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Zipalertinib

CAS No. : 1661854-97-2

MCE 站：Zipalertinib

产品活性：Zipalertinib (TAS6417; CLN-081) 是高效的、具有口服活性的、广泛的 EGFR 突变型的抑制剂，可独特的结合到 EGFR 铰链区的 ATP 结合位点，其 IC₅₀ 值为 1.1-8.0 nM。

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

作用靶点：EGFR  |  Apoptosis

In Vitro: Zipalertinib (TAS6417) inhibits EGFR phosphorylation ａnd downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions, resulting in caspase activation.
?Zipalertinib (TAS6417) is a robust inhibitor against the most common EGFR mutations (exon 19 deletions ａnd L858R) ａnd the most potent against cells harboring EGFR-T790M (1st/2nd generation TKI resistance mutation).
?Zipalertinib (TAS6417) covalently modified the cysteine residue at position 797 of recombinant EGFR harboring an in-frame insertion mutation in the exon 20 region.
?Zipalertinib (TAS6417) inhibits EGFR signal transduction, leading to cell growth inhibition ａnd apoptosis induction in NSCLC cells driven by EGFR exon 20 insertion mutations.
?Zipalertinib (TAS6417) (0-10 μM) inhibits cell proliferation ａnd EGFR signaling in NSCLC cell lines harboring EGFR common mutations in the presence or absence of T790M.

In Vivo: Zipalertinib (TAS6417) (10-200 mg/kg) causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues.
?Zipalertinib (TAS6417) had no effect on EGFR-independent proliferation in NCI-H23 or NCI-H460 cells.
?Zipalertinib (TAS6417) administered at 20 mg/kg, which achieves complete suppression of tumor growth, induces a significant decrease in pEGFR, leading to reduction of pAKT ａnd pERK at 1 h. The inhibitory effect is still noted at 6 h, ａnd phosphorylation of EGFR, ATK, ａnd ERK recovered by 24 h.
?Zipalertinib (TAS6417) (100 ａnd 200 mg/kg/day) prolongs survival of animals bearing lung cancer.

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