Alpelisib hydrochloride (Synonyms: BYL-719 hydrochloride)

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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.

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Alpelisib hydrochloride Chemical Structure

CAS No. : 1584128-91-5

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97 Publications Citing Use of MCE Alpelisib hydrochloride

Cell Viability Assay

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17.; Alpelisib (50 mg/kg; p.o.). Western blot and quantification of P-AKTSer473 and P-S6RP of the skin of PIK3CA^WT and PIK3CA^Tie2-CreER mice treated with either vehicle, rapamycin, miransertib or alpelisib (n = 3–4 per group).

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17.; Alpelisib (50 mg/kg; p.o.). Representative immunofluorescence staining of KI67 in the skin of PIK3CA^WT and PIK3CA^Tie2-CreER mice treated with either vehicle, rapamycin, miransertib or alpelisib. Scale bar: 10 μm.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2023 Jun 12;41(6):1103-1117.e12. [Abstract]; Quantification of image-based cell death of organoid lines after 72 h treatment with alpelisib, idelalisib, umbralisib in indicated concentrations (0 as in DMSO vehicle control, 10, 50, and 100 μM) and bortezomib (10 μM, positive control). Cell death is estimated as the percentage of PI-positive cells out of total number of Hoechst 33342-positive nuclei, followed by normalization to the DMSO vehicle control (negative control) and positive control (bortezomib) values.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Aug 25;CD-23-0396. [Abstract]; Correlation plot of alpelisib and STX-478 comparing pAKT IC50 at 1 hour and viability [CellTiter-Glo (CTGlo)] GI50 at 72 hours across the indicated panel of cell lines.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Aug 25;CD-23-0396. [Abstract]; Alpelisib (50 mg/kg q.d.; administered for 3 days in the PK/PD group and 28 days in the efficacy group) reduces pAKT/AKT in the skeletal muscle of mice with CAL-33 (H1047R PI3Kα-mutant) xenograft models.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2021 Oct 6;13(614):eabg0809. [Abstract]; Alpelisib (50 mg/kg/day; p.o.; approximately 3 months) inhibits the PI3K/AKT/mTOR pathway in lymphatic tissues of PIK3CA^VEGFR3-CreER mice, reducing phosphorylation levels of AKT and S6RP.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2019 Jan;440-441:54-63. [Abstract]; The siNC- or siBTF3-transfected breast cancer cells are treated with BYL-719 and are then subjected to an immunoblotting analysis.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2018 Jun;558(7711):540-546. [Abstract]; Western blot of P-AKT (Ser⁴⁷³), P-AKT (Thr³⁰⁸) and P-S6RP in liver, heart and muscles, respectively, from PIK3CA^WT and PIK3CA^CAGG-CreER mice treated with or without BYL719 directly after Cre induction (preventive) or seven days later (therapeutic).

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]; (A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

MedChemExpress (MCE) 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.

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 (t_1/2=2.9±0.2 h) for rat (1 mg/kg, iv)^[1].

MedChemExpress (MCE) 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:	T_1/2=2.9±0.2 hours.

Clinical Trial

Molecular Weight

477.93

Formula

C₁₉H₂₃ClF₃N₅O₂S

CAS No.

1584128-91-5

SMILES

CC(N=C(S1)NC(N2CCC[C@H]2C(N)=O)=O)=C1C3=CC(C(C)(C(F)(F)F)C)=NC=C3.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Alpelisib hydrochloride Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alpelisib1584128-91-5BYL-719BYL719BYL 719PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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