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Dacomitinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dacomitinib图片
CAS NO:1110813-31-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
达克替尼
PF-00299804
PF-299804
产品介绍
Dacomitinib (PF-00299804) 是一种特异,不可逆的ERBB家族抑制剂,作用于EGFRERBB2ERBB4IC50分别为 6 nM,45.7 nM 和 73.7 nM。
生物活性

Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of theERBBfamily of kinases withIC50s of 6 nM, 45.7 nM and 73.7 nM forEGFR,ERBB2, andERBB4, respectively[1].

IC50& Target

EGFR

6 nM (IC50)

ErbB2

45.7 nM (IC50)

ErbB4

73.7 nM (IC50)

体外研究
(In Vitro)

Dacomitinib (PF00299804) effectively inhibits the in vitro kinase activity of wild-typeEGFR(IC50=6 nM)with similar efficacy. Dacomitinib also effectively inhibits wild-type ERBB2 with IC50of 45.7 nM. In H441, an IC50is reached with Dacomitinib but only at a very high concentration (4 μM) and likely reflects off-target effects. In cell lines wild-type for both EGFR and K-ras (H322, H1819, and Calu-3), ZD1839 and Dacomitinib both effectively inhibit growth of H1819 and Calu-3 cells but not of H322 cells. Dacomitinib is a pan-ERBB inhibitor and most EGFR mutant cell lines express multiple ERBB family members, the effects on EGFR phosphorylation could potentially be indirect. Dacomitinib inhibits EGFR phosphorylation in all of the different EGFR T790M proteins whereas ZD1839 is ineffective even at 10 μM. In the NIH3T3 cells, phosphorylation of EGFR L858R/T790M is completely inhibited by 1 nM Dacomitinib, whereas 100 nM or greater is required to inhibit EGFR WT/T790M or Del/T790M[1]. The HER2-amplified cell lines are most sensitive to growth inhibition by Dacomitinib (IC50<1 μm in 14 of 16 lines; 87.5%) as compared with 5 28 (17.9%) her2-nonamplified lines (excluding immortalized lines)[2].

体内研究
(In Vivo)

To evaluate the efficacy of Dacomitinib, xenografts innu/numice are generated using HCC827 GFP and HCC827 Del/T790M cells and treated the mice with Dacomitinib. Dacomitinib (10 mg/kg/d by daily oral gavage) effectively inhibits the growth of HCC827 GFP xenografts. In contrast, HCC827 Del/T790M xenografts are resistant to ZD1839, whereas Dacomitinib treatment is substantially more effective at inhibiting growth of this xenograft model[1].

Clinical Trial
分子量

469.94

性状

Solid

Formula

C24H25ClFN5O2

CAS 号

1110813-31-4

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 40 mg/mL(85.12 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1279 mL10.6397 mL21.2793 mL
5 mM0.4256 mL2.1279 mL4.2559 mL
10 mM0.2128 mL1.0640 mL2.1279 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.32 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2.5 mg/mL (5.32 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.32 mM) 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.32 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。