2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Apoptosis
  4. Copanlisib

Copanlisib  (Synonyms: 库潘尼西; BAY 80-6946)

目录号: HY-15346 纯度: 99.50%
COA 产品使用指南

摩尔计算器

Copanlisib (BAY 80-6946) 是一种有效的，选择性的和 ATP 竞争性的泛 I 类 PI3K 抑制剂，对 PI3Kα，PI3Kδ，PI3Kβ 和 PI3Kγ 的 IC50 分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。除 mTOR 外，Copanlisib 对其他脂质和蛋白激酶的选择性超过 2000 倍。Copanlisib 具有优异的抗肿瘤活性。

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Copanlisib Chemical Structure

Copanlisib Chemical Structure

CAS No. : 1032568-63-0

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规格 价格 是否有货 数量
2 mg ￥750
In-stock
5 mg ￥1300
In-stock
10 mg ￥1650
In-stock
50 mg ￥4000
In-stock
100 mg ￥5700
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Copanlisib:

Copanlisib 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target[1]

PI3Kα

0.5 nM (IC50)

PI3Kδ

0.7 nM (IC50)

PI3Kβ

3.7 nM (IC50)

PI3Kγ

6.4 nM (IC50)

mTOR

45 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
0.12 μM
Compound: Copanlisib
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
[PMID: 32069401]
HT-29 IC50
0.95 μM
Compound: Copanlisib
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
[PMID: 32069401]
LoVo IC50
0.053 μM
Compound: Copanlisib
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
[PMID: 32069401]
MCF7 IC50
0.01 μM
Compound: Copanlisib
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
[PMID: 32069401]
体外研究
(In Vitro)

Copanlisib (BAY 80-6946；20 -200 nM；24 小时；BT20 乳腺癌细胞) 处理诱导对拉帕替尼和曲妥珠单抗耐药的肿瘤细胞系子集发生细胞凋亡[1]。
Copanlisib (BAY 80-6946；0.5-500 nM；2 小时；ELT3 细胞) 处理显示完全抑制 ELT3 细胞中 PI3K 介导的 AKT 磷酸化[1]。
Copanlisib 有效抑制一组人类肿瘤细胞系中的细胞增殖。Copanlisib 对具有 PIK3CA 激活突变的细胞系的平均 IC50 值为 19 nM，对 HER2 阳性细胞系的平均 IC50 值为 17 nM，而在 PIK3CA 野生型和HER2 阴性细胞的效力要低约 40 倍[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Copanlisib 相关抗体:

Apoptosis Analysis[1]

Cell Line: BT20 breast cancer cells
Concentration: 20 nM and 62 nM, 200 nM
Incubation Time: 24 hours
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.

Western Blot Analysis[1]

Cell Line: ELT3 cells
Concentration: 0.5 nM, 5 nM, 50 nM, 500 nM
Incubation Time: 2 hours
Result: Complete inhibition of PI3K-mediated AKT phosphorylation was clearly shown at a concentration of 5 nM.
体内研究
(In Vivo)

Copanlisib (BAY 80-6946；0.5-6 mg/kg；静脉注射；每两天一次，每三天一次；持续 60 天；无胸腺裸鼠) 处理在大鼠 KPL4 肿瘤异种移植模型中显示出强大的抗肿瘤活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic nude rats injected with KPL4 tumor cells[1]
Dosage: 0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kg
Administration: Intravenous injection; every second day, every third day; for 60 days
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.
Clinical Trial
分子量

480.52

Formula

C23H28N8O4
CAS 号
性状

固体

颜色

Off-white to light brown

中文名称

库潘尼西
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

1M HCl 中的溶解度 : 100 mg/mL (208.11 mM; 超声助溶)

1M HCl 中的溶解度 : 100 mg/mL (208.11 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0811 mL 10.4054 mL 20.8108 mL
5 mM 0.4162 mL 2.0811 mL 4.1622 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (10.41 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.50%

COA (190 KB) RP-HPLC (173 KB) 元素分析报告 (206 KB)

产品使用指南 (1538 KB)
参考文献

Copanlisib 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
1M HCl / 1M 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
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
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Copanlisib1032568-63-0BAY 80-6946库潘尼西PI3KApoptosisPhosphoinositide 3-kinaseAKTphosphorylationantitumorintravenousadministrationsub-nanomolarantiproliferativeInhibitorinhibitorinhibit

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