Copanlisib dihydrochloride 库潘尼西盐酸; BAY 80-6946 dihydrochloride|cas:1402152-13-9|西域试剂

Copanlisib dihydrochloride 库潘尼西盐酸; BAY 80-6946 dihydrochloride,99.55%

产品编号：Bellancom-15346A| CAS NO：1402152-13-9| 分子式：C₂₃H₃₀Cl₂N₈O₄| 分子量：553.44

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货号	价格	库存与货期
Bellancom-15346A	￥1300.00	杭州北京（现货）
Bellancom-15346A	￥1900.00	杭州北京（现货）
Bellancom-15346A	￥5200.00	杭州北京（现货）
Bellancom-15346A	￥8500.00	杭州北京（现货）

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Copanlisib dihydrochloride 库潘尼西盐酸; BAY 80-6946 dihydrochloride

产品介绍

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 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 dihydrochloride 对其他脂质和蛋白激酶的选择性超过 2000 倍。Copanlisib dihydrochloride 具有优异的抗肿瘤活性。

生物活性

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 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 dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.

体外研究

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.
Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells.
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.

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

Apoptosis Analysis

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

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.

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

Animal Model:	Athymic nude rats injected with KPL4 tumor cells
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.

体内研究

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

Animal Model:	Athymic nude rats injected with KPL4 tumor cells
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.

体内研究

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

Animal Model:	Athymic nude rats injected with KPL4 tumor cells
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.

性状

Solid

溶解性数据

In Vitro:

H₂O : 20 mg/mL (36.14 mM; Need ultrasonic)

DMSO : 5 mg/mL (9.03 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8069 mL	9.0344 mL	18.0688 mL
5 mM	0.3614 mL	1.8069 mL	3.6138 mL
10 mM	0.1807 mL	0.9034 mL	1.8069 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 (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；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