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Buparlisib
$72 – $540
Products Details
Product 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.
Web ID
– HY-70063
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C18H21F3N6O2
Citations
– 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.|Biomedicines. 2022, 10(8), 1988.|bioRxiv. 2023 Aug 13.|bioRxiv. 2023 Jul 24.|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 Lett. 2019 Jan;440-441:54-63.|Cancer Res. 2022 Jul 27;CAN-22-0042.|Cancers (Basel). 2022, 14(22), 5481|Cell Commun Signal. 2019 May 15;17(1):44.|Cell Syst. 2020 Jan 22;10(1):66-81.e11. |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.|Molecules. 2020 Apr 23;25(8):1980.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|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.|Oncogene. 2016 Jul 7;35(27):3607-12. |Oncogene. 2022 Jan 20.|Oncoimmunology. 2019 Mar 16;8(5):e1581556.|Patent. US20160215053A1.|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.|World J Gastroenterol. 2023 Oct 28.|Cell Rep. 2020 Sep 29;32(13):108196.
References
– [1]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.|[2]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.|[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.
CAS Number
– 944396-07-0
Molecular Weight
– 410.39
Compound Purity
– 99.90
SMILES
– FC(F)(C1=C(C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=NC(N)=C1)F
Clinical Information
– Phase 3
Research Area
– Cancer
Solubility
– DMSO : 100 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Apoptosis;PI3K
Isoform
– PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ;Vps34
Pathway
– Apoptosis;PI3K/Akt/mTOR
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
