产品
编 号：F489819
分子式：C26H25ClF3N5O3
分子量：547.96
分子式：C26H25ClF3N5O3
分子量：547.96
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 871026-44-7
产品详情
生物活性：
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
体内研究：
TAK-285 (Compound 34e; 50-100 mg/kg; oral administration; twice daily; for 14 days; female BALB/cAJcl mice) treatment exhibits dose-dependent tumor growth inhibition (tumor/control ratio [T/C]): 44% and 11% at 50 and 100 mg/kg, respectively) without significant body weight loss in mice.Animal Model:Female BALB/cAJcl mice (7-weeks old) with 4?1ST xenograft models
Dosage:50 mg/kg, 100 mg/kg
Administration:Oral administration; twice daily; for 14 days
Result:Exhibited dose-dependent tumor growth inhibition.
体外研究：
TAK-285 (Compound 34e) shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM.TAK-285 (Compound 34e) exhibits HER4 inhibitory activity with an IC50 value of 260 nM. TAK-285 also inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK andLyn B with IC50s of 1100 nM, 5700 nM, 4200 nM, 1700 nM, 2400 nM, 4700 nM and 5200 nM, respectively.
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
体内研究：
TAK-285 (Compound 34e; 50-100 mg/kg; oral administration; twice daily; for 14 days; female BALB/cAJcl mice) treatment exhibits dose-dependent tumor growth inhibition (tumor/control ratio [T/C]): 44% and 11% at 50 and 100 mg/kg, respectively) without significant body weight loss in mice.Animal Model:Female BALB/cAJcl mice (7-weeks old) with 4?1ST xenograft models
Dosage:50 mg/kg, 100 mg/kg
Administration:Oral administration; twice daily; for 14 days
Result:Exhibited dose-dependent tumor growth inhibition.
体外研究：
TAK-285 (Compound 34e) shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM.TAK-285 (Compound 34e) exhibits HER4 inhibitory activity with an IC50 value of 260 nM. TAK-285 also inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK andLyn B with IC50s of 1100 nM, 5700 nM, 4200 nM, 1700 nM, 2400 nM, 4700 nM and 5200 nM, respectively.
产品资料
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