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Copanlisib dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Copanlisib dihydrochloride图片
CAS NO:1402152-13-9
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
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PI3KαPI3KδPI3KβPI3KγIC50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 IPI3Kinhibitor, withIC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM forPI3Kα,PI3Kδ,PI3KβandPI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except formTOR. Copanlisib dihydrochloride 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)

mTOP

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 meanIC50values 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].

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 anEC50of 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].

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

553.44

性状

Solid

Formula

C23H30Cl2N8O4

CAS 号

1402152-13-9

中文名称

库潘尼西盐酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8069 mL9.0344 mL18.0688 mL
5 mM0.3614 mL1.8069 mL3.6138 mL
10 mM0.1807 mL0.9034 mL1.8069 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (180.69 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。