TAS0728

Research use only, not for human use.

TAS0728 is a HER2 inhibitor with antitumor activity.

TAS0728 is a HER2 inhibitor with antitumor activity.

Cell Cytotoxicity Assay Cell Line:HER2-amplified SK-BR-3/AU565/BT-474/NCI-N87/Calu-3 cells Concentration:Incubation Time:Result:The GI50 values of TAS0728 were 5.0/5.1/3.6/1.6/6.9 nM relatively for HER2-amplified SK-BR-3/AU565/BT-474/NCI-N87/Calu-3 cells. Inhibited the in vitro proliferation of five HER2-amplified cell lines.Showed potent inhibitory activities against cancer cell lines with HER2 amplification.Western Blot Analysis Cell Line:SK-BR-3 cells Concentration:30-300 nM Incubation Time:3 and 48 hours Result:Showed sustained inhibition of HER2, HER3, AKT and ERK phosphorylation.

Animal Model:Male nude miceDosage:7.5, 15, 30 and 60 mg/kg Administration:Oral gavage; 7.5, 15, 30 and 60 mg/kg a day;14 days Result:Rapidly eliminated within 24 hours.Animal Model:Mice bearing NCI-N87 xenografts Dosage:60 mg/kg Administration:Oral gavage; 60 mg/kg a day; 14 days Result:Revealed sustained target inhibition of HER2, HER3, AKT and ERK. Animal Model:Mice with NCI-N87 HER2–amplified human gastric cancer Dosage:7.5, 15, 30 and 60 mg/kg Administration:Oral gavage; 7.5, 15, 30 and 60 mg/kg a day; 14 days Result:Well tolerated in all mice.Significant tumor regression was observed in mice treated with 60 mg/kg/day.Animal Model:NCI-N87 peritoneal dissemination model Dosage:30 and 60 mg/kg Administration:Oral gavage; 30and 60 mg/kg a day; 120 days Result:No evident toxicity, including diarrhea and body weight loss in the long-term dosing of TAS0728.

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Angiogenesis

HER/HSP

HER2

Cancer

Advanced Solid Tumors

2088323-16-2

504.58

C26H32N8O3

>98% (HPLC)

DMSO:125 mg/mL (247.73 mM)

C=CC(=O)N1CCCC(n2nc(C(=O)Nc3ccc(CC(=O)N(C)C)c(C)c3C)c3c(N)ncnc32)C1

(R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-23-dimethylphenyl)-1H-pyrazolo[34-d]pyrimidine-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years