells assessed as inhibition of cell growth
Antiproliferative activity against human MES-SA cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| NCI-H460 | IC50 |
0.38 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| NCI-H460 | IC50 |
380 nM
Compound: 2
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Antiproliferative activity against human H460 cells after 3 days by methylene blue stain technique
Antiproliferative activity against human H460 cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
| NCI-N87 | IC50 |
0.6 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth
Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| NCI-N87 | IC50 |
601 nM
Compound: 2
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Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue stain technique
Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
| NHDF | IC50 |
6.14 μM
Compound: Chemical probe: Compound 1
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Cytotoxicity against human HDF cells assessed as inhibition of cell growth
Cytotoxicity against human HDF cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| PC-3 | IC50 |
6.82 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| PC-3 | IC50 |
6820 nM
Compound: 2
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Antiproliferative activity against human PC3 cells after 3 days by methylene blue stain technique
Antiproliferative activity against human PC3 cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
| RKO | IC50 |
0.4 μM
Compound: Chemical probe: Compound 1
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Antiproliferative activity against human RKO cells assessed as inhibition of cell growth
Antiproliferative activity against human RKO cells assessed as inhibition of cell growth
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[PMID: 17267659] |
| RKO | IC50 |
398 nM
Compound: 2
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Antiproliferative activity against human RKO cells after 3 days by methylene blue stain technique
Antiproliferative activity against human RKO cells after 3 days by methylene blue stain technique
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[PMID: 19097784] |
GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC50s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53, with an IC50 of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells[1]. GW843682X inhibits proliferation of U937 cells with an EC50 of 120 nM. GW843682X (500 nM) in combination with 5 μM VP-16 suppresses 50% of entry into mitosis in U937 cells[2]. GW843682X (0.06-1 μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 660868-91-7
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性状 Solid
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分子量 477.46
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分子式 C22H18F3N3O4S
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Color Light yellow to yellow
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SMILES
O=C(C1=C(OCC2=CC=CC=C2C(F)(F)F)C=C(N3C4=CC(OC)=C(OC)C=C4N=C3)S1)N
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別名
GW843682
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Large-scale and high-resolution mass spectrometry-based proteomics defines molecular subtypes of nasopharyngeal carcinoma for therapeutic targeting. [Abstract]2026 Jun 23;11(1):244. PMID: 42331772 -
Sci Adv
FeaSion decodes the regulatory landscape and functional diversity of RNA polymerase II CTD phosphorylation. [Abstract]2025 Nov 28;11(48):eadz2345. PMID: 41313762 -
Cell Rep
miR-24 controls the regenerative competence of hair follicle progenitors by targeting Plk3. [Abstract]2021 Jun 8;35(10):109225. PMID: 34107258 -
Sci Rep
Identification of Polo-like kinases as potential novel drug targets for influenza A virus. [Abstract]2017 Aug 17;7(1):8629. PMID: 28819179 -
Mol Oncol
Repositioning VU-0365114 as a novel microtubule-destabilizing agent for treating cancer and overcoming drug resistance. [Abstract]2024 Feb;18(2):386-414. PMID: 37842807 -
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溶剤 & 溶解度
DMSO : 33.33 mg/mL (69.81 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, 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (5.24 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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.
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.
プロトコル
PLK1 and PLK3 proteins are prepared from baculovirus-infected Trichoplusia ni cells. Enzyme activity for PLK1 and PLK3 is determined as follows. All measurements are obtained under conditions where signal production increased linearly with time and enzyme. Test compounds are added to white 384-well assay plates (0.1 μL for 10 μL and some 20 μL assays, 1 μL for some 20 μL assays) at variable known concentrations in 100% DMSO. DMSO (1-5% final) and EDTA (65 mM) are used as controls. Reaction Mix containes the following components at 22°C: 25 mM HEPES (pH 7.2); 15 mM MgCl2; 1 μM ATP; 0.05 μCi/well [γ-33P]ATP (10 Ci/mmol); 1 μM substrate peptide (Biotin-Ahx-SFNDTLDFD); 0.15 mg/mL bovine serum albumin; 1 mM DTT; and 2 nM PLK1 kinase domain or 5 nM full-length PLK3. Reaction Mix (10 or 20 μL) is quickly added to each well immediately following addition of enzyme via automated liquid handlers and incubated for 1 to 1.5 h at 22°C. The 20 μL enzymatic reactions are stopped with 50 μL of stop mix [50 mM EDTA, 4.0 mg/mL streptavidin SPA beads in Dulbecco's PBS (without Mg2+ and Ca2+), 50 μM ATP] per well. The 10 μL reactions are stopped with 10 μL of stop mix [50 mM EDTA, 3.0 mg/mL streptavidin-coupled SPA Imaging Beadsin Dulbecco's PBS (without Mg2+ and Ca2+), 50 μM ATP] per well. Plates are sealed, spun at 500 × g for 1 min or settled overnight, and counted in Packard TopCount for 30 s/well or imaged with a Viewlux imager. Signal above background (EDTA controls) is converted to percent inhibition relative to that obtained in control (DMSO-only) wells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Assays are carried out and data analyzed. In these assays, H460 cells are plated at a density of 2,000 per well, HDF cells are plated at 5,000 per well, and the drug-resistant cell line MES-SA/DX5 and its sensitive parent line MES-SA are plated at 7,000 and 6,000 per well, respectively, in a 96-well plate. These densities allowed vehicle controls to grow logarithmically during the course of the 3-day assay. All cells are exposed to 3-fold dilutions of the compound (30-0.00152 μM) in low-glucose DMEM containing 5% FBS, 50 μg/mL gentamicin, and 0.3% (v/v) DMSO (HDF cells); RPMI 1640 containing 5% FBS, 50 μg/mL gentamicin, and 0.3% (v/v) DMSO (H460); or McCoy's 5A containing 5% FBS, 50 μg/mL gentamicin, and 0.3% (v/v) DMSO (MES-SA and MES-SA/DX5)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (286 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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取扱説明書 (2659 KB)
参考文献
[1]. Lansing TJ, et al. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol Cancer Ther. 2007 Feb;6(2):450-9. Epub 2007 Jan 31. [Content Brief]
[2]. Didier C, et al. Evaluation of Polo-like Kinase 1 inhibition on the G2/M checkpoint in Acute Myelocytic Leukaemia. Eur J Pharmacol. 2008 Sep 4;591(1-3):102-5. [Content Brief]
[3]. Ikezoe T, et al. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76. [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 | 2.0944 mL | 10.4721 mL | 20.9442 mL | 52.3604 mL |
| 5 mM | 0.4189 mL | 2.0944 mL | 4.1888 mL | 10.4721 mL | |
| 10 mM | 0.2094 mL | 1.0472 mL | 2.0944 mL | 5.2360 mL | |
| 15 mM | 0.1396 mL | 0.6981 mL | 1.3963 mL | 3.4907 mL | |
| 20 mM | 0.1047 mL | 0.5236 mL | 1.0472 mL | 2.6180 mL | |
| 25 mM | 0.0838 mL | 0.4189 mL | 0.8378 mL | 2.0944 mL | |
| 30 mM | 0.0698 mL | 0.3491 mL | 0.6981 mL | 1.7453 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5236 mL | 1.3090 mL | |
| 50 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 mL | |
| 60 mM | 0.0349 mL | 0.1745 mL | 0.3491 mL | 0.8727 mL |
GW843682X 関連分類
HY-11003 関連分類
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