2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. EGFR-IN-107

EGFR-IN-107 (compound 3r) 是一种具有口服活性的 EGFR 抑制剂，对 EGFRWT 和 EGFRL858R/T790M 的 IC50 值分别为 0.4333 μM 和 0.0438 μM。EGFR-IN-107 具有抗增殖活性，能抑制 H1975 细胞的增殖并诱导其凋亡 (apoptosis)。EGFR-IN-107 可用于癌症研究。

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EGFR-IN-107 Chemical Structure

EGFR-IN-107 Chemical Structure

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EGFR-IN-107 相关抗体

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查看 EGFR 亚型特异性产品:

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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-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research[1].

体外研究
(In Vitro)

EGFR-IN-107 对 EGFRL858R/T790M 激酶的 IC50 值为 5 nM[1]。
EGFR-IN-107 对 Osimertinib (HY-15772) 耐药 H1975 细胞系 (H1975OR) 的 IC50 值为 1.9 μM[1]。
EGFR-IN-107 (1 μM, 24 小时) 在 H1975 细胞中能诱导细胞凋亡及抑制细胞迁移[1]。

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

EGFR-IN-107 相关抗体:

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 1 μM
Incubation Time: 24h
Result: Up-regulated the expression levels of Bax, cleaved caspase-3 and E-cadherin, and down-regulated the expression levels of matrix metalloproteinase-2 (MMP-2) and anti-apoptotic marker Bcl-2.
体内研究
(In Vivo)

EGFR-IN-107 (compound 3r) (5, 10, 20 mg/kg; 口服; 21 天) 在 H1975 异种移植小鼠模型中具有较强的抗肿瘤活性，并且能够显著抑制 H1975 异种移植小鼠模型的增殖[1]。

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

Animal Model: H1975 xenograft mouse model[1]
Dosage: 5, 10, 20 mg/kg
Administration: Oral gavage (p.o.); 21days
Result: At 20 mg/kg showed the same antitumor effect as Osimertinib (HY-15772) (20 mg/kg).
Leaded to the down-regulation of p-EGFR.
Did not cause significant weight loss or tissue damage.
分子量

593.69

Formula

C34H36FN7O2
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-107 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-107EGFRApoptosisEpidermal growth factor receptorErbB-1HER1H1975 cellsanti-proliferationCell migrationH1975 xenograft mouse modelInhibitorinhibitorinhibit

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