TAS0728

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].

Product Specifications

CAS Number

[2088323-16-2]

UNSPSC

12352005

Hazard Statement

H315, H319

Target

Ser/Thr Kinase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TAS0728.html

Concentration

10mM

Purity

99.71

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 Formula

C26H32N8O3

Molecular Weight

504.58

Precautions

H315, H319

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.