产品
编 号：F255531
分子式：C26H32N8O3
分子量：504.58
分子式：C26H32N8O3
分子量：504.58
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2088323-16-2
产品详情
生物活性：
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors.
体内研究：
TAS0728 揭示了对 HER2、HER3、AKT 和 ERK 磷酸化的持续和靶向抑制。TAS0728 还显示出肿瘤消退和低毒性的能力。Animal Model:Male nude mice
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: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.
体外研究：
TAS0728 是 HER2 激酶的共价结合抑制剂，对 HER2 激酶表现出高选择性。它还显示出对 BMX、HER4、BLK、EGFR、JAK3、SLK 和 LOK 的抑制活性。
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors.
体内研究：
TAS0728 揭示了对 HER2、HER3、AKT 和 ERK 磷酸化的持续和靶向抑制。TAS0728 还显示出肿瘤消退和低毒性的能力。Animal Model:Male nude mice
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: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.
体外研究：
TAS0728 是 HER2 激酶的共价结合抑制剂，对 HER2 激酶表现出高选择性。它还显示出对 BMX、HER4、BLK、EGFR、JAK3、SLK 和 LOK 的抑制活性。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备