2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-74

EGFR-IN-74 (Compound 21) 是一种有效的 EGFR 抑制剂，对 EGFR L858R/T790M 的 IC50 为 138 nM。EGFR-IN-74 诱导癌细胞凋亡 (apoptosis)。

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EGFR-IN-74

EGFR-IN-74 Chemical Structure

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EGFR-IN-74 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-IN-74 (Compound 21) is a potent EGFR inhibitor with an IC50 of 138 nM against EGFR L858R/T790M. EGFR-IN-74 induces cancer cell apoptosis[1].

IC50 & Target[1]

EGFRL858R/T790M

138 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.99 μM
Compound: 21
Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human A549 cells overexpressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
A549 IC50
2.99 μM
Compound: 21
Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
BEAS-2B IC50
85.14 μM
Compound: 21
Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
HCC827 IC50
0.01 μM
Compound: 21
Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human HCC827 cells harboring EGFR E746_A750 del mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
NCI-H1975 IC50
0.21 μM
Compound: 21
Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
Anticancer activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 36375337]
体外研究
(In Vitro)

EGFR-IN-74 (Compound 21) (72 h) 显示出对具有不同 EGFR 状态的细胞的抗癌活性[1]。
EGFR-IN-74 (0.01 μM; 24 and 48 h) 诱导癌细胞凋亡[1]。
EGFR-IN-74 与 EGFR 酶形成稳定的复合物，没有太多的结构重排[1]。

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

EGFR-IN-74 相关抗体:

Cell Viability Assay[1]

Cell Line: HCC827 (EGFR Del E746-A750), NCI–H1975 (EGFR L858R/T790 M), A549 (WT EGFR), A549 and BEAS-2B cells
Concentration:
Incubation Time: 72 h
Result: Inhibited cell viability with IC50s of 0.010 ± 0.02, 0.21 ± 0.99, 0.99 ± 0.11, 2.99 ± 0.21 and 85.14 ± 0.12 μM against HCC827 (EGFR Del E746-A750), NCI–H1975 (EGFR L858R/T790 M), A549 (WT EGFR), A549 and BEAS-2B cells respectively.

Western Blot Analysis[1]

Cell Line: HCC827 cells
Concentration: 0.01, 0.10 and 1.00 μM
Incubation Time:
Result: Showed an ability to phosphorylate AKT.

Apoptosis Analysis[1]

Cell Line: HCC827 cells
Concentration: 0.010 μM (IC50 value)
Incubation Time: 24 and 48 h
Result: Induced early apoptosis and late apoptosis of 26.8% and 4.2% respectively, in comparison with control, with early apoptosis of 2.1% and late apoptosis of 1.1%.
分子量

729.57

Formula

C32H28BrF3N6O4S
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-74 相关分类

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  • 稀释计算器

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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-IN-74EGFREpidermal growth factor receptorErbB-1HER1HCC827NCI–H1975A549Inhibitorinhibitorinhibit

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