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

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

目錄號(hào): HY-15346 純度: 99.50%
COA 產(chǎn)品使用指南

Copanlisib (BAY 80-6946) 是一種有效的，選擇性的和 ATP 競(jìng)爭性的泛 I 類 PI3K 抑制劑，對(duì) PI3Kα，PI3Kδ，PI3Kβ 和 PI3Kγ 的 IC50 分別為 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。除 mTOR 外，Copanlisib 對(duì)其他脂質(zhì)和蛋白激酶的選擇性超過 2000 倍。Copanlisib 具有優(yōu)異的抗腫瘤活性。

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Copanlisib Chemical Structure

Copanlisib Chemical Structure

CAS No. : 1032568-63-0

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規(guī)格 價(jià)格 是否有貨 數(shù)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   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Copanlisib:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

細(xì)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]
體外研究
(In Vitro)

Copanlisib (BAY 80-6946；20 -200 nM；24 小時(shí)；BT20 乳腺癌細(xì)胞) 處理誘導(dǎo)對(duì)拉帕替尼和曲妥珠單抗耐藥的腫瘤細(xì)胞系子集發(fā)生細(xì)胞凋亡[1]。
Copanlisib (BAY 80-6946；0.5-500 nM；2 小時(shí)；ELT3 細(xì)胞) 處理顯示完全抑制 ELT3 細(xì)胞中 PI3K 介導(dǎo)的 AKT 磷酸化[1]。
Copanlisib 有效抑制一組人類腫瘤細(xì)胞系中的細(xì)胞增殖。Copanlisib 對(duì)具有 PIK3CA 激活突變的細(xì)胞系的平均 IC50 值為 19 nM，對(duì) HER2 陽性細(xì)胞系的平均 IC50 值為 17 nM，而在 PIK3CA 野生型和HER2 陰性細(xì)胞的效力要低約 40 倍[1]。

MCE 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.
體內(nèi)研究
(In Vivo)

Copanlisib (BAY 80-6946；0.5-6 mg/kg；靜脈注射；每兩天一次，每三天一次；持續(xù) 60 天；無胸腺裸鼠) 處理在大鼠 KPL4 腫瘤異種移植模型中顯示出強(qiáng)大的抗腫瘤活性[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 號(hào)
性狀

固體

中文名稱

庫潘尼西
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

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

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

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (10.41 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.50%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
Copanlisib
目錄號(hào)：
HY-15346
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