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Alpelisib (hydrochloride)

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].

Product Specifications

CAS Number

[1584128-91-5]

Product Name Alternative

BYL-719 (hydrochloride)

UNSPSC

12352005

Target

PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/alpelisib-hydrochloride.html

Purity

99.55

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C19H23ClF3N5O2S

Molecular Weight

477.93

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Citation 01

Cancers (Basel) . 2022 Jan 2;14 (1) :214.|Am J Cancer Res. 2021 Mar 1;11 (3) :773-792.|Am J Transl Res. 2025 Jun 15;17 (6) :4689-4700. |Anal Bioanal Chem. 2025 Nov 17.|Antioxidants. 2025 Jul 7;14 (7) :833.|Biochem Biophys Res Commun. 2020 Sep 24;530 (3) :520-526.|Biomaterials. 2022 Oct:289:121800.|Biomed Pharmacother. 2020 Sep;129:110397.|Biomed Rep. 2023 Oct 13;19 (6) :94.|Biomolecules. 2021 Jan 25;11 (2) :150.|bioRxiv. 2020 Jan.|bioRxiv. 2023 Aug 22.|bioRxiv. 2023 May 30:2023.05.28.542643.|bioRxiv. 2024 August 18.|bioRxiv. 2024 July 07.|bioRxiv. 2024 November 03.|bioRxiv. 2025 Sep 20:2025.09.17.676669.|Biosci Rep. 2020 Oct 30;40 (10) :BSR20201128.|Blood. 2019 Jan 3;133 (1) :70-80.|Blood. 2024 Jul 5:blood.2023021705.|Br J Cancer. 2023 Jan;128 (1) :148-159.|Br J Haematol. 2020 May;189 (4) :731-744.|Breast Cancer Res. 2021 May 21;23 (1) :57.|Cancer Biomark. 2025 Oct;42 (10) :18758592251390145.|Cancer Cell. 2023 Jun 12;41 (6) :1103-1117.e12.|Cancer Cell. 2024 Jul 8;42 (7) :1286-1300.e8.|Cancer Discov. 2020 Aug;10 (8) :1226-1239.|Cancer Discov. 2023 Nov 1;13 (11) :2432-2447.|Cancer Lett. 2019 Jan:440-441:54-63.|Cancer Lett. 2024 Aug 10:597:217074.|Cancer Lett. 2024 Sep 5:217219.|Cancer Metab. 2025 Feb 7;13 (1) :6.|Cancer Nanotechnol. 2023 Mar 29.|Cancer Res. 2021 May 1;81 (9) :2470-2480.|Cancers (Basel) . 2022 Jul 22;14 (15) :3559.|Cell Biochem Biophys. 2025 Mar 22.|Cell Biosci. 2022 Dec 30;12 (1) :210.|Cell Death Differ. 2025 Apr 9.|Cell Death Dis. 2020 Oct 6;11 (10) :831.|Cell Death Dis. 2022 Jan 12;13 (1) :54.|Cell Death Dis. 2023 Dec 14;14 (12) :831.|Cell Death Dis. 2025 May 29;16 (1) :423.|Cell Metab. 2021 Nov 2;33 (11) :2247-2259.e6.|Cell Rep. 2020 Sep 29;32 (13) :108196.|Cell Rep. 2023 Dec 26;42 (12) :113535.|Cell Rep. 2024 Apr 23;43 (4) :114088.|Cell Rep. 2024 May 2;43 (5) :114174.|Cell Signal. 2025 Apr 9:111799.|Cell Syst. 2018 Apr 25;6 (4) :424-443.e7.|Cell Syst. 2019 Jul 24;9 (1) :35-48.e5. |Cell Syst. 2020 Jan 22;10 (1) :66-81.e11.|Cell. 2025 May 29;188 (11) :3065-3080.e21. |Cells. 2022 Aug 4;11 (15) :2402.|Diabetes. 2024 Sep 12:db240402.|EMBO Mol Med. 2025 Jul;17 (7) :1556-1574.|EMBO Mol Med. 2025 Jun;17 (6) :1325-1354. |Endocrinology. 2023 Aug 28;164 (10) :bqad135.|Front Oncol. 2021 Jul 13:11:704042.|Front Oncol. 2021 Nov 24:11:766298.|Gynecol Oncol. 2020 Dec;159 (3) :827-838.|Harvard Medical School LINCS LIBRARY|Int J Cancer. 2024 Jul 15;155 (2) :324-338.|Int J Mol Sci. 2019 Jul 10;20 (14) :3383.|Int J Mol Sci. 2023 Aug 30;24 (17) :13418.|Int J Oncol. 2022 Apr;60 (4) :37.|J Anal Sci Technol. 13, 31 (2022) .|J Clin Invest. 2021 Dec 15;131 (24) :e140436.|J Exp Med. 2023 Nov 6;220 (11) :e20211743.|J Exp Med. 2023 Nov 6;220 (11) :e20230926.|J Hematol Oncol. 2020 Feb 22;13 (1) :13.|J Med Chem. 2024 Sep 12;67 (17) :15387-15410.|J Proteome Res. 2021 May 7;20 (5) :2964-2972.|J Transl Med. 2022 Jun 7;20 (1) :263.|JCI Insight. 2022 Aug 22;7 (16) :e155899.|Mol Cancer Res. 2020 Jun;18 (6) :822-834.|Mol Psychiatry. 2021 Nov;26 (11) :6451-6468.|Molecules. 2020 Apr 23;25 (8) :1980.|Nat Aging. 2023 Feb;3 (2) :162-172.|Nat Biomed Eng. 2018 Aug;2 (8) :578-588.|Nat Commun. 2020 Aug 13;11 (1) :4053.|Nat Commun. 2022 Jan 11;13 (1) :245.|Nat Commun. 2023 Jul 13;14 (1) :4084.|Nature Cancer. 2021 Jan;2 (1) :34-48.|Nature. 2018 Jun;558 (7711) :540-546. |Neoplasia. 2023 Sep:43:100913.|NPJ Precis Oncol. 2025 Nov 7;9 (1) :343.|Oncogene. 2016 Jul 7;35 (27) :3607-12. |Oncogene. 2025 Sep;44 (34) :3142-3148.|Oncol Rep. 2019 Nov;42 (5) :2097-2107.|Patent. US20220249511A1.|Patent. US20220313694A1.|PLoS One. 2024 Aug 2;19 (8) :e0308051.|PLoS One. 2025 Jul 10;20 (7) :e0326491.|Preprints. 2024 Feb 16.|Proc Natl Acad Sci U S A. 2022 Nov 16;119 (46) :e2215621119.|Proc Natl Acad Sci U S A. 2025 Jul;122 (26) :e2424867122.|Research Square Preprint. 2020 Aug.|Research Square Preprint. 2022 Jan.|Research Square Preprint. 2023 May 10.|Research Square Preprint. 2023 May 9.|RSC Adv. 2024 Oct 18;14 (45) :32876-32882.|Sci Adv. 2022 Dec 9;8 (49) :eade7823.|Sci Rep. 2021 Jan 11;11 (1) :291.|Sci Rep. 2025 Jan 18;15 (1) :2415.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Sci Transl Med. 2021 Oct 6;13 (614) :eabg0809.|Science. 2017 Dec 1;358 (6367) :eaan4368.|Science. 2021 Oct;374 (6563) :eabf3067.|Signal Transduct Target Ther. 2024 Jun 17;9 (1) :146.|Signal Transduct Target Ther. 2025 Nov 18;10 (1) :373.|STAR Protoc. 2023 Nov 16;4 (4) :102683.|Ther Adv Med Oncol. 2020 Dec 14:12:1758835920975621.|University of Cologne. 2024.|Virulence. 2025 Dec;16 (1) :2580104.

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