库潘尼西|T6322

Copanlisib
1032568-63-0

￥426 1mg 起订

￥613 2mg 起订

￥932 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 库潘尼西

英文名称：: Copanlisib

CAS号：: 1032568-63-0

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.88%

产品类别：: 抑制剂

货号：: T6322

Product Introduction

Bioactivity

名称	Copanlisib
描述	Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.
细胞实验	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)
激酶实验	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.
体外活性	在KPL4细胞和LPA刺激的PC3细胞中，Copanlisib降低pAKT水平。在一组存在PIK3CA突变和/或HER2过表达的人类癌症细胞系中，Copanlisib展示了抗增殖活性并诱导了凋亡。[1] HER2靶向疗法与Copanlisib的联合应用比单独使用任一疗法更有效地抑制增长，并能在细胞中恢复对trastuzumab和lapatinib的敏感性。[2]
体内活性	在大鼠KPL4或HCT116肿瘤异种移植模型中，Copanlisib（6 mg/kg，静脉注射）可诱导100%的完全肿瘤消退。在携带Lu7860厄洛替尼耐药、源自患者的非小细胞肺癌和MAXF1398源自患者的腺泡状乳腺肿瘤模型的裸鼠中，Copanlisib（14 mg/kg，静脉注射）同样可抑制肿瘤生长。[1]
存储条件	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.
关键字	PI3K \| Apoptosis \| antiproliferative \| antitumor \| Inhibitor \| administration \| phosphorylation \| sub-nanomolar \| AKT \| Phosphoinositide 3-kinase \| inhibit \| Copanlisib \| intravenous
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库潘尼西|||可泮利塞|||BAY 80-6946|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子