1. Apoptosis Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. Apoptosis EGFR
  3. EGFR-IN-47

EGFR-IN-47 是一种有效的且具有口服活性的 EGFRL858R/T790M/C797S 抑制剂,其 IC50 值为 0.01 μM。EGFR-IN-47 诱导细胞周期停滞和细胞凋亡 (apoptosis)。EGFR-IN-47 具有 NSCLC 的研究潜力。

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EGFR-IN-47 Chemical Structure

EGFR-IN-47 Chemical Structure

CAS No. : 3034649-73-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-47 is a potent and orally active EGFRL858R/T790M/C797S inhibitor with an IC50 of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

0.07 μM (IC50)

体外研究
(In Vitro)

EGFR-IN-47 (compound 14aj) (72 h) shows anti-proliferative effects with IC50s of 0.013 μM, 2.972 μM, 1.031 μM for PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells, respectively[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM; 24 h) induces cell cycle attest at the G0/G1-phase[1].
EGFR-IN-47 (0.01, 0.05, 0.25 μM) induces cell deathvia apoptosis in a concentration-dependent manner[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM) inhibits phosphorylation of the EGFR downstream mediators[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferative effects with IC50s of 0.013 µM, 2.972 µM, 1.031 µM for PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: PC-9 EGFRL858R/T790M/C797S cells
Concentration: 0.01, 0.05, 0.25, 1 µM
Incubation Time: 24 h
Result: Cells were arrest at the G0/G1-phase.

Apoptosis Analysis[1]

Cell Line: PC-9 EGFRL858R/T790M/C797S cells
Concentration: 0.01, 0.05, 0.25 µM
Incubation Time: 24 h
Result: Induced cell deathvia apoptosis in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: PC-9 EGFRL858R/T790M/C797S cells
Concentration: 0.01, 0.05, 0.25, 1 µM
Incubation Time:
Result: Inhibited phosphorylation of the EGFR downstream mediators.
体内研究
(In Vivo)

EGFR-IN-47 (10, 20, 40 mg/kg; i.g.) shows anti-tumor effect with low toxicity[1].
EGFR-IN-47 (20 mg/kg for i.v.; 20 mg/kg for p.o.) shows an ideal oral bioavailability of 66.05%[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley rats[1].

parameter iv (20 mg/kg) po (20 mg/kg)
AUC0-∞ (mg/Lh) 15.889 10.494
Cmax (mg/L) 6.845 0.77
Tmax (h) 0.083 6
F (%) 66.05
MRT0-∞ (h) 16.439 16.791
Vss (L/kg) 16.015 28.101
CL (L/h/kg) 1.272 2.151
t(1/2) (h) 8.922 11.154
Male Sprague-Dawley rats; 20 mg/kg for i.v.; 20 mg/kg for p.o.[1]

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

Animal Model: 6-8 weeks, BALB/c nude mice (PC-9 EGFRL858R/T790M/C797S cells )[1]
Dosage: 10, 20, 40 mg/kg (dissolved in 25% (v/v) PEG400 plus 5% DMSO)
Administration: I.g.
Result: Showed anti-tumor effect with low toxicity.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: 20 mg/kg
Administration: I.v.; p.o.
Result: Showed an ideal oral bioavailability of 66.05%.
分子量

481.64

Formula

C29H35N7

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 : 20 mg/mL (41.52 mM; 超声助溶 (<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 2.0762 mL 10.3812 mL 20.7624 mL
5 mM 0.4152 mL 2.0762 mL 4.1525 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

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

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 2.0762 mL 10.3812 mL 20.7624 mL 51.9060 mL
5 mM 0.4152 mL 2.0762 mL 4.1525 mL 10.3812 mL
10 mM 0.2076 mL 1.0381 mL 2.0762 mL 5.1906 mL
15 mM 0.1384 mL 0.6921 mL 1.3842 mL 3.4604 mL
20 mM 0.1038 mL 0.5191 mL 1.0381 mL 2.5953 mL
25 mM 0.0830 mL 0.4152 mL 0.8305 mL 2.0762 mL
30 mM 0.0692 mL 0.3460 mL 0.6921 mL 1.7302 mL
40 mM 0.0519 mL 0.2595 mL 0.5191 mL 1.2976 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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产品名称:
EGFR-IN-47
目录号:
HY-143337
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