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Copanlisib
別名: BAY 80-6946 中文名稱：庫潘尼西
Copanlisib是一個高效的泛I型 PI3K抑制劑，其對PI3Kα/β/γ/δ抑制的IC50分別為0.5, 3.7, 6.4, and 0.7 nM。Phase 3。此產(chǎn)品溶解度不佳，動物實驗可用，細胞實驗請謹(jǐn)慎選擇！
Copanlisib Chemical Structure
CAS: 1032568-63-0
產(chǎn)品質(zhì)控
批次：
純度：
99.97%
99.97
常與Copanlisib一起在實驗中被使用的化合物
Copanlisib和Darolutamide通過強烈誘導(dǎo)細胞凋亡和防止促凋亡基因下調(diào)，抑制體外前列腺癌模型的增殖。
Sugawara T, et al. Cancer Res (2022) 82 (12_Supplement): 651.
Copanlisib和Tazemetostat聯(lián)合使用可在Calu3、Sw1573和所有BEAS2B細胞系中誘導(dǎo)較高的PIK3IP1表達。
Copanlisib和Anetumab ravtansine組合顯示體外OVCAR-3和OVCAR-8細胞系細胞凋亡增加。
Quanz M, et al. Oncotarget. 2018 Sep 25; 9(75): 34103–34121.
Copanlisib聯(lián)合Venetoclax可通過下調(diào)BCL-XL/MCL1基因誘導(dǎo)MCL和MZL細胞凋亡。
Copanlisib和Abemaciclib聯(lián)合療法可有效克服venetoclax耐藥性，成為未來難治性/復(fù)發(fā)患者的有效治療方案。
Copanlisib相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Copanlisib是一個高效的泛I型 PI3K抑制劑，其對PI3Kα/β/γ/δ抑制的IC50分別為0.5, 3.7, 6.4, and 0.7 nM。Phase 3。此產(chǎn)品溶解度不佳，動物實驗可用，細胞實驗請謹(jǐn)慎選擇！ | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | BAY 80-6946是PI3K抑制劑，具有抗腫瘤活性。BAY 86-9766抑制HuCCT-1 (KRASG12D) 和EGI-1 (KRASG12D) 細胞系增殖，IC50分別為147 nM 和137 nM。[2] |
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|---|---|---|---|---|
| 激酶實驗 | PI3Kα和PI3Kβ放射性脂質(zhì)激酶檢測 | |||
| p110α生化檢測是一種放射性測定，測量33P滲透進p110α底物磷脂酰肌醇（PI）的程度。His標(biāo)記的N-末端截短的(ΔN 1-108) p110α和同樣截短的缺乏p85結(jié)合域的p110β(ΔN 1-108) 蛋白在Sf9細胞中表達，且純化到50%以上純度。為了獲得 IC50值,使用 MaxiSorp 板在以下條件下在384孔板中進行反應(yīng)。每孔使用2 μg在氯仿稀釋的摩爾比為1:1的磷脂酰肌醇（PI）和磷脂酰絲氨酸（PS）包被實驗板。將實驗板置于通風(fēng)櫥中過夜，蒸發(fā)有機溶液。將實驗板密封在4°C貯存1個月。每孔加入7.5 ng截短的p110α蛋白，每孔中含9 μL 實驗 buffer (50mM MOPSO pH 7.0,100 mM NaCl, 4mM MgCl2, 0.1%(w/v)BSA)，除了對照組只含實驗 buffer。1μL 溶于DMSO的實驗化合物從稀釋液中轉(zhuǎn)移，獲得8點劑量反應(yīng) (0.0, 0.003, 0.01, 0.03, 0.1, 0.3, 1.0, 3.0 和 10 μM 終濃度BAY化合物)。加入含 20 μCi/mL [γ-33P]-ATP 的40 μM ATP 溶液開始反應(yīng)，反應(yīng)在室溫下溫和混合進行2小時。 加入 5μL 25 mM EDTA儲存液終止反應(yīng)。不使用洗滌劑清洗實驗板，而使用384孔實驗板洗滌器，然后每孔加入25μL UltimaGold 閃爍使用BetaPlate液體閃爍計數(shù)器測定滲透進固定化PI底物的放射性。 | ||||
| 細胞實驗 | 細胞系 | KPL4, BT474, T47D, BT20, MCF7, MDA-MB-468, SK-Br-3, LNCaP, PC3, Colo205, HT29, HCT116, A549, H460, U87MG, 786O. | ||
| 濃度 | 0.0, 0.003, 0.01, 0.03, 0.1, 0.3, 1.0, 3.0 和 10 μM | |||
| 孵育時間 | 72 小時 | |||
| 方法 | 藥物處理72小時后，使用Cell Titer-Glo 發(fā)光法細胞活力檢測試劑盒測定細胞增殖。細胞按每孔500-1000個細胞接種到 384孔板中，孔中含 25 μL 生長培養(yǎng)基。對于每種細胞系的測定，細胞接種到單獨的實驗板上，在t=0小時和t=72小時測定發(fā)光值。在37°C下溫育過夜，每孔加入25μL Cell Titer-Glo 溶液測定t=0時樣品的發(fā)光值，轉(zhuǎn)移實驗板到搖床上，在室溫下進行10分鐘，然后使用發(fā)光檢測儀（最大光檢測在428 nm處測定）在Wallac Victor2 1420 Multilable HTS計數(shù)板上對實驗板進行讀數(shù)。使用在生長培養(yǎng)基中稀釋的化合物（終體積為30 μL）處理t=72小時的劑量板。細胞在37°C下溫育72小時。每孔加入30μL Cell Titer-Glo溶液測定t=72小時樣品的發(fā)光值，然后將細胞置于搖床上在室溫下進行10分鐘，然后使用Victor發(fā)光檢測儀讀讀取發(fā)光值。進行數(shù)據(jù)處理，實驗組和對照組中t=72小時發(fā)光值減去t=0時發(fā)光值。實驗組和對照組的發(fā)光值百分比差異用來測定生長抑制百分?jǐn)?shù)。 |
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| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | 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 |
|
24436048 | |
| Growth inhibition assay | Cell viability |
|
24436048 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | BAY 80-6946 耐受性良好，MTD(最大耐受劑量)為0.8 mg/kg。PK（藥代動力學(xué)）研究結(jié)果支持每周給藥。按MTD處理，在第一個24小時期間出現(xiàn)2/3級高血糖。PK, 臨床SD和FDG-PET 數(shù)據(jù)與有效處理和PI3K 通路抑制情況一致。[1] |
|
|---|---|---|
| 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 |
化學(xué)信息&溶解度
| 分子量 | 480.52 | 分子式 | C23H28N8O4 |
| CAS號 | 1032568-63-0 | SDF | Download Copanlisib SDF |
| Smiles | COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
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) |
摩爾濃度計算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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