2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. EGFR Akt ERK
  4. EGFR-IN-451

EGFR-IN-451 是一种 EGFR 抑制剂，其 IC50 值为 0.02 nM。EGFR-IN-451 还可抑制突变体 EGFRL858R、EGFRT790M 及 EGFRL858R/T790M ，对应的 IC50 值为 0.26-34 nM。EGFR-IN-451 可抑制 AKT 和 ERK 的活化，并抑制 EGFR 突变型癌细胞的增殖。EGFR-IN-451 可用于 EGFR 驱动型癌症的研究。

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EGFR-IN-451

EGFR-IN-451 Chemical Structure

CAS No. : 220576-72-7

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EGFR-IN-451 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-451 is an EGFR inhibitor with an IC50 value of 0.02 nM. EGFR-IN-451 also inhibits mutant EGFRL858R, EGFRT790M, and EGFRL858R/T790M with IC50 values of 0.26-34 nM. EGFR-IN-451 inhibits AKT and ERK activation and inhibits proliferation of EGFR-mutant cancer cells. EGFR-IN-451 can be used for the research of EGFR-driven cancer[1].

IC50 & Target[1]

EGFR

0.02 nM (IC50)

EGFRL858R

0.26 nM (IC50)

EGFRT790M

25 nM (IC50)

EGFRL858R/T790M

34 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-451 (Compound R14) (0.1-10000 nM) 可在无细胞的 caliper 迁移变动实验中强效抑制野生型 EGFR (IC50 = 0.02 nM)、EGFRL858R (IC50 = 0.26 nM)、EGFRT790M (IC50 = 25 nM) 及 EGFRL858R/T790M (IC50 = 34 nM)[1]。
EGFR-IN-451 可在 MTT 实验中抑制 HCC827 细胞 (IC50 = 2.47 μM) 和 H1975 细胞 (IC50 = 18.07 μM) 的活性[1]。
EGFR-IN-451 (0.01-10 μM; 1-12 h) 可在 0.01 μM 浓度下就能抑制 HCC827 细胞中的磷酸化 EGFR，在 0.1、1 和 10 μM 浓度下抑制 H1975 细胞中的磷酸化 EGFR，且能使 HCC827 细胞中磷酸化 EGFR 的水平在 12 h 内持续降低，并抑制 P-AKT、P-ERK 的表达[1]。

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

EGFR-IN-451 相关抗体:

Western Blot Analysis[1]

Cell Line: HCC827 cells, H1975 cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 1, 4, 8, 12 h (time-course in HCC827 cells)
Result: Inhibited phosphorylated EGFR in HCC827 cells at 0.01, 0.1 μM.
Reduced phosphorylated EGFR levels in HCC827 cells at 1, 4, 8, and 12 h post-treatment.
Inhibited phosphorylated EGFR in H1975 cells at 0.1, 1, and 10 μM.
Reduced P-AKT, P-ERK expression.
分子量

329.36

Formula

C19H15N5O
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-451 相关分类

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Keywords:

EGFR-IN-451220576-72-7EGFRAktERKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BExtracellular signal regulated kinasesH1975 cellsEGFR T790MHCC827 cellsEGFR L858REGFR L858R/T790MAKTphosphorylated EGFREGFR-driven cancerInhibitorinhibitorinhibit

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