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

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Copanlisib (Synonyms: 库潘尼西; BAY 80-6946) 纯度: 99.50%

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。

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

Copanlisib Chemical Structure

CAS No. : 1032568-63-0

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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)

PI3Kβ

3.7 nM (IC50)

PI3Kδ

0.7 nM (IC50)

PI3Kγ

6.4 nM (IC50)

mTOR

45 nM (IC50)

体外研究
(In Vitro)

Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab[1].
Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells[1].
Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC50 values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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; intravenous injection; every second day, every third day; for 60 days; athymic nude rats) treatment displays robust antitumor activity in the rat KPL4 tumor xenograft model[1].

上海金畔生物科技有限公司 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

1032568-63-0
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

1M HCl : 100 mg/mL (208.11 mM; Need ultrasonic)

DMSO : 1 mg/mL (2.08 mM; Need ultrasonic)

H2O : 0.67 mg/mL (1.39 mM; Need ultrasonic)

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
10 mM 0.2081 mL 1.0405 mL 2.0811 mL

*

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, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Liu N, et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013 Nov;12(11):2319-30.

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