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

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

目录号: HY-13272 纯度: 99.69%
COA 产品使用指南

摩尔计算器

Dacomitinib (PF-00299804) 是一种特异，不可逆的 ERBB 家族抑制剂，作用于 EGFR，ERBB2 和 ERBB4 的 IC50 分别为 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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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1024
In-stock
2 mg ￥600
In-stock
5 mg ￥990
In-stock
10 mg ￥1350
In-stock
50 mg ￥3850
In-stock
100 mg ￥5450
In-stock
200 mg 现货 询价
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Dacomitinib:

Dacomitinib 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

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)

细胞效力
(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]
体外研究
(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 细胞中，仅在高浓度 (4 μM) 下达到 IC50，可能反映了非特异性效应。在野生型 EGFR 和 K-ras 的细胞系 (H322, H1819, Calu-3) 中，对 H1819 和 Calu-3 细胞有效抑制，但对 H322 无效。抑制 EGFR 磷酸化，对 EGFR 突变体 (L858R/T790M) 的作用更强；在 NIH3T3 细胞中 1 nM 完全抑制 EGFR L858R/T790M 的磷酸化，而对 WT/T790M 或 Del/T790M 突变需要 100 nM 或更高。HER2 放大细胞系对其最敏感 (IC50<1 μM; 87.5%) [1]. [2].

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

Dacomitinib 相关抗体:
体内研究
(In Vivo)

为了评估Dacomitinib 的疗效，使用 HCC827 GFP 和 HCC827 Del/T790M 细胞在 nu/nu 小鼠中生成异种移植瘤，并用Dacomitinib 治疗小鼠。Dacomitinib (每日口服管饲 10 mg/kg/d)可有效抑制 HCC827 GFP 异种移植瘤的生长。相比之下，HCC827 Del/T790M 异种移植瘤对 ZD1839 具有抗性，而Dacomitinib 治疗在抑制这种异种移植瘤模型的生长方面效果明显更好[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 号
性状

固体

颜色

White to yellow

中文名称

达克替尼；达克米替尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 40 mg/mL (85.12 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.32 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

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

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂： 0.5% CMC/saline water

    Solubility: 5 mg/mL (10.64 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.74%

COA (197 KB) HNMR (214 KB) LCMS (350 KB) 元素分析报告 (213 KB)

产品使用指南 (1538 KB)
参考文献
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.
参考文献

Dacomitinib 相关分类

完整储备液配制表

* 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°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 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.

Keywords:

Dacomitinib1110813-31-4PF-00299804 PF-299804达克替尼达克米替尼PF00299804PF 00299804PF299804PF 299804PF-299804EGFRApoptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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