Copanlisib
Based on 36 publication(s) in Google Scholar
Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.
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- 純度: 99.35%
- CAS 番号: 1032568-63-0
- 分子式: C23H28N8O4
- 分子量:480.52
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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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生物活性
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化学情報
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溶剤 & 溶解度
- 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 Copanlisib
More- Signal Transduct Target Ther. 2025 Oct 31;10(1):356. [Abstract]
- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]
- Mol Cancer. 2023 Mar 30;22(1):64. [Abstract]
- Cancer Discov. 2025 Jan 13;15(1):202-226. [Abstract]
- Nat Cancer. 2024 Aug;5(8):1250-1266. [Abstract]
- Blood. 2019 Jan 3;133(1):70-80. [Abstract]
- Cancer Res. 2025 Dec 31. [Abstract]
- J Clin Invest. 2021 Dec 15;131(24):e140436. [Abstract]
- Theranostics. 2020 Jan 1;10(4):1531-1543. [Abstract]
- Carbohydr Polym. 2024 Feb 15:326:121637. [Abstract]
- J Immunother Cancer. 2022 Mar;10(3):e003402. [Abstract]
- Cancer Lett. 2022 Jan 1:524:151-160. [Abstract]
- Genes Dis. 2021 Jul 1;9(6):1650-1661. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Blood Adv. 2022 Apr 12;6(7):2346-2360. [Abstract]
- Br J Cancer. 2025 Oct 6. [Abstract]
- Cell Biosci. 2022 Dec 30;12(1):210. [Abstract]
- Cell Biosci. 2022 Aug 2;12(1):122. [Abstract]
- Cell Biosci. 2020 Feb 12;10:16. [Abstract]
- Front Immunol. 2021 Oct 15;12:699478. [Abstract]
- Mol Cancer Ther. 2025 Jul 10. [Abstract]
- Bioorg Chem. 2025 Apr 5:160:108424. [Abstract]
- RSC Adv. 2019 Feb 21;9(11):6409-6418. [Abstract]
- Cell Rep Methods. 2026 Jun 15;6(6):101339. [Abstract]
- FASEB J. 2026 Jun 15;40(11):e71954. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Sci Rep. 2025 Aug 10;15(1):29265. [Abstract]
- Front Oncol. 2022 Sep 8:12:944537. [Abstract]
- Front Oncol. 2021 Jul 13:11:704042. [Abstract]
- Mol Carcinog. 2024 Jul;63(7):1334-1348. [Abstract]
- Breast Cancer Res Treat. 2020 Jan;179(2):337-347. [Abstract]
- Technical University of Dresden. 2025.
- bioRxiv. 2025 Jan 16:2025.01.10.632413. [Abstract]
- Université de Lausanne. 2024 Feb 7.
- J Oncol. 2022 Apr 29;2022:1515416. [Abstract]
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Apoptosis Analysis
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RT-PCR
生物活性
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PI3Kα 0.5 nM (IC50) |
PI3Kδ 0.7 nM (IC50) |
PI3Kβ 3.7 nM (IC50) |
PI3Kγ 6.4 nM (IC50) |
mTOR 45 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.12 μM
Compound: Copanlisib
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Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
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[PMID: 32069401] |
| HCT-116 | IC50 |
0.13 μM
Compound: Copanlisib
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| HT-29 | IC50 |
0.93 μM
Compound: Copanlisib
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Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| HT-29 | IC50 |
0.95 μM
Compound: Copanlisib
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Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
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[PMID: 32069401] |
| HUVEC | IC50 |
34.75 μM
Compound: Copanlisib
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Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| HUVEC | IC50 |
35.42 μM
Compound: Copanlisib
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Cytotoxicity against HUVEC assessed as reduction in cell viability
Cytotoxicity against HUVEC assessed as reduction in cell viability
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[PMID: 32069401] |
| LoVo | IC50 |
0.053 μM
Compound: Copanlisib
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Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
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[PMID: 32069401] |
| LoVo | IC50 |
0.06 μM
Compound: Copanlisib
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Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
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[PMID: 36586298] |
| MCF7 | IC50 |
0.01 μM
Compound: Copanlisib
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Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
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[PMID: 32069401] |
Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab[1].
Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells[1].
Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC50 values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT20 breast cancer cells
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Concentration:20 nM and 62 nM, 200 nM
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Incubation Time:24 hours
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Result:Significantly increased caspase9 activities. Also increased levels of phosphorylated p53 at Ser15and cleaved PARP. Induced caspase-9 activation with an EC50 of 340 nM.
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Cell Line:ELT3 cells
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Concentration:0.5 nM, 5 nM, 50 nM, 500 nM
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Incubation Time:2 hours
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Result:Complete inhibition of PI3K-mediated AKT phosphorylation was clearly shown at a concentration of 5 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude rats injected with KPL4 tumor cells[1]
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Dosage:0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kg
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Administration:Intravenous injection; every second day, every third day; for 60 days
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Result:On day 25, tumor growth inhibition (TGI) rates of 77%, 84%, 99%, and 100% were observed at doses of 0.5, 1, 3, and 6 mg/kg, respectively. All rats remained tumor free at the termination of the study on day 73.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1032568-63-0
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性状 Solid
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分子量 480.52
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分子式 C23H28N8O4
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Color Off-white to yellow
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SMILES
O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25
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別名
BAY 80-6946
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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 (36)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Alpha-enolase influences ATP pool of cytoplasm and lactate homeostasis by regulating glycolysis in gastric cancer. [Abstract]2025 Oct 31;10(1):356. PMID: 41168198 -
Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Mol Cancer
Sulindac (K-80003) with nab-paclitaxel and gemcitabine overcomes drug-resistant pancreatic cancer. [Abstract]2024 Sep 30;23(1):215. PMID: 39350121
Copanlisib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]
Western blot analysis of Akt, p-Akt (Ser473), p-Akt (Thr308), and cleaved caspase 3/8 expression after 6 h of treatment with copanlisib (2 nM, pan-PI3K inhibitor) and GEM treatment.
Copanlisib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]
Colony formation by cells overexpressing cFAM124A after 6 h of treatment with different inhibitors and GEM treatment in 6-well dishes (800 cells/well) for 2 weeks. Each inhibitor, Copanlisib (2 nM, pan-PI3K inhibitor) or K-80003 (5 nM, tRXRα-dependent Akt activation inhibitor).
Copanlisib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]
Subcutaneous xenograft model of mice in the different groups treated with GEM (40 mg/kg i.p. 2×/week for 4 weeks), Copanlisib (1 mg/kg, iv. 2×/week for 4 weeks), or K-80003 (20 mg/ kg i.p. 2×/week for 4 weeks) at 2 weeks after subcutaneous injection of 5 × 106 cells overexpressing cFAM124A and control cells.
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Mol Cancer
CDK9 inhibition induces epigenetic reprogramming revealing strategies to circumvent resistance in lymphoma. [Abstract]2023 Mar 30;22(1):64. PMID: 36998071 -
Cancer Discov
Neuro-mesenchymal interaction mediated by a β2 adrenergic-nerve growth factor feedforward loop promotes colorectal cancer progression. [Abstract]2025 Jan 13;15(1):202-226. PMID: 39137067 -
Nat Cancer
A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. [Abstract]2024 Aug;5(8):1250-1266. PMID: 38992135 -
Blood
Targeted inhibition of PI3Kα/δ is synergistic with BCL-2 blockade in genetically defined subtypes of DLBCL. [Abstract]2019 Jan 3;133(1):70-80. PMID: 30322870
Copanlisib purchased from MedChemExpress. Usage Cited in: Blood. 2019 Jan 3;133(1):70-80. [Abstract]
Induction of apoptosis after 96-hour exposure to DMSO, Entospletinib (ENTO, 2 μM), Ibrutinib (IBRU, 0.1 μM), Copanlisib (COPA, 0.25 μM), or Pictilisib (PICTI, 0.5 μM) shown as percentage of annexin V/PI-positive cells plus or minus SEM from at least 3 biological replicates.
Copanlisib purchased from MedChemExpress. Usage Cited in: Blood. 2019 Jan 3;133(1):70-80. [Abstract]
HRK, BCL-xL, BFL-1, or BIM transcript abundance after 24-hour exposure to DMSO, Entospletinib (2 μM), Ibrutinib (0.1 μM), Copanlisib (0.25 μM), or Pictilisib (0.5 μM) was determined with RT-qPCR relative to PPIA.
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Cancer Res
2025 Dec 31. PMID: 41474982 -
J Clin Invest
WWP1 inactivation enhances efficacy of PI3K inhibitors while suppressing their toxicities in breast cancer models. [Abstract]2021 Dec 15;131(24):e140436. PMID: 34907909 -
Theranostics
Response to mTOR and PI3K inhibitors in enzalutamide-resistant luminal androgen receptor triple-negative breast cancer patient-derived xenografts. [Abstract]2020 Jan 1;10(4):1531-1543. PMID: 32042320 -
Carbohydr Polym
Inulin-like polysaccharide ABWW may impede CCl4 induced hepatic stellate cell activation through mediating the FAK/PI3K/AKT signaling pathway in vitro & in vivo. [Abstract]2024 Feb 15:326:121637. PMID: 38142102 -
J Immunother Cancer
PI3K activation allows immune evasion by promoting an inhibitory myeloid tumor microenvironment. [Abstract]2022 Mar;10(3):e003402. PMID: 35264433 -
Cancer Lett
EZH2 inhibition confers PIK3CA-driven lung tumors enhanced sensitivity to PI3K inhibition. [Abstract]2022 Jan 1:524:151-160. PMID: 34655667 -
Genes Dis
PGRN exacerbates the progression of non-small cell lung cancer via PI3K/AKT/Bcl-2 antiapoptotic signaling. [Abstract]2021 Jul 1;9(6):1650-1661. PMID: 36157487 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Blood Adv
Triple combination of BET plus PI3K and NF-κB inhibitors exhibit synergistic activity in adult T-cell leukemia/lymphoma. [Abstract]2022 Apr 12;6(7):2346-2360. PMID: 35030628 -
Br J Cancer
Bypassing cisplatin resistance in Nrf2 hyperactivated head and neck cancer through effective PI3Kinase targeting. [Abstract]2025 Oct 6. PMID: 41053162 -
Cell Biosci
Inhibition of PI3 kinase isoform p110α suppresses neuroblastoma growth and induces the reduction of Anaplastic Lymphoma Kinase. [Abstract]2022 Dec 30;12(1):210. PMID: 36585695 -
Cell Biosci
AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer. [Abstract]2022 Aug 2;12(1):122. PMID: 35918763 -
Cell Biosci
Loss of PI3 kinase association improves the sensitivity of secondary mutation of KIT to Imatinib. [Abstract]2020 Feb 12;10:16. PMID: 32082541 -
Front Immunol
"γδT Cell-IL17A-Neutrophil" Axis Drives Immunosuppression and Confers Breast Cancer Resistance to High-Dose Anti-VEGFR2 Therapy. [Abstract]2021 Oct 15;12:699478. PMID: 34721375 -
Mol Cancer Ther
2025 Jul 10. PMID: 40635161 -
Bioorg Chem
2025 Apr 5:160:108424. PMID: 40209351 -
RSC Adv
Reactive intermediates in copanlisib metabolism identified by LC-MS/MS: phase I metabolic profiling. [Abstract]2019 Feb 21;9(11):6409-6418. PMID: 35517257 -
Cell Rep Methods
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]2026 Jun 15;6(6):101339. PMID: 42134319 -
FASEB J
Polyphosphates Attenuate Interleukin-12 Production in Macrophages Infected With Legionella pneumophila. [Abstract]2026 Jun 15;40(11):e71954. PMID: 42219888 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
Sci Rep
Afatinib amplifies cAMP-induced fluid secretion in a mouse mini-gut model via TMEM16A-mediated fluid secretion and secretory cell differentiation. [Abstract]2025 Aug 10;15(1):29265. PMID: 40784986 -
Front Oncol
Co-administration of MDR1 and BCRP or EGFR/PI3K inhibitors overcomes lenvatinib resistance in hepatocellular carcinoma. [Abstract]2022 Sep 8:12:944537. PMID: 36158676 -
Front Oncol
Patient-Derived Xenograft Models for Intrahepatic Cholangiocarcinoma and Their Application in Guiding Personalized Medicine. [Abstract]2021 Jul 13:11:704042. PMID: 34327143 -
Mol Carcinog
Four and a half LIM domains 2 (FHL2) attenuates tumorigenesis of gastrointestinal stromal tumors (GISTs) by negatively regulating KIT signaling. [Abstract]2024 Jul;63(7):1334-1348. PMID: 38629424 -
Breast Cancer Res Treat
2020 Jan;179(2):337-347. PMID: 31655920 -
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bioRxiv
Bypassing cisplatin resistance in Nrf2 hyperactivated head and neck cancer through effective PI3Kinase targeting. [Abstract]2025 Jan 16:2025.01.10.632413. PMID: 39868226 -
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J Oncol
2022 Apr 29;2022:1515416. PMID: 35528239
溶剤 & 溶解度
1 M HCl : 100 mg/mL (208.11 mM; Need ultrasonic)
DMSO : 5 mg/mL (10.41 mM; ultrasonic and adjust pH to 5 with HCl; 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)
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: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (10.41 mM); Suspended solution; Need ultrasonic
純度とドキュメンテーション
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データシート (276 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)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
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 M HCl | 1 mM | 2.0811 mL | 10.4054 mL | 20.8108 mL | 52.0270 mL |
| 5 mM | 0.4162 mL | 2.0811 mL | 4.1622 mL | 10.4054 mL | |
| 10 mM | 0.2081 mL | 1.0405 mL | 2.0811 mL | 5.2027 mL | |
| 1 M HCl | 15 mM | 0.1387 mL | 0.6937 mL | 1.3874 mL | 3.4685 mL |
| 20 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 25 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0811 mL | |
| 30 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7342 mL | |
| 40 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 50 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0405 mL | |
| 60 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8671 mL | |
| 80 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL | |
| 100 mM | 0.0208 mL | 0.1041 mL | 0.2081 mL | 0.5203 mL |
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