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Chemical Structure : TAS6417
CAS No.: 1661854-97-2
Catalog No.: PC-63499Not For Human Use, Lab Use Only.
Zipalertinib (TAS6417, CLN-081) is a novel potent, selective inhibitor of EGFR exon 20 insertion mutations with IC50 of 1.1-8.0 nM, >100-fold selectivity over WT EGFR.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $288 | In stock | |
| 25 mg | $488 | In stock | |
| 100 mg | $1280 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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Zipalertinib (TAS6417, CLN-081) is a novel potent, selective inhibitor of EGFR exon 20 insertion mutations with IC50 of 1.1-8.0 nM, >100-fold selectivity over WT EGFR.
Zipalertinib (TAS6417) fits into the ATP-binding site of the EGFR hinge region.
Zipalertinib (TAS6417) inhibits EGFR phosphorylation and downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions (IC50=20-100 nM), resulting in caspase activation.
Zipalertinib (TAS6417) inhibits the proliferation of Ba/F3 cells driven by various EGFR exon 20 insertion mutations with IC50 of 5.05-150 nM.
Zipalertinib (TAS6417) causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models.
| M.Wt | 396.454 | |
| Formula | C23H20N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide |
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1. Hasako S, et al. Mol Cancer Ther. 2018 May 10. pii: molcanther.1206.2017.
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