Y15
Based on 29 publication(s) in Google Scholar
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
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- 純度: 98.0%
- CAS 番号: 4506-66-5
- 分子式: C6H14Cl4N4
- 分子量:284.01
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保管条件:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Y15
More- Nat Commun. 2025 Mar 31;16(1):3093. [Abstract]
- J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]
- Autophagy. 2025 Mar;21(3):664-673. [Abstract]
- Adv Sci (Weinh). 2024 Nov 8:e2405705. [Abstract]
- Neuro Oncol. 2024 Jan 5;26(1):137-152. [Abstract]
- J Adv Res. 2025 Nov 19:S2090-1232(25)00929-4. [Abstract]
- Carbohydr Polym. 2026 Feb 15:374:124706. [Abstract]
- NPJ Precis Oncol. 2023 Aug 11;7(1):74. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2021;11(3):683-696. [Abstract]
- Stem Cell Res Ther. 2021 Oct 7;12(1):523. [Abstract]
- Cell Biosci. 2025 Oct 31;15(1):150. [Abstract]
- Atherosclerosis. 2023 Jul:377:43-59. [Abstract]
- ACS Biomater Sci Eng. 2024 Jul 8;10(7):4463-4479. [Abstract]
- Front Cell Dev Biol. 2021 May 28:9:607001. [Abstract]
- FASEB J. 2024 May 31;38(10):e23698. [Abstract]
- Exp Neurol. 2024 Jun:376:114776. [Abstract]
- J Hypertens. 2022 Sep 1;40(9):1666-1681. [Abstract]
- Acta Biochim Biophys Sin (Shanghai). 2018 Oct 1;50(10):976-983. [Abstract]
- Am J Cancer Res. 2023 May 15;13(5):1718-1743. [Abstract]
- Biomed Res Int. 2021 Mar 1:2021:6685493. [Abstract]
- Exp Ther Med. 2020 Aug;20(2):1405-1414. [Abstract]
- Biochem Biophys Res Commun. 2025 Apr 10:763:151788. [Abstract]
- Comp Biochem Physiol A Mol Integr Physiol. 2020 Mar;241:110639. [Abstract]
- Reprod Dev Med. October 27, 2022.
- bioRxiv. 2025 May 14:2025.05.12.653281. [Abstract]
- Patent. US20240100051A1
- bioRxiv. 2023 Feb 5.
- Patent. US20200383981A1.
- Oncotarget. 2017 Oct 5;8(56):95586-95595. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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IP
生物活性
FAK[1]
Y15 directly blocks autophosphorylation activity of FAK. Y15 inhibits Y397 phosphorylation of FAK starting at 0.1 μM in Panc-1 cells. At a dose of 100 μM, Y15 has the same or better inhibition as TAE226. Of note, total FAK is downregulated at higher doses of Y15. Y15 also blocks phosphorylation of the FAK downstream substrate, paxillin. Total paxillin is decreased at higher doses similar to FAK. Thus, Y15 inhibits FAK phosphorylation in a dose-dependent manner[1]. MTS assay is completed using a range of Y15 doses on all cell lines (TT, K1, BCPAP, and TPC1, respectively).Y15 inhibited cell viability in a dose-dependent manner across all thyroid cell lines evaluated. IC50 is 2.05, 5.74, 9.99, and 17.54 μM for TT, TPC1, BCPAP, and K1, respectively[2].
In macrophages treated with Y15, the filopodia and lamellipodia remain mobile. The lawn of particles surrounding macrophages appeared larger in cells treated with Y15[4].
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.
化学情報
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CAS 番号 4506-66-5
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性状 Solid
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分子量 284.01
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分子式 C6H14Cl4N4
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Color Off-white to gray
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SMILES
[H]Cl.[H]Cl.[H]Cl.[H]Cl.NC1=CC(N)=C(N)C=C1N
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別名
FAK Inhibitor 14; 1,2,4,5-ベンゼンテトラアミン·4塩酸塩
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
Publications (29)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 Mar 31;16(1):3093. PMID: 40164597
Y15 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 31;16(1):3093. [Abstract]
Y15 (100 μg/kg). Expression levels of bone formation-related proteins (Runx2/ALP/OPN/OCN) in peri-implant bone tissue after 2 weeks of treatment with different antagonists/inhibitors.
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J Extracell Vesicles
Exomeres From Adventitial Fibroblasts of Spontaneously Hypertensive Rats Promote Vascular Remodelling via Transferring Osteopontin. [Abstract]2025 Aug;14(8):e70146. PMID: 40767027
Y15 purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146. [Abstract]
The effects of FAK inhibitor Y15 (2.5 µM; bar chart 3), PI3K inhibitor LY294002 (5 µM), or AKT inhibitor AKTi1/2 (0.5 µM) on S-EMs-induced VSMC proliferation and migration. S-EMs (40 µg/mL) were administered 2 hours after inhibitor application. VSMC proliferation and migration were assessed by the percentage of EdU-positive cells and Boyden chamber assays.
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Autophagy
Deciphering melanophagy: role of the PTK2-ITCH-MLANA-OPTN cascade on melanophagy in melanocytes. [Abstract]2025 Mar;21(3):664-673. PMID: 39477686
Y15 purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar;21(3):664-673. [Abstract]
B16F1/TPC2-mRFP-EGFP cells stimulated with α-MSH were treated with TCTE (10 μg/ml) and Y15 (1.5 μM) for 24 hours. The cells were then fixed and imaged using a confocal microscope.
Y15 purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar;21(3):664-673. [Abstract]
α-MSH-stimulated B16F1 cells were cotreated with TCTE (10 μg/ml) and PTK2 inhibitor Y15 (1.5 μM) for 24 h. Then, the cells were harvested and analyzed by western blotting with indicated antibodies.
Y15 purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar;21(3):664-673. [Abstract]
α-MSH-stimulated B16F1 cells were cotransfected with HA-UBC and MLANA-Flag. After 1 day, the cells were further treated with α-MSH (1 μM) for 48 h and exposed to TCTE (10 μg/ml) with Y15 (1.5 μM) or DC (25 μM) for 24 h. Then, the cells were further treated with MG132 (10 μM) for 4 h and pulled down with anti-Flag antibody conjugated with agarose beads. The immunoprecipitates were analyzed by western blotting with indicated antibodies.
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Adv Sci (Weinh)
Piezo1 Regulates Stiffness-Dependent DRG Axon Regeneration via Modifying Cytoskeletal Dynamics. [Abstract]2024 Nov 8:e2405705. PMID: 39514408 -
Neuro Oncol
A disintegrin and metalloproteinase 22 activates integrin β1 through its disintegrin domain to promote the progression of pituitary adenoma. [Abstract]2024 Jan 5;26(1):137-152. PMID: 37555799 -
J Adv Res
Dysregulated ITGA3/FAK/YAP axis mediates impaired alveolar type II epithelial cells function in COPD. [Abstract]2025 Nov 19:S2090-1232(25)00929-4. PMID: 41270956 -
Carbohydr Polym
Decoding the pharmacokinetics of intravenous lentinan: A multiscale journey from the blood to hepatic Kupffer cells' lysosomes. [Abstract]2026 Feb 15:374:124706. PMID: 41371850 -
NPJ Precis Oncol
Chimeric antibody targeting unique epitope on onco-mucin16 reduces tumor burden in pancreatic and lung malignancies. [Abstract]2023 Aug 11;7(1):74. PMID: 37567918 -
Cell Mol Gastroenterol Hepatol
2021;11(3):683-696. PMID: 33075564 -
Stem Cell Res Ther
Regulation of the integrin αVβ3- actin filaments axis in early osteogenesis of human fibroblasts under cyclic tensile stress. [Abstract]2021 Oct 7;12(1):523. PMID: 34620239 -
Cell Biosci
FAK-dependent activation of src family kinase member BLK contributed to endometrial fibrosis via endoplasmic reticulum stress. [Abstract]2025 Oct 31;15(1):150. PMID: 41174819 -
Atherosclerosis
SIRT3-and FAK-mediated acetylation-phosphorylation crosstalk of NFATc1 regulates Nε-carboxymethyl-lysine-induced vascular calcification in diabetes mellitus. [Abstract]2023 Jul:377:43-59. PMID: 37392543 -
ACS Biomater Sci Eng
Hydroxyapatite Nanoparticles Promote the Development of Bone Microtissues for Accelerated Bone Regeneration by Activating the FAK/Akt Pathway. [Abstract]2024 Jul 8;10(7):4463-4479. PMID: 38848471 -
Front Cell Dev Biol
Hepatoma Cell-Derived Extracellular Vesicles Promote Liver Cancer Metastasis by Inducing the Differentiation of Bone Marrow Stem Cells Through microRNA-181d-5p and the FAK/Src Pathway. [Abstract]2021 May 28:9:607001. PMID: 34124029 -
FASEB J
FOXS1 acts as an oncogene and induces EMT through FAK/PI3K/AKT pathway by upregulating HILPDA in prostate cancer. [Abstract]2024 May 31;38(10):e23698. PMID: 38780613 -
Exp Neurol
LAMC1 attenuates neuronal apoptosis via FAK/PI3K/AKT signaling pathway after subarachnoid hemorrhage. [Abstract]2024 Jun:376:114776. PMID: 38609046 -
J Hypertens
WNT1-inducible signalling pathway protein 1 stabilizes atherosclerotic plaques in apolipoprotein-E-deficient mice via the focal adhesion kinase/mitogen-activated extracellular signal-regulated kinase/extracellular signal-regulated kinase pathway. [Abstract]2022 Sep 1;40(9):1666-1681. PMID: 35881419 -
Acta Biochim Biophys Sin (Shanghai)
Insulin-like growth factor 1 receptor signaling regulates embryonic epicardial cell proliferation through focal adhesion kinase pathway. [Abstract]2018 Oct 1;50(10):976-983. PMID: 30184089 -
Am J Cancer Res
Linc00662 m6A promotes the progression and metastasis of pancreatic cancer by activating focal adhesion through the GTF2B-ITGA1-FAK pathway. [Abstract]2023 May 15;13(5):1718-1743. PMID: 37293163 -
Biomed Res Int
Focal Adhesion Kinase Inhibitor Inhibits the Oxidative Damage Induced by Central Venous Catheter via Abolishing Focal Adhesion Kinase-Protein Kinase B Pathway Activation. [Abstract]2021 Mar 1:2021:6685493. PMID: 33748278 -
Exp Ther Med
Collagen triple helix repeat containing 1 promotes endometrial cancer cell migration by activating the focal adhesion kinase signaling pathway. [Abstract]2020 Aug;20(2):1405-1414. PMID: 32742375 -
Biochem Biophys Res Commun
FAK regulates trophoblast functions of invasion and proliferation through Rap1 pathway in early-onset preeclampsia. [Abstract]2025 Apr 10:763:151788. PMID: 40220488 -
Comp Biochem Physiol A Mol Integr Physiol
Focal adhesion kinase and osmotic responses in ionocytes of Fundulus heteroclitus, a euryhaline teleost fish. [Abstract]2020 Mar;241:110639. PMID: 31863842 -
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bioRxiv
Epithelial eversion, a collective rearrangement from apical-in to apical-out polarity, is initiated by α6β4 integrins and sustained by increased cell proliferation and anchorage-independence. [Abstract]2025 May 14:2025.05.12.653281. PMID: 40463241 -
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Oncotarget
Collagen I promotes hepatocellular carcinoma cell proliferation by regulating integrin β1/FAK signaling pathway in nonalcoholic fatty liver. [Abstract]2017 Oct 5;8(56):95586-95595. PMID: 29221151
溶剤 & 溶解度
H2O : 50 mg/mL (176.05 mM; ultrasonic and warming and heat to 50°C)
DMSO : 25 mg/mL (88.03 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (8.80 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 (8.80 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 10 mg/mL (35.21 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
プロトコル
10 μCi of [γ-32P]-ATP in a kinase buffer 20 mM HEPES, pH 7.4, 5 mM MgCl2, 5 mM MnCl2, 0.1 mM Na3VO4 with 0.1 μg of purified FAK protein are incubated in a kinase buffer with 10 μCi of [γ-32P]-ATP. The kinase reaction is performed for 5 minutes at room temperature and stopped by addition of 2× Laemmli buffer. Proteins are separated on a Ready SDS-10% PAGE gel, and the phosphorylated enolase is visualized by autoradiography[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The cells are treated with Y15 or TAE226 at different concentrations for 24 hours. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium compound from Promega Viability kit is added, and the cells are incubated at 37°C for 1-2 hours. The optical density on 96-plate is analyzed with a microplate reader at 490 nm to determine cell viability. In addition, cells are stained with trypan blue after 24 hours of treatment with Y15 and the percent of cells that stained positive are determined with a hemacytometer[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Six-week-old, female nude mice are used. 5×106 Panc si5-IGF-1R cells are mixed with matrigel and injected subcutaneously into the flank of athymic nude mice (day 0). Animals are randomly divided into two groups on day 7. One group (n=5) received Y15 (30 mg/kg) and the other received PBS as control treatment (n=5). For Panc si-ctrl xenografts, 5×106 Panc si-ctrl cells are mixed with matrigel and injected subcutaneously into the flank of nude mice. These animals are also randomly divided into two groups on day 7, and one group (n=5) received TAE226 (30 mg/kg), the other group received PBS (n=5) as control treatment. The drugs and PBS are administered through intraperitoneal injection in a total volume of 0.1 mL. Tumor sizes are measured every 3 or 4 d in length (mm)×width (mm) starting from day 10. Tumor volume is calculated as volume (cm3)= 1/2×length (cm)×width(cm)2.
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 (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hochwald SN, et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle. 2009 Aug;8(15):2435-43. [Content Brief]
[2]. O'Brien S, et al. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59. [Content Brief]
[3]. Zheng D, et al. A novel strategy to inhibit FAK and IGF-1R decreases growth of pancreatic cancer xenografts. Mol Carcinog. 2010 Feb;49(2):200-9. [Content Brief]
[4]. Xuchen Hu, et al. Release of cholesterol-rich particles from the macrophage plasma membrane during movement of filopodia and lamellipodia. Elife. 2019 Sep 5;8:e50231. [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, 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 / H2O | 1 mM | 3.5210 mL | 17.6050 mL | 35.2100 mL | 88.0251 mL |
| 5 mM | 0.7042 mL | 3.5210 mL | 7.0420 mL | 17.6050 mL | |
| 10 mM | 0.3521 mL | 1.7605 mL | 3.5210 mL | 8.8025 mL | |
| 15 mM | 0.2347 mL | 1.1737 mL | 2.3473 mL | 5.8683 mL | |
| 20 mM | 0.1761 mL | 0.8803 mL | 1.7605 mL | 4.4013 mL | |
| 25 mM | 0.1408 mL | 0.7042 mL | 1.4084 mL | 3.5210 mL | |
| 30 mM | 0.1174 mL | 0.5868 mL | 1.1737 mL | 2.9342 mL | |
| 40 mM | 0.0880 mL | 0.4401 mL | 0.8803 mL | 2.2006 mL | |
| 50 mM | 0.0704 mL | 0.3521 mL | 0.7042 mL | 1.7605 mL | |
| 60 mM | 0.0587 mL | 0.2934 mL | 0.5868 mL | 1.4671 mL | |
| 80 mM | 0.0440 mL | 0.2201 mL | 0.4401 mL | 1.1003 mL | |
| H2O | 100 mM | 0.0352 mL | 0.1761 mL | 0.3521 mL | 0.8803 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Y15 関連分類
HY-12444 関連分類
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