Copanlisib
别名: BAY 80-6946 中文名称：库潘尼西
Copanlisib是一个高效的泛I型 PI3K抑制剂，其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3。此产品溶解度不佳，动物实验可用，细胞实验请谨慎选择！
Copanlisib Chemical Structure
CAS: 1032568-63-0
产品质控
批次：
纯度：
99.97%
99.97
常与Copanlisib一起在实验中被使用的化合物
Copanlisib和Darolutamide通过强烈诱导细胞凋亡和防止促凋亡基因下调，抑制体外前列腺癌模型的增殖。
Sugawara T, et al. Cancer Res (2022) 82 (12_Supplement): 651.
Copanlisib和Tazemetostat联合使用可在Calu3、Sw1573和所有BEAS2B细胞系中诱导较高的PIK3IP1表达。
Copanlisib和Anetumab ravtansine组合显示体外OVCAR-3和OVCAR-8细胞系细胞凋亡增加。
Quanz M, et al. Oncotarget. 2018 Sep 25; 9(75): 34103–34121.
Copanlisib联合Venetoclax可通过下调BCL-XL/MCL1基因诱导MCL和MZL细胞凋亡。
Copanlisib和Abemaciclib联合疗法可有效克服venetoclax耐药性，成为未来难治性/复发患者的有效治疗方案。
Copanlisib相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| BT-474 | Function assay | 50 nM | 0.5, 2, 4, 8, 24 h | rapidly inhibits the phosphorylation of AKT (S473, T308) as well as its direct substrates PRAS40 (T246) and GSK3β (S9), and inhibition was sustained for up to 24 hours | 24436048 |
| HepG2 | Growth inhibiton assay | 100 nM | Copanlisib dose-dependently inhibited cell growth in vitro. IC50=31.6 nM. | 30962952 | |
| Huh7 | Growth inhibiton assay | 100 nM | Copanlisib dose-dependently inhibited cell growth in vitro. IC50=47.9 nM. | 30962952 | |
| MCF-7 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| BT-20 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| MDA-MB-361 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| MDA-MB-453 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| HCC-1954 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| UACC-893 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| SK-BR-3 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| JVM-3 | Function assay | 48 h | inhibits metabolic activity with an IC50 of 2 μM in the XTT assay | 25912635 | |
| T-47D | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| HCC1806 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| NCI-H292 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| NCI-H1650 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| CCRF-SB | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| U937 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| SU-DHL-4 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| SU-DHL-5 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| HCT116 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| A549 cells | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| SK-MEL-30 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| SK-MEL-2 cells | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| NCI-H1703 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| NCI-H661 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| PC9 | Function assay | 0, 1, 2, 4 h | downregulation of P-AKT | 24436048 | |
| Chang | Growth inhibiton assay | IC50=442 nM | 30962952 | ||
| PLCPRF5 | Growth inhibiton assay | IC50=283 nM | 30962952 | ||
| Hep3B | Growth inhibiton assay | IC50=72.4 nM | 30962952 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Copanlisib是一个高效的泛I型 PI3K抑制剂，其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3。此产品溶解度不佳，动物实验可用，细胞实验请谨慎选择！ | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | BAY 80-6946是PI3K抑制剂，具有抗肿瘤活性。BAY 86-9766抑制HuCCT-1 (KRASG12D) 和EGI-1 (KRASG12D) 细胞系增殖，IC50分别为147 nM 和137 nM。[2] |
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|---|---|---|---|---|
| 激酶实验 | PI3Kα和PI3Kβ放射性脂质激酶检测 | |||
| p110α生化检测是一种放射性测定，测量33P渗透进p110α底物磷脂酰肌醇（PI）的程度。His标记的N-末端截短的(ΔN 1-108) p110α和同样截短的缺乏p85结合域的p110β(ΔN 1-108) 蛋白在Sf9细胞中表达，且纯化到50%以上纯度。为了获得 IC50值,使用 MaxiSorp 板在以下条件下在384孔板中进行反应。每孔使用2 μg在氯仿稀释的摩尔比为1:1的磷脂酰肌醇（PI）和磷脂酰丝氨酸（PS）包被实验板。将实验板置于通风橱中过夜，蒸发有机溶液。将实验板密封在4°C贮存1个月。每孔加入7.5 ng截短的p110α蛋白，每孔中含9 μL 实验 buffer (50mM MOPSO pH 7.0,100 mM NaCl, 4mM MgCl2, 0.1%(w/v)BSA)，除了对照组只含实验 buffer。1μL 溶于DMSO的实验化合物从稀释液中转移，获得8点剂量反应 (0.0, 0.003, 0.01, 0.03, 0.1, 0.3, 1.0, 3.0 和 10 μM 终浓度BAY化合物)。加入含 20 μCi/mL [γ-33P]-ATP 的40 μM ATP 溶液开始反应，反应在室温下温和混合进行2小时。 加入 5μL 25 mM EDTA储存液终止反应。不使用洗涤剂清洗实验板，而使用384孔实验板洗涤器，然后每孔加入25μL UltimaGold 闪烁使用BetaPlate液体闪烁计数器测定渗透进固定化PI底物的放射性。 | ||||
| 细胞实验 | 细胞系 | KPL4, BT474, T47D, BT20, MCF7, MDA-MB-468, SK-Br-3, LNCaP, PC3, Colo205, HT29, HCT116, A549, H460, U87MG, 786O. | ||
| 浓度 | 0.0, 0.003, 0.01, 0.03, 0.1, 0.3, 1.0, 3.0 和 10 μM | |||
| 孵育时间 | 72 小时 | |||
| 方法 | 药物处理72小时后，使用Cell Titer-Glo 发光法细胞活力检测试剂盒测定细胞增殖。细胞按每孔500-1000个细胞接种到 384孔板中，孔中含 25 μL 生长培养基。对于每种细胞系的测定，细胞接种到单独的实验板上，在t=0小时和t=72小时测定发光值。在37°C下温育过夜，每孔加入25μL Cell Titer-Glo 溶液测定t=0时样品的发光值，转移实验板到摇床上，在室温下进行10分钟，然后使用发光检测仪（最大光检测在428 nm处测定）在Wallac Victor2 1420 Multilable HTS计数板上对实验板进行读数。使用在生长培养基中稀释的化合物（终体积为30 μL）处理t=72小时的剂量板。细胞在37°C下温育72小时。每孔加入30μL Cell Titer-Glo溶液测定t=72小时样品的发光值，然后将细胞置于摇床上在室温下进行10分钟，然后使用Victor发光检测仪读读取发光值。进行数据处理，实验组和对照组中t=72小时发光值减去t=0时发光值。实验组和对照组的发光值百分比差异用来测定生长抑制百分数。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-AKT / AKT / p-PRAS40(T246) / p-GSK3β(S9) / cleaved caspase-3 / cleaved caspase-7 / PI3K-p85 p-FoxO4(T28) / p-S6(S235/236) / p-4E-BP1(S65) / p-4E-BP1(T37/46) / p-HER3(Y1197) / HER3 / p-IGF1Rβ/ IGF1R / p-HER2 / p-EGFR / p-STAT3 / p-ERK |
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24436048 | |
| Growth inhibition assay | Cell viability |
|
24436048 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | BAY 80-6946 耐受性良好，MTD(最大耐受剂量)为0.8 mg/kg。PK（药代动力学）研究结果支持每周给药。按MTD处理，在第一个24小时期间出现2/3级高血糖。PK, 临床SD和FDG-PET 数据与有效处理和PI3K 通路抑制情况一致。[1] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05082025 | Active not recruiting | Endometrial Cancer|Ovarian Cancer |
M.D. Anderson Cancer Center|Bayer |
September 27 2022 | Phase 2 |
| NCT05217914 | Active not recruiting | Relapsed or Refractory Indolent Non-Hodgkin Lymphoma |
Bayer |
July 1 2022 | -- |
| NCT04939272 | Suspended | Recurrent Mantle Cell Lymphoma|Refractory Mantle Cell Lymphoma |
City of Hope Medical Center|National Cancer Institute (NCI) |
June 29 2022 | Phase 1|Phase 2 |
| NCT04572763 | Active not recruiting | Diffuse Large B Cell Lymphoma|Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma |
Dana-Farber Cancer Institute|AbbVie|Bayer |
September 8 2021 | Phase 1|Phase 2 |
| NCT04803123 | Terminated | Leukemia Acute Lymphocytic |
Dorothy Sipkins MD PhD|Bayer|Duke University |
June 21 2021 | Early Phase 1 |
化学信息&溶解度
| 分子量 | 480.52 | 分子式 | C23H28N8O4 |
| CAS号 | 1032568-63-0 | SDF | Download Copanlisib SDF |
| Smiles | COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
5%TFA : 6.01 mg/mL (12.5 mM) Ethanol : 0.01 mg/mL (0.02 mM) Water : 0.002 mg/mL (0.0 mM) |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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