Medchemexpress LLC 1H-Pyrazolo[3,4-d]pyrimidine-3-carboxamide, 4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]] | 2088323-16-2 | 99.7% | 504.58 | 25 MG

Supplier:  Medchemexpress LLC 25MGHY111553

TAS0728 is a potent, selective, orally active, irreversible, and covalent-binding HER2 inhibitor with an IC50 of 13 nM. It also demonstrates inhibitory activities against BMX, HER4, BLK, EGFR, JAK3, SLK, and LOK with IC50s of 4.9, 8.5, 31, 65, 33, 25, and 86 nM, respectively. TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors.

• Inhibits proliferation of five HER2-amplified cell lines with GI50 values ranging from 1.6 to 6.9 nM.
• Shows sustained inhibition of HER2, HER3, AKT, and ERK phosphorylation in SK-BR-3 cells.
• Provides sustained and targeted inhibition of HER2, HER3, AKT, and ERK phosphorylation in vivo.
• Causes tumor regression and exhibits low toxicity in animal models.
• Demonstrated sustained target inhibition and was well tolerated in male nude mice.
• Significant tumor regression observed at higher doses in xenograft models.

Catalog No. 50-003-46692