2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Stem Cell/Wnt Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. EGFR ERK PARP Caspase Bcl-2 Family Apoptosis
  4. EGFR-IN-197

EGFR-IN-197 是一种 EGFR 抑制剂，对 EGFRL858R/T790M 和 EGFRL858R/T790M/C797S 的 IC50 值分别为 19.5 nM 和 12.0 nM。EGFR-IN-197 可将 NCI-H1975 细胞周期阻滞于 G2/M 期，同时抑制该细胞的增殖、集落形成与迁移，还能抑制线粒体易位并上调线粒体 H2S 水平。EGFR-IN-197 可通过调控凋亡相关蛋白破坏抗凋亡信号通路；诱导 DNA 损伤，激活促凋亡通路诱导细胞凋亡 (apoptosis)。EGFR-IN-197 可用于非小细胞肺癌 (NSCLC) 的相关研究。

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EGFR-IN-197

EGFR-IN-197 Chemical Structure

CAS No. : 3060883-16-8

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EGFR-IN-197 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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ERK ERK1 ERK2 ERK5 ERK8

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-197 is an EGFR inhibitor with IC50 values of 19.5 nM and 12.0 nM against EGFRL858R/T790M and EGFRL858R/T790M/C797S, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H2S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFRL858R/T790M

19.5 nM (IC50)

EGFRL858R/T790M/C797S

12.0 nM (IC50)

ERK

 

PARP

 

Caspase 3

 

Bcl-xL

 

体外研究
(In Vitro)

EGFR-IN-197 (compound 6e) (72 h) 可强效抑制 NCI-H1975、HCC827 和 A431 细胞的增殖，其 IC50 值分别为 0.0473 μM、0.0185 μM 和 0.0226 μM[1]。
EGFR-IN-197 可强效抑制 EGFRL858R/T790M 和 EGFRL858R/T790M/C797S 突变激酶，其 IC50 值分别为 19.5 nM 和 12.0 nM[1]。
EGFR-IN-197 (0.05-0.5 μM; 14 d) 浓度依赖性地抑制 NCI-H1975 细胞的集落形成[1]。
EGFR-IN-197 (0.05-0.5 μM; 24 h) 可浓度依赖性地抑制 NCI-H1975 细胞的迁移[1]。
EGFR-IN-197 (0.05-0.5 μM) 可破坏 NCI-H1975 细胞中 EGFR 的线粒体转位[1]。
EGFR-IN-197 (0.05-0.5 μM) 可浓度依赖性地上调 NCI-H1975 细胞中的线粒体 H2S 水平[1]。
EGFR-IN-197 (0.005-0.5 μM; 24 h) 可浓度依赖性地抑制 NCI-H1975 细胞中 EGFR 和 ERK1/2 的磷酸化，并在 0.5 μM 时显著抑制 AKT 的磷酸化[1]。
EGFR-IN-197 (0.005-0.5 μM; 24 h) 可浓度依赖性调控 NCI-H1975 细胞中凋亡相关蛋白的表达，上调 Cleaved PARP 和 Cleaved caspase-3 水平并下调 Bcl-xL 水平[1]。
EGFR-IN-197 (0.1-1 μM; 24 h) 可浓度依赖性地诱导 NCI-H1975 细胞发生细胞凋亡，在 0.5 μM 及以上浓度时可强烈诱导晚期细胞凋亡[1]。
EGFR-IN-197 (0.05-0.5 μM; 24 h) 可浓度依赖性地将 NCI-H1975 细胞阻滞于 G2/M 期，在 0.5 μM 浓度下，有 62.29% 的细胞处于 G2/M 期[1]。
EGFR-IN-197 (0.05-0.5 μM; 72 h) 以浓度依赖的方式诱导 NCI-H1975 细胞发生 DNA 损伤，在 0.1 μM 及以上浓度时可观察到显著损伤[1]。

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

EGFR-IN-197 相关抗体:

Cell Proliferation Assay[1]

Cell Line: NCI-H1975 cells
Concentration: 0.05 μM, 0.1 μM, 0.5 μM
Incubation Time: 14 d
Result: Concentration-dependently suppressed colony formation of NCI-H1975 cells.

Cell Migration Assay[1]

Cell Line: NCI-H1975 cells
Concentration: 0.05 μM, 0.1 μM, 0.5 μM
Incubation Time: 72 h
Result: Significantly inhibited migration of NCI-H1975 cells, with effects detectable at 0.05 μM.

Cell Migration Assay [1]

Cell Line: NCI-H1975 cells
Concentration: 0.05 μM, 0.1 μM, 0.5 μM
Incubation Time: 12 h, 24 h
Result: EGFR-IN-197 concentration-dependently inhibits migration of NCI-H1975 cells.

Western Blot Analysis[1]

Cell Line: NCI-H1975 cells
Concentration: 0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM
Incubation Time: 24 h
Result: Concentration-dependently suppressed phosphorylation of EGFR (p-EGFR) and ERK1/2 (p-ERK1/2) in NCI-H1975 cells.
Significantly inhibited phosphorylation of AKT (p-AKT) at 0.5 μM.\nConcentration-dependently increased expression of Cleaved PARP and Cleaved caspase-3, and decreased expression of Bcl-xL in NCI-H1975 cells.

Apoptosis Analysis[1]

Cell Line: NCI-H1975 cells
Concentration: 0.1 μM, 0.5 μM, 1 μM
Incubation Time: 24 h
Result: Concentration-dependently induced apoptosis in NCI-H1975 cells.
Increased the proportion of late apoptotic cells sharply at 0.5 μM.
Induced late apoptosis in 30.5% of cells and early apoptosis in 0.73% of cells at 1 μM.

Cell Cycle Analysis[1]

Cell Line: NCI-H1975 cells
Concentration: 0.05 μM, 0.1 μM, 0.5 μM
Incubation Time: 24 h
Result: Concentration-dependently arrested NCI-H1975 cells at the G2/M phase.
Resulted in 36.42% of cells in G0/G1 phase and 32.14% in G2/M phase at 0.05 μM.
Resulted in 20.85% of cells in G0/G1 phase and 54.52% in G2/M phase at 0.1 μM.
Resulted in 12.40% of cells in G0/G1 phase and 62.29% in G2/M phase at 0.5 μM.

Immunofluorescence[1]

Cell Line: NCI-H1975 cells
Concentration: 0.05 μM, 0.1 μM, 0.5 μM
Incubation Time: 24 h
Result: EGFR-IN-197 disrupts mitochondrial translocation of EGFR in NCI-H1975 cells.
分子量

512.40

Formula

C23H26BrN7O2
CAS 号
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-197 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

EGFR-IN-1973060883-16-8EGFRERKPARPCaspaseBcl-2 FamilyApoptosisEpidermal growth factor receptorErbB-1HER1Extracellular signal regulated kinasespoly ADP ribose polymerase EGFR inhibitorG2/M phase cell cycle arrestinduce DNA damage and apoptosisregulate apoptosis-related proteinsinhibit colony formation and cell migrationinhibit EGFR mitochondrial translocationupregulate mitochondrial H?S levelsnon-small cell lung cancer (NSCLC)NCI-H1975 cellsHCC827 cellsA431 cellsInhibitorinhibitorinhibit

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