2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-7

EGFR-IN-7 是一种有效的选择性 EGFR 激酶抑制剂，具有口服活性。EGFR-IN-7 对 EGFR (WT) 和 EGFR (突变体 C797S/T790M/L858R) 具有抑制作用，IC50 值分别为 7.92 nM 和 0.218 nM。EGFR-IN-7 可用于各种癌症的研究。

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EGFR-IN-7 Chemical Structure

EGFR-IN-7 Chemical Structure

CAS No. : 2267329-76-8

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Customer Review

EGFR-IN-7 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers[1].

IC50 & Target[1]

EGFR (WT)

7.92 nM (IC50)

EGFR (C797S/T790M/L858R)

0.218 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
17 nM
Compound: TQB3804
Antiproliferative activity against mouse BaF3 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
[PMID: 35254067]
BaF3 IC50
21 nM
Compound: TQB3804
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
[PMID: 35254067]
NCI-H1975 IC50
910 nM
Compound: TQB3804
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction on cell growth incubated for 72 hrs by MTT assay
[PMID: 35254067]
PC-9 IC50
45 nM
Compound: TQB3804
Antiproliferative activity against human PC-9 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-9 cells expressing EGFR deletion19/T790M/C797S mutant assessed as reduction on cell growth growth incubated for 72 hrs by MTT assay
[PMID: 35254067]
体外研究
(In Vitro)

EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC50 values of 7.92 nM, 0.218 nM and 0.16 nM, respectively[1].
EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM[1].
EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC50 value of 22 nM[1].
EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC50 value of 19 nM[1].

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

EGFR-IN-7 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A431 cells; Ba/F 3 (EGFRΔ19del/T790M/C797S) suspension cells
Concentration: 1 mM; 10 μM-0.508 nM
Incubation Time: 3 days
Result: Inhibited proliferation in cells.
体内研究
(In Vivo)

EGFR-IN-7 (compound 34; 5-45 mg/kg; p.o.; daily; for 13 days) shows potent anti-tumor activity in a subcutaneously implanted Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mouse resistance model[1].
EGFR-IN-7 (25 and 50 mg/kg; p.o.; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model[1].

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

Animal Model: Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)[1]
Dosage: 5, 15, 45 mg/kg
Administration: Oral administration, daily, for 13 days
Result: Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice.
Animal Model: Subcutaneous xenograft PC-9 (Δ19del) model[1]
Dosage: 0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg
Administration: Oral administration, once a day, 3 weeks
Result: Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy.
分子量

694.60

Formula

C32H41BrN9O2P
CAS 号
性状

固体

颜色

Light yellow to yellow

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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 5 mg/mL (7.20 mM; ultrasonic and warming and adjust pH to 5 with 0.1 M HCL and heat to 60°C; 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 1.4397 mL 7.1984 mL 14.3968 mL
5 mM 0.2879 mL 1.4397 mL 2.8794 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 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: ≥ 1.25 mg/mL (1.80 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (1.80 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 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。
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: 99.76%

COA (261 KB) HNMR (205 KB) LCMS (121 KB)

产品使用指南 (1538 KB)
参考文献

EGFR-IN-7 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4397 mL 7.1984 mL 14.3968 mL 35.9919 mL
5 mM 0.2879 mL 1.4397 mL 2.8794 mL 7.1984 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:

EGFR-IN-72267329-76-8EGFREpidermal growth factor receptorErbB-1HER1oralEGFR (epidermal growth factor receptor)TKI (tyrosine kinase inhibitor)C797S/T790M/L858Ranti-tumorlung canceInhibitorinhibitorinhibit

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