TAS0728

Names

[ CAS No. ]:
2088323-16-2

[ Name ]:
TAS0728

Biological Activity

[Description]:

TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

HER4:8.5 nM (IC50)

HER2:13 nM (IC50)

Human HER2:36 nM (IC50)

EGFR:65 nM (IC50)

BMX:4.9 nM (IC50)

BLK:31 nM (IC50)

JAK3:33 nM (IC50)

SLK:25 nM (IC50)

LOK:86 nM (IC50)

[References]

[1]. Irie H, et al. TAS0728, a covalent-binding, HER2-selective kinase inhibitor shows potent antitumor activity in preclinical models. Mol Cancer Ther. 2019 Feb 20.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₃₂N₈O₃

[ Molecular Weight ]:
504.58

Related Compounds

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