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Buparlisib

Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

Product Specifications

CAS Number

944396-07-0

Product Name Alternative

BKM120; NVP-BKM120

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; PI3K

Type

Reference compound

Related Pathways

Apoptosis; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/NVP-BKM120.html

Concentration

10mM

Purity

99.90

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

FC(F)(C1=C(C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=NC(N)=C1)F

Molecular Formula

C18H21F3N6O2

Molecular Weight

410.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Burger MT, et al. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. ACS Med Chem Lett. 2011 Aug 26;2 (10) :774-9.|[2]Zheng Y, et al. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity. J Mol Med (Berl) . 2012 Jun;90 (6) :695-706.|[3]Ni J, et al. Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. Nat Med. 2016 Jul;22 (7) :723-6.|[4]Liu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8 (3) :354-369.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ; Vps34

Citation 01

ACS Appl Mater Interfaces. 2019 Apr 3;11 (13) :12342-12356. |Am J Transl Res. 2019 Sep 15;11 (9) :6055-6065.|Anticancer Res. 2018 Jun;38 (6) :3375-3385.|Autophagy. 2022 Jul;18 (7) :1551-1571.|Biomed Pharmacother. 2024 Nov:180:117569.|Biomedicines. 2022 Aug 16;10 (8) :1988.|bioRxiv. 2022 Aug 02.|bioRxiv. 2023 Aug 13.|bioRxiv. 2023 Jul 24:2023.07.23.550235.|bioRxiv. 2024 Dec 10:2024.12.09.627542.|bioRxiv. 2025 Apr 9.|bioRxiv. 2025 February 23.|BMC Anesthesiol. 2021 Aug 30;21 (1) :210.|Brain Behav. 2018 Nov;8 (11) :e01123.|Cancer Cell Int. 2020 Mar 18;20:86.|Cancer Commun (Lond) . 2022 Mar;42 (3) :223-244.|Cancer Discov. 2018 Mar;8 (3) :354-369.|Cancer Discov. 2019 Sep;9 (9) :1306-1323. |Cancer Discov. 2020 Aug;10 (8) :1226-1239.|Cancer Immunol Immunother. 2024 May 7;73 (7) :122.|Cancer Lett. 2019 Jan:440-441:54-63.|Cancer Res. 2022 Sep 16;82 (18) :3223-3235.|Cancers (Basel) . 2022 Nov 8;14 (22) :5481.|Cancers (Basel) . 2024 Aug 7;16 (16) :2785.|Carcinogenesis. 2025 Aug 21:bgaf048.|Cell Commun Signal. 2019 May 15;17 (1) :44.|Cell Rep. 2024 Apr 23;43 (5) :114132.|Cell Signal. 2025 Nov:135:112068.|Cell Signal. 2025 Nov:135:112077.|Cell Syst. 2020 Jan 22;10 (1) :66-81.e11.|Cell. 2025 May 29;188 (11) :3065-3080.e21. |Cell. 2025 Oct 30;188 (22) :6301-6316.e29.|Clin Med Insights Oncol. 2024 Oct 16:18:11795549241285387.|Cold Spring Harb Mol Case Stud. 2020 Jun 12;6 (3) :a004853.|Diabetologia. 2021 May;64 (5) :1144-1157.|Endocrinology. 2023 Aug 28;164 (10) :bqad135.|Eur J Pharmacol. 2023 Jul 15:951:175747.|Gastroenterologie, Hepatologie und Endokrinologie. 2020 Oct.|Harvard Medical School LINCS LIBRARY|Hepatol Commun. 2019 Feb 5;3 (3) :423-436.|In Vitro Cell Dev Biol Anim. 2021 May;57 (5) :510-518.|J Cell Biol. 2020 Dec 7;219 (12) :e202001031.|J Cell Biol. 2023 Sep 4;222 (9) :e202208150.|J Cell Sci. 2025 Apr 7:jcs.263688.|J Clin Endocrinol Metab. 2021 Jan 1;106 (1) :e232-e246.|J Endocr Soc. 2021 Jun 1;5 (8) :bvab102.|J Exp Med. 2023 Nov 6;220 (11) :e20211743.|J Transl Med. 2024 Nov 7;22 (1) :1004.|JCI Insight. 2024 Dec 20;9 (24) :e178535.|Mol Carcinog. 2022 Jul;61 (7) :664-676.|Mol Carcinog. 2024 Apr 17|Molecules. 2020 Apr 23;25 (8) :1980.|Nat Biomed Eng. 2018 Aug;2 (8) :578-588.|Nat Cancer. 2024 Aug;5 (8) :1250-1266.|Nat Commun. 2020 May 19;11 (1) :2487.|Nat Commun. 2021 Jun 8;12 (1) :3444.|Nat Commun. 2022 Sep 29;13 (1) :5723.|Nat Med. 2016 Jul;22 (7) :723-6.|Nature. 2018 Aug;560 (7719) :499-503.|Nature. 2022 Dec;612 (7940) :555-563.|Nature. 2024 Sep;633 (8031) :895-904.|Oncogene. 2016 Jul 7;35 (27) :3607-12. |Oncogene. 2022 Feb;41 (8) :1140-1154.|Oncoimmunology. 2019 Mar 16;8 (5) :e1581556.|Patent. US20160215053A1.|Patent. US20210236501A1.|PLoS One. 2016 Jan 28;11 (1) :e0147682. |PLoS One. 2018 Jul 5;13 (7) :e0200014.|Proc Natl Acad Sci U S A. 2018 Oct 9;115 (41) :E9570-E9579. |Programa de Doctorado en Biomedicina. 2020 Sep.|Prostate. 2018 Feb;78 (3) :166-177.|Res Sq. 2023 Jan 10:rs.3.rs-2320717.|Research Square Print. November 7th, 2022|Sci Adv. 2022 Jan 21;8 (3) :eabh2635.|Sci Adv. 2025 Apr 25;11 (17) :eads6385.|Sci Rep. 2025 Nov 18;15 (1) :40619.|Sci Rep. 2019 Jan 30;9 (1) :978.|Sci Signal. 2019 May 28;12 (583) . pii: eaaw9450. |Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Sci Transl Med. 2023 Feb 22;15 (684) :eade1857.|Science. 2025 Mar 14;387 (6739) :eadm9805.|University of Gothenburg. 2023 Jun 27.|World J Gastroenterol. 2023 Oct 28;29 (40) :5543-5556.|Cell Rep. 2020 Sep 29;32 (13) :108196.

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