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Alpelisib hydrochloride

Catalog No. T14191 CAS 1584128-91-5

Synonyms: BYL-719 hydrochloride

Alpelisib hydrochloride (BYL-719 hydrochloride) exhibits anticancer properties[1][2]. As a potent, selective PI3Kα inhibitor with high oral bioavailability, it demonstrates IC50 values of 5 nM for p110α, 250 nM for p110γ, 290 nM for p110δ, and 1200 nM for p110β, indicating its efficacy in targeting specific enzymes involved in cancer cell proliferation.

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Alpelisib hydrochloride Chemical Structure

Alpelisib hydrochloride, CAS 1584128-91-5

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,970.00
50 mg	8-10 weeks	$ 2,580.00
100 mg	8-10 weeks	$ 3,400.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description	Alpelisib hydrochloride (BYL-719 hydrochloride) exhibits anticancer properties[1][2]. As a potent, selective PI3Kα inhibitor with high oral bioavailability, it demonstrates IC50 values of 5 nM for p110α, 250 nM for p110γ, 290 nM for p110δ, and 1200 nM for p110β, indicating its efficacy in targeting specific enzymes involved in cancer cell proliferation.
In vitro	Alpelisib (BYL-719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50s~4 nM). 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]. 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 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].
In vivo	Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv)[1]. 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].

Synonyms	BYL-719 hydrochloride
Molecular Weight	477.93
Formula	C19H23ClF3N5O2S
CAS No.	1584128-91-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

Alpelisib hydrochloride 1584128-91-5 Others BYL-719 Hydrochloride Alpelisib Hydrochloride BYL-719 hydrochloride BYL 719 Hydrochloride BYL719 Hydrochloride inhibitor inhibit

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