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Medchemexpress LLC Zipalertinib | 1661854-97-2 | 99.6% | 396.44 | 10 MG

Supplier: Medchemexpress LLC HY11229910MG
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active, and pan-mutation-selective EGFR tyrosine kinase inhibitor. It features a unique scaffold that fits into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM. It inhibits EGFR phosphorylation and downstream molecules in NSCLC cell lines and causes persistent tumor regression in EGFR exon 20 insertion-driven tumor models.
- Highly effective, orally active, and pan-mutation-selective EGFR tyrosine kinase inhibitor
- Inhibits EGFR phosphorylation and downstream molecules
- Causes caspase activation
- Robust against common EGFR mutations and potent against cells with EGFR-T790M
- Inhibits mutant EGFR in tumors but not wild-type EGFR in skin
- Promotes cell growth inhibition and apoptosis
- Prolongs survival in animal models of lung cancer
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