2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. EGFR T790M/L858R-IN-2

EGFR T790M/L858R-IN-2 

目录号: HY-149824 纯度: 99.66%
COA 产品使用指南

摩尔计算器

EGFRT790M/L858R-IN-2 是一种有效的选择性 EGFRT790M/L858R 抑制剂，对 EGFRT790M/L858R 和 EGFR WT 的 IC50 值分别为 3.5, 1290 nM。EGFRT790M/L858R-IN-2 降低 p-EGFR、P-AKT、P-ERK1/2 的表达。EGFRT790M/L858R-IN-2 诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G1 期。EGFRT790M/L858R-IN-2 具有抗癌活性。

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EGFR T790M/L858R-IN-2 Chemical Structure

EGFR T790M/L858R-IN-2 Chemical Structure

CAS No. : 2955607-40-4

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EGFR T790M/L858R-IN-2 相关抗体

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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 T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity[1].

IC50 & Target[1]

EGFRL858R/T790M

3.5 nM (IC50)

EGFR (WT)

1290 nM (IC50)

EGFRT790M

6.7 nM (IC50)

EGFRL858R

2.1 nM (IC50)

体外研究
(In Vitro)

EGFR T790M/L858R-IN-2 (compound 28f) (0.1, 1, 10 µM; 4 h)以剂量依赖性方式降低 H1975、HCC827 细胞中 p-EGFR、P-AKT、P-ERK1/2 的表达[1].
EGFR T790M/L858R-IN-2 (0.1、1、10 µM；48 小时) 在 H1975、HCC827 细胞中诱导细胞凋亡和细胞周期停滞于 G1 期[1]。
EGFR T790M/L858R-IN-2 (0.1、1、10 µM；14 天) 以剂量依赖性方式抑制集落形成和细胞迁移[1]。

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

EGFR T790M/L858R-IN-2 相关抗体:

Western Blot Analysis[1]

Cell Line: H1975, HCC827, A549, A431cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 4 h
Result: Decreased the expression of p-EGFR, P-AKT, P-ERK1/2 in a dose-dependent manner in H1975, HCC827 cells, showed a weak inhibitory effect on EGF-induced EGFR and AKT and ERK1/2 phosphorylation in A549 and A431 cells.

Apoptosis Analysis[1]

Cell Line: H1975, HCC827, A549, A431cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 48 h
Result: Significantly induced apoptosis of H1975 and HCC827 cells in a dose-dependent manner, exhibited weaker apoptosis-inducing ability than osimertinib in A549 and A431 cells, inducing only 14.80 and 17.93% apoptosis, respectively, at 10 μM.

Cell Cycle Analysis[1]

Cell Line: H1975, HCC827, A549, A431cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 48 h
Result: Induced cell cycle arrest in the G1 phase with the G0/G1 phase ratios approximately 80.5% for H1975 and approximately 81.1% for HCC827，approximately 63.8% for A549 and approximately 64.5% for A431 cells.
体内研究
(In Vivo)

EGFR T790M/L858R-IN-2 (5、10、20 mg/kg；i.p.；每天) 以剂量依赖性方式抑制肿瘤生长[1]。

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

Animal Model: 6-8 weeks, BALB/c female nude mice(H1975 cell xenografts)[1]
Dosage: 5, 10, 20 mg/kg
Administration: I.p.; once per day
Result: Inhibited tumor growth, both in volume and weight in a dose-dependent manner.
分子量

497.57

Formula

C28H28FN7O
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (200.98 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 2.0098 mL 10.0488 mL 20.0977 mL
5 mM 0.4020 mL 2.0098 mL 4.0195 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

EGFR T790M/L858R-IN-2 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 2.0098 mL 10.0488 mL 20.0977 mL 50.2442 mL
5 mM 0.4020 mL 2.0098 mL 4.0195 mL 10.0488 mL
10 mM 0.2010 mL 1.0049 mL 2.0098 mL 5.0244 mL
15 mM 0.1340 mL 0.6699 mL 1.3398 mL 3.3496 mL
20 mM 0.1005 mL 0.5024 mL 1.0049 mL 2.5122 mL
25 mM 0.0804 mL 0.4020 mL 0.8039 mL 2.0098 mL
30 mM 0.0670 mL 0.3350 mL 0.6699 mL 1.6748 mL
40 mM 0.0502 mL 0.2512 mL 0.5024 mL 1.2561 mL
50 mM 0.0402 mL 0.2010 mL 0.4020 mL 1.0049 mL
60 mM 0.0335 mL 0.1675 mL 0.3350 mL 0.8374 mL
80 mM 0.0251 mL 0.1256 mL 0.2512 mL 0.6281 mL
100 mM 0.0201 mL 0.1005 mL 0.2010 mL 0.5024 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 T790M/L858R-IN-22955607-40-4EGFRApoptosisEpidermal growth factor receptorErbB-1HER1p-EGFRP-AKTP-ERK1/2apoptosisanti-cancerH1975HCC827 cellsInhibitorinhibitorinhibit

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