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  2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. Dacomitinib

Dacomitinib  (Synonyms: 達(dá)克替尼; PF-00299804; PF-299804)

目錄號(hào): HY-13272 純度: 99.74%
COA 產(chǎn)品使用指南 技術(shù)支持

Dacomitinib (PF-00299804) 是一種特異，不可逆的 ERBB 家族抑制劑，作用于 EGFR，ERBB2 和 ERBB4 的 IC50 分別為 6 nM，45.7 nM 和 73.7 nM。

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Dacomitinib Chemical Structure

Dacomitinib Chemical Structure

CAS No. : 1110813-31-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1024
In-stock
1 mg ￥394
In-stock
2 mg ￥600
In-stock
5 mg ￥990
In-stock
10 mg ￥1350
In-stock
25 mg ￥2475
In-stock
50 mg ￥3850
In-stock
100 mg ￥5450
In-stock
200 mg 現(xiàn)貨 詢(xún)價(jià)
500 mg 現(xiàn)貨 詢(xún)價(jià)
1 g   詢(xún)價(jià)  
5 g   詢(xún)價(jià)  

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Customer Review

Other Forms of Dacomitinib:

  • 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

Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].

IC50 & Target[1]

EGFR

6 nM (IC50)

ErbB2

45.7 nM (IC50)

ErbB4

73.7 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
LoVo IC50
0.011 μM
Compound: 5
Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
[PMID: 23930994]
NCI-H1975 IC50
0.042 μM
Compound: 5
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
[PMID: 23930994]
NCI-H1975 IC50
0.44 μM
Compound: 32; PF00299804
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay
[PMID: 28754471]
PC-9 IC50
0.00063 μM
Compound: 5
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
[PMID: 23930994]
Sf9 IC50
0.006 μM
Compound: 54; PF-00299804
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
0.046 μM
Compound: 54; PF-00299804
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
0.074 μM
Compound: 54; PF-00299804
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]
Sf9 IC50
3.57 μM
Compound: 54; PF-00299804
Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic acid-tyrosine phosphorylation after 30 mins by ELISA
Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic acid-tyrosine phosphorylation after 30 mins by ELISA
[PMID: 27491023]
體外研究
(In Vitro)

Dacomitinib (PF00299804) 有效抑制野生型 EGFR 激酶活性 (IC50=6 nM) ，也抑制野生型 ERBB2 (IC50=45.7 nM) 。在 H441 細(xì)胞中，僅在高濃度 (4 μM) 下達(dá)到 IC50，可能反映了非特異性效應(yīng)。在野生型 EGFR 和 K-ras 的細(xì)胞系 (H322, H1819, Calu-3) 中，對(duì) H1819 和 Calu-3 細(xì)胞有效抑制，但對(duì) H322 無(wú)效。抑制 EGFR 磷酸化，對(duì) EGFR 突變體 (L858R/T790M) 的作用更強(qiáng)；在 NIH3T3 細(xì)胞中 1 nM 完全抑制 EGFR L858R/T790M 的磷酸化，而對(duì) WT/T790M 或 Del/T790M 突變需要 100 nM 或更高。HER2 放大細(xì)胞系對(duì)其最敏感 (IC50<1 μM; 87.5%) [1]. [2].

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

為了評(píng)估Dacomitinib 的療效，使用 HCC827 GFP 和 HCC827 Del/T790M 細(xì)胞在 nu/nu 小鼠中生成異種移植瘤，并用Dacomitinib 治療小鼠。Dacomitinib (每日口服管飼 10 mg/kg/d)可有效抑制 HCC827 GFP 異種移植瘤的生長(zhǎng)。相比之下，HCC827 Del/T790M 異種移植瘤對(duì) ZD1839 具有抗性，而Dacomitinib 治療在抑制這種異種移植瘤模型的生長(zhǎng)方面效果明顯更好[1]。

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

469.94

Formula

C24H25ClFN5O2
CAS 號(hào)
性狀

固體

顏色

White to yellow

中文名稱(chēng)

達(dá)克替尼；達(dá)克米替尼
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)： 

DMSO 中的溶解度 : 40 mg/mL (85.12 mM; 超聲助溶; 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 2.1279 mL 10.6397 mL 21.2793 mL
5 mM 0.4256 mL 2.1279 mL 4.2559 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)：

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(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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.32 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 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: 2.5 mg/mL (5.32 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 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(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： 0.5% CMC/saline water

    Solubility: 5 mg/mL (10.64 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(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
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，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.74%

參考文獻(xiàn)
Cell Assay
[2]

Cells are seeded in duplicate at 5×103 to 5×104 cells per well in 24-well plates, and growth inhibition data is calculated. Briefly, day after plating, Dacomitinib is added at 10 μM and 2-fold dilutions over 12 concentrations are carried out to generate a dose-response curve. Control wells without the drug are also seeded. The cells are counted on day 1 when the drug is added, as well as after 6 days when the experiment ended. After the trypsinization cells are placed in an Isotone solution and immediately counted using a Coulter Z1 particle counter. The suspension cultures are counted using a Coulter Vi-Cell counter[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Nude mice (nu/nu; 6-8 weeks old) are used for in vivo studies. A suspension of 5×106 HCC827-GFP or HCC827-Del/T790M lung cancer cells (in 0.2 mL of PBS) are inoculated s.c. into the lower-right quadrant of the flank of each mouse. Five mice are inoculated with either HCC827-GFP or HCC827-Del/T790M cells in the ZD1839 treatment group. Tumors are measured twice weekly using calipers, and volume is calculated using the following formula: length×width2×0.52. Mice are monitored daily for body weight and general condition. Mice are randomized to treatment when the mean tumor volume is 400 to 500 mm3. ZD1839 is administered at 150 mg/kg/d by daily oral gavage. Dacomitinib is administered at 10 mg/kg/d by daily oral gavage. The experiment is terminated when the mean size of the control tumors reached 2000 mm3.

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, 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
DMSO 1 mM 2.1279 mL 10.6397 mL 21.2793 mL 53.1983 mL
5 mM 0.4256 mL 2.1279 mL 4.2559 mL 10.6397 mL
10 mM 0.2128 mL 1.0640 mL 2.1279 mL 5.3198 mL
15 mM 0.1419 mL 0.7093 mL 1.4186 mL 3.5466 mL
20 mM 0.1064 mL 0.5320 mL 1.0640 mL 2.6599 mL
25 mM 0.0851 mL 0.4256 mL 0.8512 mL 2.1279 mL
30 mM 0.0709 mL 0.3547 mL 0.7093 mL 1.7733 mL
40 mM 0.0532 mL 0.2660 mL 0.5320 mL 1.3300 mL
50 mM 0.0426 mL 0.2128 mL 0.4256 mL 1.0640 mL
60 mM 0.0355 mL 0.1773 mL 0.3547 mL 0.8866 mL
80 mM 0.0266 mL 0.1330 mL 0.2660 mL 0.6650 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(chēng)：
Dacomitinib
目錄號(hào)：
HY-13272
需求量：