BYL-719CAS号： 1217486-61-7分子式： C19H22F3N5O2S分子量： 441.47描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
BLY719 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
阿培利司; Alpelisib; BYL-719; BYL 719
|
| 外观 |
White solid
|
| 可溶性/溶解性 |
DMSO：88 mg/mL (199.33 mM)
Ethanol 2 mg/mL (4.53 mM) |
| 生物活性 | |
| 靶点 |
PI3Kα
|
| In vitro(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.
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| In vivo(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.
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分子结构图
