Alpelisib (BYL719)，中国库存，PI3K抑制剂，Selleck Chemicals美国品牌，CAS#1217486-61-7。
产品名称： Alpelisib (BYL719)，中国库存，PI3K抑制剂，Selleck Chemicals美国品牌，CAS#1217486-61-7。
英文名称： Alpelisib (BYL719)
产品编号： S2814
产品价格： 0
产品产地： 美国
品牌商标： SELLECK
更新时间： null
使用范围： null
selleck产品在文献中的引用:
| Br J Haematol, 2013, 10.1111/bjh.12734 |
客户使用selleck产品的实验数据：
更多详情请访问中国唯一官方网站www.selleck.cn/products/byl719.html
生物活性
| 产品描述 | BYL719是一种有效的，选择性的PI3Kα抑制剂，IC50为5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 1/2。 | |||||
|---|---|---|---|---|---|---|
| 靶点 | PI3Kα | |||||
| IC50 | ||||||
| 体外研究 | BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway. [1] | |||||
| 体内研究 | BYL719(>270 mg/d) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC in human. BYL719(270mg/d) shows first signs of clinical efficacy include 1 confirmed partial response in a patient with ER+ breast cancer, and significant PET responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17 evaluated patients. [1] | |||||
| 临床实验 | BYL719 is currently in Phase II clinical trial in adult patients with selected advanced solid tumors. | |||||
| 特征 | ||||||