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Nazartinib

CAS No. : 1508250-71-2

MCE 国际站：Nazartinib

产品活性：Nazartinib (EGF816) 是一种 EGFR 抑制剂，对 EGFR(L858R/790M) 突变体的 K_i 和 K_inact 值分别为 31 nM 和 0.222 min⁻¹。

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

作用靶点：EGFR

In Vitro: Nazartinib (EGF816) has inhibitory effect on the mutant cell lines with IC₅₀s of 4, 6, 2 nM in H1975, H3255, and HCC827, respectively, and demonstrates improved ADME and PK properties. Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines with EC₅₀ values of 5, 1, and 3 nM, respectively. Nazartinib inhibits cell proliferation, with EC₅₀ values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Nazartinib has an OC₅₀ (compound concentration at 50% occupancy) value of 2 and 5 nM on HCC827 and H1975, respectively.

In Vivo: In H1975 mouse xenograft model, Nazartinib (EGF816; 50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near complete tumor cells regression at the highest dose tested (50 mg/kg). In H1975 mouse model, Nazartinib (EGF816; 10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, -61% and -80%, respectively). In the H3255 xenograft model, Nazartinib (30 mg/kg, p.o.) shows significant antitumor activity. Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations.

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