MCE 的所有产品仅用作科学研究，我们不为任何个人用途提供产品和服务。

Alpelisib hydrochloride

CAS No. : 1584128-91-5

MCE 站：Alpelisib hydrochloride

产品活性：Alpelisib hydrochloride (BYL-719 hydrochloride) 是有效，具有口服活性的，选择性的 PI3Kα 抑制剂，抑制 p110α/p110γ/p110δ/p110β 的 IC₅₀ 分别为 5 nM，250 nM，290 nM，1200 nM。Alpelisib hydrochloride (BYL-719 hydrochloride) 具有抗肿瘤活性。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: Alpelisib (BYL-719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC₅₀s~4 nM). Alpelisib potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC₅₀=74±15 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (≥15-fold compared with PI3Kα).
Alpelisib (BYL-719, 0-50 μM; 72 hours) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 and MOS-J in a dose-dependent manner.
Alpelisib (BYL-719) significantly alters the distribution of cell cycle phases. Alpelisib (BYL-719, 25 μM; 18 hours) induces a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell lines.

In Vivo: Alpelisib (BYL-719) (12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice; oral administration; daily) significantly reduces tumor volumes and deposition of ectopic bone matrix.
Alpelisib has moderate terminal elimination half-life (t_1/2=2.9±0.2 h) for rat (1 mg/kg, iv).

相关产品：3-Methyladenine  |  LY294002  |  Alpelisib  |  Wortmannin  |  Quercetin  |  Copanlisib  |  Buparlisib  |  Idelalisib  |  740 Y-P  |  Pictilisib  |  IPI549  |  Dactolisib  |  Fimepinostat  |  SAR405  |  Duvelisib  |  PI-103  |  GDC-0077  |  LY3023414  |  Rigosertib sodium  |  PF-04691502  |  GSK2636771  |  Omipalisib  |  YM-201636  |  Taselisib  |  ZSTK474  |  Gedatolisib  |  Parsaclisib  |  TG100-115  |  1,3-Dicaffeoylquinic acid

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。