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Erlotinib

CAS No. : 183321-74-6

MCE 国际站：Erlotinib

产品活性：Erlotinib (CP-358774) 是一种直接作用的 EGFR 酪氨酸激酶抑制剂，对人 EGFR 的 IC₅₀ 为 2 nM。Erlotinib 可降低完整肿瘤细胞的 EGFR 自磷酸化，IC₅₀ 为 20 nM。Erlotinib 用于非小细胞肺癌的研究。Erlotinib 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点：EGFR  |  Autophagy

In Vitro: Erlotinib (CP-358774) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC₅₀ of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC₅₀ of 100 nM for an 8-day proliferation assay. The combination of B-DIM and Erlotinib (2 μM) results in a significant inhibition of colony formation in BxPC-3 cells when compared with either agent alone. The combination of B-DIM and Erlotinib (2 μM) results in a significant induction of apoptosis only in BxPC-3 cells when compare with the apoptotic effect of either agent alone.

In Vivo: Under the experimental conditions, the combination of B-DIM and Erlotinib (50 mg/kg, i.p.) treatment shows significant decrease (P <0.01) in tumor weight compared with untreated control. Erlotinib (20 mg/kg, p.o.) significantly attenuates Cisplatin (CP)-induced body weight (BW) loss when compared to the CP+vehicle (V) rats (P<0.05). Erlotinib treatment significantly improves renal function in CP-N(normal control group, NC) rats. The CP+Erlotinib (E) rats show significant reduction of the levels of Serum creatinine (s-Cr) (P<0.05), blood urea nitrogen (BUN) (P<0.05), urinary N-acetyl-β-D-glucosaminidase (NAG) index (P<0.05), and significant increase of urine volume (UV) (P<0.05) and Cr clearance (Ccr) (P<0.05) compare to the CP+V rats^[3]</sup.

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