Alpelisib-hydrochloride-BYL-719-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAlpelisib hydrochlorideCat. No.: HY-15244ACAS No.: 1584128-91-5Synonyms: BYL-719 hydrochloride分式: CHClFNOS分量: 477.93作靶点: PI3K作通路: PI3K/Akt/mTOR储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL A

2、CTIVITY物活性 Alpelisib hydrochloride (BYL-719 hydrochloride)有效，选择性的 PI3K 抑制剂，抑制 p110/p110/p110/p110 的 IC50 分别为 5 nM，250 nM，290 nM，1200 nM 1。体外研究Alpelisib (BYL-719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K;IC50s4 nM). Alpelisib potently inhibits Akt phosphorylation in

3、 cells transformed with PI3K (IC50=7415nM) and shows significant reduced inhibitory activity in PI3K or PI3K isoforms transformed cells (15-foldcompared with PI3K) 2.Alpelisib (BYL-719, 0-50 M; 72 hours) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 and MOS-J in a dose-depende

4、nt manner 3.Alpelisib (BYL-719) significantly alters the distribution of cell cycle phases. Alpelisib (BYL-719, 25 M; 18hours) induces a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell lines 3.Cell Proliferation Assay 3Cell Line: MG63, HOS, POS-1, MOS-JConcentration: 10, 2

5、0, 30, 40, 50 MIncubation Time: 72 hoursResult: Inhibited the cell growth of all osteosarcoma cell lines tested in a dose-dependentmanner with IC50s of 6-15 M and with IC90s of 24-42 M.1/3 Master of Small Molecules 您边的抑制剂师www.MedChemECell Cycle Analysis 3Cell Line: MG63, HOS, POS-1, MOS-JConcentrati

6、on: 25 MIncubation Time: 18 hoursResult: Induced a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell.体内研究 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

7、 deposition of ectopic bone matrix 3.Alpelisib has moderate terminal elimination half-life (t1/2=2.90.2 h) for rat (1 mg/kg, iv) 1.Animal Model: A 5-week-old female Rj:NMRI-nude mice with human HOS-MNNG osteosarcoma cells; A5-week-old male C57Bl/6J mice with mouse MOS-J osteosarcoma cells 3Dosage: 1

8、2.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude miceAdministration: Oral administration; dailyResult: Significantly reduced tumor volumes and simultaneously reduced tumor growth.Animal Model: Female Sprague Dawley rats 1Dosage: 1 mg/kg (Pharmacokinetic Study)Administration

9、: I.V.Result: T1/2=2.90.2 hours. Nature. 2018 Jun;558(7711):540-546. Science. 2017 Dec 1;358(6367). Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Nat Biomed Eng. 2018;2:578-588. Blood. 2019 Jan 3;133(1):70-80.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Furet P, et al.

10、 Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinicalevaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. Fritsch C, et al. Characterization of the novel and specific PI3K inhibito

11、r NVP-BYL719 and development of the patient stratificationstrategy for clinical trials. Mol Cancer Ther. 2014 May;13(5):1117-29.3. Gobin B, et al. BYL719, a new -specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for thetreatment of osteosarcoma. Int J Cancer. 2015 Feb 15;136(4):784-96.McePdfHeightCaution: Product has no