2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-61

EGFR-IN-61 (compound 22a) 是一种有效的 EGFR 激酶抑制剂，IC50 值分别为 42 nM (L858R/T790 M)、137 nM (L858R/T790 M/C797S) 和 743 nM (WT)。 EGFR-IN-61 对 A549 和 H1975 细胞具有抗增殖活性，IC50 分别为 2.14 和 1.82 μM。

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EGFR-IN-61 Chemical Structure

EGFR-IN-61 Chemical Structure

CAS No. : 2890261-81-9

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EGFR-IN-61 相关抗体

Top Publications Citing Use of Products

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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-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively[1].

IC50 & Target

EGFRL858R/T790M

42 ± 2 nM (IC50)

EGFRL858R/T790M/C797S

137 ± 6 nM (IC50)

EGFR (WT)

743 ± 20 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
2.14 μM
Compound: 22a
Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 35696862]
NCI-H1975 IC50
1.82 μM
Compound: 22a
Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 35696862]
体外研究
(In Vitro)

EGFR-IN-61 (compound 22a) shows excellent kinase selectivity against the L858R/T790M/C797S mutant EGFR kinase rather than the wild-type, which reached 5.4 times[1].

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

EGFR-IN-61 相关抗体:
分子量

629.15

Formula

C33H37ClN8O3
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-61 相关分类

  • 摩尔计算器

  • 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-612890261-81-9EGFREpidermal growth factor receptorErbB-1HER1A549H1975osimertinib derivativesreversible EGFR kinase InhibitorsL858R/T790M/C797S mutationantitumor activityInhibitorinhibitorinhibit

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