Zipalertinib (TAS6417) | EGFR Ex20Ins inhibitor | Probechem Biochemicals

Chemical Structure : TAS6417

CAS No.: 1661854-97-2

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TAS6417 (Zipalertinib, TAS-6417, CLN-081)

货号: 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.

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10 mg	￥2280	In stock
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50 mg	￥5980	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	396.454
分子式	C23H20N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide

参考文献

1. Hasako S, et al. Mol Cancer Ther. 2018 May 10. pii: molcanther.1206.2017.

TAS6417 (Zipalertinib, TAS-6417, CLN-081)

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物理化学性质&存储条件

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TAS6417 (Zipalertinib, TAS-6417, CLN-081)

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