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

Copanlisib dihydrochloride  (Synonyms: 庫(kù)潘尼西鹽酸; BAY 80-6946 dihydrochloride)

目錄號(hào): HY-15346A 純度: 99.55%
COA 產(chǎn)品使用指南 技術(shù)支持

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 是一種有效的，選擇性的和 ATP 競(jìng)爭(zhēng)性的泛 I 類(lèi) 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 dihydrochloride 對(duì)其他脂質(zhì)和蛋白激酶的選擇性超過(guò) 2000 倍。Copanlisib dihydrochloride 具有優(yōu)異的抗腫瘤活性。

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Copanlisib dihydrochloride Chemical Structure

Copanlisib dihydrochloride Chemical Structure

CAS No. : 1402152-13-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in Water ￥1583
In-stock
1 mg ￥590
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(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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Customer Review

Other Forms of Copanlisib dihydrochloride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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[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)

體外研究
(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].

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; 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].

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

553.44

Formula

C23H30Cl2N8O4
CAS 號(hào)
性狀

固體

顏色

Off-white to light yellow

中文名稱(chēng)

庫(kù)潘尼西鹽酸
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

H2O 中的溶解度 : 50 mg/mL (90.34 mM; 超聲助溶)

DMSO 中的溶解度 : 5 mg/mL (9.03 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

  • 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑： PBS

    Solubility: 100 mg/mL (180.69 mM); 澄清溶液; 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(guò)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
該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.55%

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.8069 mL 9.0344 mL 18.0688 mL 45.1720 mL
5 mM 0.3614 mL 1.8069 mL 3.6138 mL 9.0344 mL
H2O 10 mM 0.1807 mL 0.9034 mL 1.8069 mL 4.5172 mL
15 mM 0.1205 mL 0.6023 mL 1.2046 mL 3.0115 mL
20 mM 0.0903 mL 0.4517 mL 0.9034 mL 2.2586 mL
25 mM 0.0723 mL 0.3614 mL 0.7228 mL 1.8069 mL
30 mM 0.0602 mL 0.3011 mL 0.6023 mL 1.5057 mL
40 mM 0.0452 mL 0.2259 mL 0.4517 mL 1.1293 mL
50 mM 0.0361 mL 0.1807 mL 0.3614 mL 0.9034 mL
60 mM 0.0301 mL 0.1506 mL 0.3011 mL 0.7529 mL
80 mM 0.0226 mL 0.1129 mL 0.2259 mL 0.5647 mL

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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(chēng)：
Copanlisib dihydrochloride
目錄號(hào)：
HY-15346A
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