Zipalertinib

Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM[1][2].

Product Specifications

CAS Number

[1661854-97-2]

Product Name Alternative

TAS6417; CLN-081

UNSPSC

12352005

Target

Apoptosis; EGFR

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/zipalertinib.html

Purity

99.62

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

NC1=C2C(N3C(C(C)=C[C@@H](C3)NC(C=C)=O)=C2C4=CC5=CC=CC=C5N=C4)=NC=N1

Molecular Formula

C23H20N6O

Molecular Weight

396.44

References & Citations

[1]Hasako S, et al. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17 (8) :1648-1658.|[2]Hibiki Udagawa, et al. TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. Mol Cancer Res. 2019 Nov;17 (11) :2233-2243.