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Erlotinib

Catalog No. A11416
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EGFR 抑制剂

Erlotinib是一种表皮生长因子受体抑制剂（EGFR抑制剂），抑制纯化 EGFR 激酶的 IC50 为2 nM。厄洛替尼以可逆方式与受体的三磷酸腺苷（ATP）结合位点结合。为了传递信号，需要将两个EGFR分子聚在一起形成同型二聚体。然后，这些分子利用ATP分子在酪氨酸残基上彼此进行反磷酸化，从而产生磷酸酪氨酸残基，将磷酸酪氨酸结合蛋白募集到EGFR，从而组装将信号级联转导至细胞核或激活其他细胞生化过程的蛋白复合物。当厄洛替尼与EGFR结合时，就不可能在EGFR中形成磷酸酪氨酸残基，并且不会引发信号级联。了解更多

Product Citations (5)

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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Manabe A, .et al. Upregulation of transient receptor potential melastatin 6 channel expression by rosiglitazone and all-trans-retinoic acid in erlotinib-treated renal tubular epithelial cells, J Cell Physiol, 2018, Nov 21 PMID: 30461012
- Yui Takashina, .et al. Sodium Citrate Increases Expression and Flux of Mg2+ Transport Carriers Mediated by Activation of MEK/ERK/c-Fos Pathway in Renal Tubular Epithelial Cells, Nutrients, 2018, Oct; 10(10): 1345 PMID: 30241394
- Furukawa C, .et al. Up-Regulation of Transient Receptor Potential Melastatin 6 Channel Expression by Tumor Necrosis Factor-α in the Presence of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, J Cell Physiol, 2017, Oct;232(10):2841-2850 PMID: 27925186
- Xiaoyu Yang, .et al. Knockdown delta-5-desaturase promotes the formation of a novel free radical byproduct from COX-catalyzed ω-6 peroxidation to induce apoptosis and sensitize pancreatic cancer cells to chemotherapy drugs, Free Radic Biol Med, 2016, Aug; 97: 342-350 PMID: 27368132
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Erlotinib mesylate

Catalog No. A15081
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EGFR 抑制剂

Erlotinib mesylate是人EGFR酪氨酸激酶的直接作用抑制剂，IC50为2 nM。了解更多

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Erlotinib HCl

Catalog No. A10362
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EGFR 抑制剂

Erlotinib hydrochloride是一种可逆的酪氨酸激酶抑制剂，作用于表皮生长因子受体（EGFR）。了解更多

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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Aikawa S, .et al. Proliferation of mouse endometrial stromal cells in culture is highly sensitive to lysophosphatidic acid signaling, Biochem Biophys Res Commun, 2017, Feb 26;484(1):202-208 PMID: 28073697
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OSI-420

Catalog No. A10678
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EGFR 抑制剂

OSI-420 (Desmethyl Erlotinib,CP-473420)是一种口服活性EGFR酪氨酸激酶抑制剂，可通过抑制细胞间结构域来抑制受体酪氨酸激酶（TKs）。了解更多

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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Janet L. Martin, .et al. Inhibition of basal-like breast cancer growth by FTY720 in combination with epidermal growth factor receptor kinase blockade, Breast Cancer Res, 2017, 19: 90 PMID: 28778177