2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis Immunology/Inflammation
  3. EGFR TNF Receptor Interleukin Related Apoptosis
  4. EGFR-IN-200

EGFR-IN-200 是靶向 EGFR、TNF-α 以及 IL-6/GP130 复合物的抑制剂，能高效靶向人源 EGFR (IC50=0.03 μM)、TNF-α (IC50=3.1 μM) 及 IL-6/GP130 复合物 (IC50=1.6 μM)。EGFR-IN-200 可结合 EGFR 的 ATP 口袋、TNF-α 的三聚体界面以及 IL-6/GP130 的细胞因子-受体界面，诱导细胞周期 G2/M 期阻滞、细胞凋亡 (apoptosis) 和抗增殖活性。EGFR-IN-200 具有较高的胃肠道吸收性、低 BBB 通透性，且符合 Lipinski 规则。EGFR-IN-200 可用于肺癌、乳腺腺癌的研究。

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EGFR-IN-200

EGFR-IN-200 Chemical Structure

CAS No. : 3102899-89-5

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EGFR-IN-200 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 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-200 is an inhibitor targeting EGFR, TNF-α, and the IL-6/GP130 complex, which potently targets human EGFR (IC50=0.03 μM), TNF-α (IC50=3.1 μM), and the IL-6/GP130 complex (IC50=1.6 μM). EGFR-IN-200 binds to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, induces G2/M cell cycle arrest, apoptosis, and antiproliferative activity. EGFR-IN-200 exhibits high gastrointestinal absorbability, low BBB permeability, and complies with the Lipinski's rule. EGFR-IN-200 can be used for the research of lung cancer and breast adenocarcinoma[1].

体外研究
(In Vitro)

EGFR-IN-200 (compound 5h) 可强效抑制 A549 和 MCF-7 癌细胞的活力，IC50 值分别为 9.2 μM 和 8.2 μM，且对恶性细胞相对非致瘤细胞表现出高选择性[1]。
EGFR-IN-200 (0.01-100 μM; 1 h) 可强效抑制 EGFR 酪氨酸激酶活性，IC50 为 0.03 μM，活性优于 Erlotinib (HY-50896)[1]。
EGFR-IN-200 直接结合 TNF-α 和 IL-6，其中与 TNF-α 结合的 Kd 为 2.3 μM，与 IL-6 结合的 Kd 为 1.8 μM[1]。
EGFR-IN-200 可诱导 A549 细胞发生 G2/M 期细胞周期阻滞，阻断有丝分裂前的进程，并诱导 A549 细胞发生凋亡，总凋亡率达 82.15%，且更倾向于诱导早期凋亡[1]。

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

EGFR-IN-200 相关抗体:
分子量

499.94

Formula

C28H22ClN3O4
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-200 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

EGFR-IN-2003102899-89-5EGFRTNF ReceptorInterleukin RelatedApoptosisEpidermal growth factor receptorErbB-1HER1Tumor Necrosis Factor ReceptorTNFRILMCF-7 cellshuman EGFRA549 cellsEGFR tyrosine kinaseTNF-αapoptosisG2/M phase cell cycle arrestlung carcinomaIL-6/GP130 complexbreast adenocarcinomaInhibitorinhibitorinhibit

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