TAS0728

Modify Date: 2024-01-14 14:03:16

TAS0728 Structure
TAS0728 structure
Common Name TAS0728
CAS Number 2088323-16-2 Molecular Weight 504.58
Density N/A Boiling Point N/A
Molecular Formula C26H32N8O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of TAS0728


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].

 Names

Name TAS0728

 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
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