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エルロチニブ

(別名: Erlotinib; NSC 718781; CP-358774; OSI-774)
143 Cited Publications
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Based on 143 publication(s) in Google Scholar

Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions.

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  • 純度: 99.96%
  • CAS 番号: 183321-74-6
  • 分子式: C22H23N3O4
  • 分子量:393.44
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • Erlotinib Chemical Structure
    Erlotinib 構造式
  • Experimental Validation Results for Erlotinib
  • Experimental Validation Results for Erlotinib
  • Experimental Validation Results for Erlotinib
  • Experimental Validation Results for Erlotinib
  • Experimental Validation Results for Erlotinib
  • Experimental Validation Results for Erlotinib
CAS 番号: 183321-74-6
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  • Erlotinib Chemical Structure
    Erlotinib Chemical Structure
    1/16
  • 1/16

    Erlotinib purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 May;13(10):e7083. [Abstract]

    Customer Validation
     FACS analysis was used to perform the MFI of cell membrane of PD‐L1 in H441 cells with control or multiply small molecular inhibitors (Seen in the Table 1, 24 h) (n = 3). AV412 (HY‐10346; 20, 50 nM), ERK1/2 inhibitor 1 (HY‐112287; 20, 50 nM), AR‐A014418 (HY‐10512; 100, 200 nM), Erlotinib (HY‐50896; 50, 100 nM).

  • 1/16

    Erlotinib purchased from MedChemExpress. Usage Cited in: Cancer Med. 2019 Dec;8(18):7793-7808. [Abstract]

    Customer Validation
     Western blots of proteins expression in EGFR signaling pathways in LN229 and U87 cells with MYST1/GFP overexpression after erlotinib (200 ng/mL)/DMSO treatment.

  • 1/16

    Erlotinib purchased from MedChemExpress. Usage Cited in: Anal Chim Acta. 2018 Nov 22:1032:138-146. [Abstract]

    Customer Validation
     30 min after EGF(100 ng/mL) and EGFP-sSH2(Arg)9 (5 μM) are added into the MDA-MB-468 cell culture medium, Erlotinib is added into the cell culture medium (100 nM), and the picture was collected at 30 min after Erlotinib treatment.

  • 1/16

    Erlotinib purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21:9:660. [Abstract]

    Customer Validation
     By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

  • 1/16

    Erlotinib purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321. [Abstract]

    Customer Validation
     Western blot analysis of total and phosphorylated EGFR expression in two breast cancer cells pretreated with different concentration Erlotinib for 4h.

  • 1/16

    Erlotinib purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 May 11;36(19):2643-2654. [Abstract]

    Customer Validation
     Effects of anti-cancer agents Oxaliplatin, Erlotinib (25 μM) and cAMP inducer Forskolin (25 μM) on FOXO3 expression in Panc-1 cells are assessed for 72 h (n=3).

  • Erlotinib