Alpelisib hydrochloride

Modify Date: 2024-01-10 20:37:50

Alpelisib hydrochloride structure	Common Name	Alpelisib hydrochloride
	CAS Number	1584128-91-5	Molecular Weight	477.93
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₉H₂₃ClF₃N₅O₂S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Alpelisib hydrochloride

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

Name	Alpelisib hydrochloride

Description	Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> PI3K/Akt/mTOR >> 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)[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]. 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.
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]. 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.
References	[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.

Molecular Formula	C₁₉H₂₃ClF₃N₅O₂S
Molecular Weight	477.93