2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage Apoptosis
  3. EGFR Akt PERK Apoptosis
  4. EGFR-IN-181

EGFR-IN-181 是一种具有口服活性，可穿透血脑屏障的强效 EGFRL858R/T790M/C797S 三重突变抑制剂 (IC50 = 1.32 nM) 。EGFR-IN-181 可抑制 EGFR 磷酸化 (p-EGFR) 及其下游信号蛋白 AKT (p-AKT) 和 ERK (p-ERK) 的磷酸化。EGFR-IN-181 可诱导细胞凋亡 (apoptosis) 并导致 G2 期阻滞。EGFR-IN-181 可用于非小细胞肺癌 (NSCLC) 和脑转移瘤的研究。

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EGFR-IN-181

EGFR-IN-181 Chemical Structure

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EGFR-IN-181 相关抗体

Top Publications Citing Use of Products

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

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases[1].

IC50 & Target

Akt

 

EGFR (C797S/T790M/L858R)

 

体外研究
(In Vitro)

EGFR-IN-181 (Compound D18) (0.001-1000 μg/mL，48 小时) 对多种 EGFR 突变细胞系表现出显著的抗增殖活性，并且对正常细胞 (MCR-5、HEK293、LX-2) 具有较高的 IC50 值[1]。
EGFR-IN-181 (50-500 nM，24 小时) 以浓度依赖的方式抑制 NCI-H1975 细胞 (携带 EGFRL858R/T790M/C797S 突变) 中 EGFR 的磷酸化 (p-EGFR) 及其下游信号蛋白 AKT (p-AKT) 和 ERK (p-ERK)[1]。
EGFR-IN-181 (50-500 nM，24 小时) 呈浓度依赖性地诱导 NCI-H1975 EGFRL858R/T790M/C797S 细胞凋亡，并导致 G2 期阻滞[1]。
EGFR-IN-181 抑制 HEK293 细胞中的 hERG 钾通道，IC50 值为 10.55 μM[1]。

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

EGFR-IN-181 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549 cell line: harboring EGFRWT BaF3™ cell line: engineered BaF3 cell line, harboring EGFRL858R/T790M/C797S NCI–H1975 cell line: harboring EGFRL858R/T790M/C797S PC-9 cell line: harboring EGFRDel19 H1975 cell line: harboring EGFRL858R/T790M MCR-5, HEK293, LX-2
Concentration: 0.001 μg/mL, 0.01 μg/mL, 0.1 μg/mL, 1 μg/mL, 10 μg/mL, 100 μg/mL, 1000 μg/mL
Incubation Time: 48 h
Result: A549 (IC50 = 2.63 μM)
PC-9 (IC50 = 0.012 μM)
H1975 (IC50 = 0.027 μM)
BaF3TM (IC50 = 0.049 μM)
NCI–H1975 (IC50 = 0.87 μM)
MCR-5 (IC50 = 4.51 μM)
HEK293 (IC50 = 36.17 μM)
LX-2 (IC50 = 4.84 μM)

Western Blot Analysis[1]

Cell Line: NCI-H1975 EGFRL858R/T790M/C797S
Concentration: 50 nM, 100 nM, 500 nM
Incubation Time: 24 h
Result: Concentration-dependently inhibited EGFR phosphorylation (p-EGFR) and its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK) in NCI-H1975 cells EGFRL858R/T790M/C797S; at a concentration of 500 nM, EGFR phosphorylation was completely inhibited.

Apoptosis Analysis[1]

Cell Line: NCI-H1975 EGFRL858R/T790M/C797S cells
Concentration: 50 nM, 150 nM, 250 nM, 500 nM
Incubation Time: 24 h
Result: Induced apoptosis in a degree-dependent manner, achieving an apoptosis rate of 37.94% at a concentration of 500 nM.

Cell Cycle Analysis[1]

Cell Line: NCI-H1975 EGFRL858R/T790M/C797S cells
Concentration: 50 nM, 150 nM, 250 nM, 500 nM
Incubation Time: 24 h
Result: Induced G2 phase arrest in a concentration-dependent manner, with the proportion of cells in G2 phase being 22.57 % at 50 nM and increasing to 65.98 % at 500 nM.
体内研究
(In Vivo)

EGFR-IN-181 (Compound D18) (12.5-25 mg/kg，口服，每日一次，持续 15 天) 以剂量依赖的方式显著抑制 NCI-H1975 细胞 EGFRL858R/T790M/C797S 异种移植小鼠中 EGFR 突变肿瘤的生长，表现出良好的安全性和耐受性，无明显毒性[1]。

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

Animal Model: A xenograft tumor model was established using female BALB/c nude mice (6-8 weeks old) by subcutaneous transplantation of NCI-H1975 cells EGFRL858R/T790M/C797S triple mutations)[1].
Dosage: 12.5 mg/kg, 25 mg/kg
Administration: P.o., once daily for 15 days
Result: At a dose of 12.5 mg/kg, the tumor growth inhibition rate (TGI) was 53.64 %; at a dose of 25 mg/kg, the TGI was 91.04 %.
The average tumor weight was significantly lower than that of the control group.
Did not experience a significant decrease in body weight, and H&E staining of the major organs (heart, liver, spleen, lung, and kidney) showed no lesions or organ failure.
分子量

482.95

Formula

C24H28ClN6OP
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

EGFR-IN-181 相关分类

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  • 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-181EGFRAktPERKApoptosisEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseNSCLCNon-Small Cell Lung CancerBlood-brain barrierInhibitorinhibitorinhibit

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