[CAS NO. 2088323-16-2] TAS0728
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PRODUCTS SPECIFICATIONS [2088323-16-2]
Catalog
SLK-S8833
Brand
Selleck
CAS
2088323-16-2
DESCRIPTION [2088323-16-2]
Overview
| MDL | MFCD31813813 |
|---|---|
| Molecular Weight | 504.58 |
| Molecular Formula | C26H32N8O3 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
TAS0728 (TPC 107) is a potent, selective, orally active, irreversible and covalent-binding inhibitor of with IC50 of 13 nM. TAS0728 inihibits BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2 with IC50 of 4.9 nM, 8.5 nM, 31 nM, 65 nM, 33 nM, 25 nM, 86 nM and 36 nM, respectively. TAS0728 shows antitumor activity.
Targets
| HER2 [1] (Cell-free assay) |
| 13 nM |
In vitro
TAS0728 covalently binds to HER2 at C805 and selectively inhibits its kinase activity. Once TAS0728 binds to HER2 kinase, the inhibitory activity is not affected by a high ATP concentration. TAS0728 possesses high specificity for HER2 over wild-type EGFR. TAS0728 potently inhibits the phosphorylation of mutated HER2 and wild-type HER2. TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors, thereby inducing apoptosis of HER2-amplified breast cancer cells.
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