Alpelisib hydrochloride(Synonyms: BYL-719 hydrochloride)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Alpelisib hydrochloride (Synonyms: BYL-719 hydrochloride)

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。

Alpelisib hydrochloride(Synonyms: BYL-719 hydrochloride)

Alpelisib hydrochloride Chemical Structure

CAS No. : 1584128-91-5

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Alpelisib hydrochloride 的其他形式现货产品:

Alpelisib

生物活性

Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. Alpelisib hydrochloride (BYL-719 hydrochloride) shows antineoplastic activity[1][2].

体外研究
(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)[2].
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[3].
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[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

Cell Line: MG63, HOS, POS-1, MOS-J
Concentration: 10, 20, 30, 40, 50 μM
Incubation Time: 72 hours
Result: Inhibited the cell growth of all osteosarcoma cell lines tested in a dose-dependent manner with IC50s of 6-15 µM and with IC90s of 24-42 µM.

Cell Cycle Analysis[3]

Cell Line: MG63, HOS, POS-1, MOS-J
Concentration: 25 μM
Incubation Time: 18 hours
Result: Induced a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell.

体内研究
(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[3].
Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A 5-week-old female Rj:NMRI-nude mice with human HOS-MNNG osteosarcoma cells; A 5-week-old male C57Bl/6J mice with mouse MOS-J osteosarcoma cells[3]
Dosage: 12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice
Administration: Oral administration; daily
Result: Significantly reduced tumor volumes and simultaneously reduced tumor growth.
Animal Model: Female Sprague Dawley rats [1]
Dosage: 1 mg/kg (Pharmacokinetic Study)
Administration: I.V.
Result: T1/2=2.9±0.2 hours.

Clinical Trial

分子量

477.93

Formula

C19H23ClF3N5O2S
CAS 号

1584128-91-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Furet P, et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8.

    [2]. Fritsch C, et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther. 2014 May;13(5):1117-29.

    [3]. Gobin B, et al. BYL719, a new α-specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for the treatment of osteosarcoma. Int J Cancer. 2015 Feb 15;136(4):784-96.

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