Copanlisib NEW
| Price | $32 | $47 | $72 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-16 |
Product Details
| Product Name: Copanlisib | CAS No.: 1032568-63-0 |
| Purity: 99.88% | Supply Ability: 10g |
| Release date: 2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | Copanlisib |
| 描述 | Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents. |
| 細(xì)胞實(shí)驗(yàn) | Cell proliferation over a 72-hour period is determined using the CellTiter-Glo? luminescent cell viability kit. Briefly, cells are plated in separate microtiter plates. Following an overnight incubation at 37oC, luminescence values in the t=0 hour plates are determined. Test compounds diluted in growth medium are added to the t=72 hour plates, and the cells are then incubated for 72 hours at 37oC. Luminescence values are determined with a Wallac 1420 Victor2? 1420 multilabel HTS counter after a 10-minute reaction with CellTiter-Glo? solution. The percentage inhibition of cell growth is calculated by subtracting the luminescence values in the t=0 hour plates from the corresponding values in the t=72 hour plates. Differences in values between drug-treated cells and controls are used to determine the percentage inhibition of cell growth.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Biochemical lipid kinase assays: The effect of BAY 80-6946 on PI3Kα, PI3Kβ, and PI3Kγ activity is measured by the inhibition of 33P incorporation into phosphatidylinositol (PI) in 384-well MaxiSorp? plates coated with 2 μg/well of PI and phosphatidylserine (PS) (1:1 molar ratio). In each PI3K isoform assay, 9 μL of reaction buffer (50 mM MOPSO, pH 7.0, 100 mM NaCl, 4 mM MgCl2, 0.1% BSA) containing 7.5 ng of His-tagged N-terminal truncated p110α or p110β protein, or 25 ng of purified human p110γ protein, is used. The reaction is started by adding 5 μL of a 40-μM ATP solution containing 20 μCi/mL [33>/sup>P]-ATP. After 2 hours incubation at room temperature, the reaction is terminated by addition of 5 μL of a 25-mM EDTA solution. The plates are washed and Ultima Gold? scintillation cocktail (25 μL) is then added. The radioactivity incorporated into the immobilized PI substrate is determined with a BetaPlate Liquid Scintillation Counter. |
| 體外活性 | In both KPL4 cells and LPA-stimulated PC3 cells, Copanlisib reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, Copanlisib shows antiproliferative activity and induces apoptosis. [1] The combination of HER2-targeted therapies and Copanlisib inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells. [2] |
| 體內(nèi)活性 | In rat KPL4 or HCT116 tumor xenograft model, Copanlisib (6 mg/kg, i.v.) induces 100% complete tumor regression. In nude mice with Lu7860 erlotinib-resistant, patient-derived NSCLC and MAXF1398 patient-derived luminal breast tumor models, Copanlisib (14 mg/kg, i.v.) also causes tumor growth inhibition. [1] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : < 1 mg/mL (insoluble or slightly soluble) H2O : Insoluble 0.01M HCl : 10 mg/mL (20.81 mM), Sonication is recommended. |
| 關(guān)鍵字 | PI3K | Apoptosis | antiproliferative | antitumor | Inhibitor | administration | phosphorylation | sub-nanomolar | AKT | Phosphoinositide 3-kinase | inhibit | Copanlisib | intravenous |
| 相關(guān)產(chǎn)品 | Stavudine | Sodium 4-phenylbutyrate | Tributyrin |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | FDA 上市藥物庫 | 抗癌上市藥物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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