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Buparlisib

Product Specifications

UNSPSC Description

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.

Target Antigen

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

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 Weight

410.39

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.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 Oct 16:180:117569.|Biomedicines. 2022, 10(8), 1988.|bioRxiv. 2022 Aug 02.|bioRxiv. 2023 Aug 13.|bioRxiv. 2023 Jul 24.|bioRxiv. 2024 Dec 10:2024.12.09.627542.|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 Feb 18.|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 Jul 27;CAN-22-0042.|Cancers (Basel). 2022, 14(22), 5481|Cancers (Basel). 2024 Aug 7;16(16):2785.|Cell Commun Signal. 2019 May 15;17(1):44.|Cell Rep. 2024 Apr 23;43(5):114132.|Cell Syst. 2020 Jan 22;10(1):66-81.e11. |Clin Med Insights Oncol. 2024 Oct 16:18:11795549241285387.|Cold Spring Harb Mol Case Stud. 2020 Jun 12;6(3):a004853.|Diabetologia. 2021 Feb 11.|Endocrinology. 2023 Sep 13;bqad135.|Eur J Pharmacol. 2023 May 2;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 5.|J Cell Biol. 2020 Dec 7;219(12):e202001031.|J Cell Biol. 2023 Sep 4;222(9):e202208150.|J Clin Endocrinol Metab. 2021 Jan 1;106(1):e232-e246.|J Exp Med. 2023 Nov 6;220(11):e20211743.|Journal of the Endocrine Society. 2021 Jun 1.|Mol Carcinog. 2022 Apr 13.|Mol Carcinog. 2024 Apr 17|Molecules. 2020 Apr 23;25(8):1980.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Nat Cancer. 2024 Jul 11.|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 Jan 20.|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.|Research Square Print. 10 Jan 2023.|Research Square Print. November 7th, 2022|Sci Adv. 2022 Jan 21;8(3):eabh2635.|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.|University of Gothenburg. 2023 Jun 27.|World J Gastroenterol. 2023 Oct 28.|Cell Rep. 2020 Sep 29;32(13):108196.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-70063/Buparlisib-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-70063/Buparlisib-SDS-MedChemExpress.pdf

Clinical Information

Phase 3

CAS Number

944396-07-0

Available Sizes

Curated Selection

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