2088323-16-2

2088323-16-2 structure

Name: TAS0728
Chemical Name: TAS0728
CAS Number: 2088323-16-2
Molecular Formula: C₂₆H₃₂N₈O₃
Molecular Weight: 504.58
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2019-03-31 00:52:34
Modify Date: 2024-01-14 14:03:16
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].

Name	TAS0728

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.

Molecular Formula	C₂₆H₃₂N₈O₃
Molecular Weight	504.58