TAS0728
Product Specifications
UNSPSC Description
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors[1].
Target Antigen
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/TAS0728.html
Purity
99.15
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
NC1=C2C(N([C@H]3CN(C(C=C)=O)CCC3)N=C2C(NC4=CC=C(CC(N(C)C)=O)C(C)=C4C)=O)=NC=N1
Molecular Weight
504.58
References & Citations
[1]Irie H, et al. TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models. Molecular cancer therapeutics. 2019;18(4):733-42. Epub 2019/02/23.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-111553/TAS0728-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-111553/TAS0728-SDS-MedChemExpress.pdf
Clinical Information
Phase 1
CAS Number
2088323-16-2
Available Sizes
Curated Selection
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