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  2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Anti-infection
  3. EGFR Orthopoxvirus
  4. Canertinib dihydrochloride

Canertinib dihydrochloride  (Synonyms: 卡紐替尼二鹽酸鹽; CI-1033 dihydrochloride; PD-183805 dihydrochloride)

目錄號(hào): HY-10367A 純度: 99.68%
COA 產(chǎn)品使用指南 技術(shù)支持

Canertinib dihydrochloride (CI-1033;PD-183805) 是有效地，不可逆的 EGFR 抑制劑；抑制細(xì)胞 EGFR 和 ErbB2 自身磷酸化的 IC50 值分別為 7.4 和 9 nM。Canertinib dihydrochloride 可以用于研究小鼠的牛痘病毒呼吸道感染。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Canertinib dihydrochloride Chemical Structure

Canertinib dihydrochloride Chemical Structure

CAS No. : 289499-45-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥270
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5 mg ￥220
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10 mg ￥330
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25 mg ￥566
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50 mg ￥850
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100 mg ￥1200
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of Canertinib dihydrochloride:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice[1][2][3][4].

IC50 & Target[1]

EGFR

7.4 nM (IC50)

ErbB2

9 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 IC50
0.002 μM
Compound: 4
Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
[PMID: 27491023]
Sf9 IC50
0.011 μM
Compound: 4
Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
[PMID: 27491023]
Sf9 IC50
0.027 μM
Compound: 4
Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA
[PMID: 27491023]
T-24 IC50
0.016 μM
Compound: 4
Irreversible inhibition of ERBB2 (unknown origin) autophosphorylation transfected in EGF-stimulated mouse T24 NIH/3T3 cells with extracellular binding domain of ERBB1 incubated for 2 hrs followed by stimulation with EGF for 10 mins
Irreversible inhibition of ERBB2 (unknown origin) autophosphorylation transfected in EGF-stimulated mouse T24 NIH/3T3 cells with extracellular binding domain of ERBB1 incubated for 2 hrs followed by stimulation with EGF for 10 mins
[PMID: 27491023]
體外研究
(In Vitro)

Canertinib dihydrochloride (CI-1033 dihydrochloride) 以劑量依賴的方式顯著抑制培養(yǎng)的黑色素瘤細(xì)胞 RaH3 和 RaH5 的生長(zhǎng)。IC50 約為 0.8 μM，在 5 μM 時(shí)，兩種細(xì)胞系在處理后 72 小時(shí)內(nèi)完全停止生長(zhǎng)。指數(shù)生長(zhǎng)的 RaH3 和 RaH5 與 1 μM canertinib 孵育后 24 小時(shí)內(nèi)，細(xì)胞在細(xì)胞周期的 G1 期積累，不誘導(dǎo)細(xì)胞凋亡。1 μM canertinib 抑制 ErbB1-3 受體磷酸化，同時(shí)降低兩種細(xì)胞系中的 Akt-、Erk1/2- 和 Stat3 活性[2]。
Canertinib dihydrochloride 也是一種有效的激活劑外泌體分泌[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Canertinib dihydrochloride (CI-1033 dihydrochloride) 表現(xiàn)出優(yōu)異的體內(nèi)抗腫瘤活性，口服給藥后 A431 異種移植物的生長(zhǎng)延遲超過 50 天[1]。
Canertinib（40 mg/kg/天； i.p.）顯在裸鼠中抑制人惡性黑色素瘤異種移植RaH3和RaH5的生長(zhǎng) [2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

558.86

Formula

C24H27Cl3FN5O3
CAS 號(hào)
性狀

固體

顏色

Light yellow to green yellow

中文名稱

卡紐替尼二鹽酸鹽
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)： 

DMSO 中的溶解度 : 50 mg/mL (89.47 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)使用新開封的 DMSO)

H2O 中的溶解度 : 16.67 mg/mL (29.83 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 1.7894 mL 8.9468 mL 17.8936 mL
5 mM 0.3579 mL 1.7894 mL 3.5787 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)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.72 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.72 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

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： PBS

    Solubility: 10 mg/mL (17.89 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: 99.68%

參考文獻(xiàn)
Kinase Assay
[1]

Enzyme assays for IC50 determinations are performed in 96-well filter plates. The total volume is 0.1 mL containing 20 mM Hepes, pH 7.4, 50 mM sodium vanadate, 40 mM magnesium chloride, 10 μM adenosine triphosphate (ATP) containing 0.5 mCi of [32P]ATP, 20 mg of polyglutamic acid/tyrosine, 10 ng of EGFR tyrosine kinase, and appropriate dilutions of inhibitor (Canertinib). All components except the ATP are added to the well and the plate is incubated with shaking for 10 min at 25°C. The reaction is started by adding [32P]ATP, and the plate is incubated at 25°C for 10 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid (TCA). The plate is kept at 4°C for at least 15 min to allow the substrate to precipitate. The wells is then washed five times with 0.2 mL of 10% TCA and 32P incorporation determined with a plate counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

RaH3 and RaH5 cells are treated with increasing concentrations (0-10 μM) of Canertinib for 72 h. The cells are suspended in buffer and counted[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: Canertinib treatment starts when the tumors show reliable growth. The mice are randomized into control and treatment groups. In the canertinib treated RaH3 group (n=4) and RaH5 group (n=7) each mouse receives i.p. injections of 1.2 mg canertinib (40 mg/kg/day) in 0.1 ml 0.15 M NaCl 5 days a week. The control RaH3 (n=3) and RaH5 (n=7) mice receive i.p. injections of vehicle only according to the same regimen. At the end of the treatment period, the mice are sacrificed by cervical dislocation where after the tumors are removed and weighed[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
H2O / DMSO 1 mM 1.7894 mL 8.9468 mL 17.8936 mL 44.7339 mL
5 mM 0.3579 mL 1.7894 mL 3.5787 mL 8.9468 mL
10 mM 0.1789 mL 0.8947 mL 1.7894 mL 4.4734 mL
15 mM 0.1193 mL 0.5965 mL 1.1929 mL 2.9823 mL
20 mM 0.0895 mL 0.4473 mL 0.8947 mL 2.2367 mL
25 mM 0.0716 mL 0.3579 mL 0.7157 mL 1.7894 mL
DMSO 30 mM 0.0596 mL 0.2982 mL 0.5965 mL 1.4911 mL
40 mM 0.0447 mL 0.2237 mL 0.4473 mL 1.1183 mL
50 mM 0.0358 mL 0.1789 mL 0.3579 mL 0.8947 mL
60 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7456 mL
80 mM 0.0224 mL 0.1118 mL 0.2237 mL 0.5592 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：
Canertinib dihydrochloride
目錄號(hào)：
HY-10367A
需求量：