Buparlisib Hydrochloride
Based on 90 publication(s) in Google Scholar
Buparlisib Hydrochloride (BKM120 Hydrochloride) is a CNS-penetrant pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 1312445-63-8
- Formula: C18H22ClF3N6O2
- Molecular Weight:446.85
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Buparlisib Hydrochloride
More- Nature. 2024 Sep;633(8031):895-904. [Abstract]
- Nature. 2022 Dec;612(7940):555-563. [Abstract]
- Nature. 2018 Aug;560(7719):499-503. [Abstract]
- Nat Med. 2016 Jul;22(7):723-6. [Abstract]
- Science. 2025 Mar 14;387(6739):eadm9805. [Abstract]
- Cell. 2025 Oct 30;188(22):6301-6316.e29. [Abstract]
- Cell. 2025 May 29;188(11):3065-3080.e21. [Abstract]
- Cancer Discov. 2020 Aug;10(8):1226-1239. [Abstract]
- Cancer Discov. 2019 Sep;9(9):1306-1323. [Abstract]
- Cancer Discov. 2018 Mar;8(3):354-369. [Abstract]
- Cancer Commun (Lond). 2022 Mar;42(3):223-244. [Abstract]
- Nat Cancer. 2024 Aug;5(8):1250-1266. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Cancer Res. 2022 Sep 16;82(18):3223-3235. [Abstract]
- Autophagy. 2022 Jul;18(7):1551-1571. [Abstract]
- Nat Commun. 2022 Sep 29;13(1):5723. [Abstract]
- Nat Commun. 2021 Jun 8;12(1):3444. [Abstract]
- Nat Commun. 2020 May 19;11(1):2487. [Abstract]
- Sci Transl Med. 2023 Feb 22;15(684):eade1857. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Adv. 2025 Apr 25;11(17):eads6385. [Abstract]
- Sci Adv. 2022 Jan 21;8(3):eabh2635. [Abstract]
- Cancer Lett. 2019 Jan:440-441:54-63. [Abstract]
- J Exp Med. 2023 Nov 6;220(11):e20211743. [Abstract]
- Cell Commun Signal. 2019 May 15;17(1):44. [Abstract]
- Diabetologia. 2021 May;64(5):1144-1157. [Abstract]
- J Transl Med. 2024 Nov 7;22(1):1004. [Abstract]
- Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):E9570-E9579. [Abstract]
- Dev Cell. 2026 Apr 29:S1534-5807(26)00150-4. [Abstract]
- Oncogene. 2022 Feb;41(8):1140-1154. [Abstract]
- Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]
- NPJ Breast Cancer. 2025 Dec 24;12(1):4. [Abstract]
- ACS Appl Mater Interfaces. 2019 Apr 3;11(13):12342-12356. [Abstract]
- Cell Rep. 2024 Apr 23;43(5):114132. [Abstract]
- World J Gastroenterol. 2023 Oct 28;29(40):5543-5556. [Abstract]
- Cell Rep. 2020 Sep 29;32(13):108196. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Cancer Cell Int. 2020 Mar 18:20:86. [Abstract]
- Sci Signal. 2019 May 28;12(583):eaaw9450. [Abstract]
- JCI Insight. 2024 Dec 20;9(24):e178535. [Abstract]
- Oncoimmunology. 2019 Mar 16;8(5):e1581556. [Abstract]
- J Cell Biol. 2023 Sep 4;222(9):e202208150. [Abstract]
- J Cell Biol. 2020 Dec 7;219(12):e202001031. [Abstract]
- Hepatol Commun. 2019 Feb 5;3(3):423-436. [Abstract]
- Cancer Immunol Immunother. 2024 May 7;73(7):122. [Abstract]
- Eur J Pharmacol. 2023 Jul 15:951:175747. [Abstract]
- J Clin Endocrinol Metab. 2021 Jan 1;106(1):e232-e246. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Sci Rep. 2025 Nov 18;15(1):40619. [Abstract]
- Sci Rep. 2019 Jan 30;9(1):978. [Abstract]
- Cancers (Basel). 2024 Aug 7;16(16):2785. [Abstract]
- Cancers (Basel). 2022 Nov 8;14(22):5481. [Abstract]
- Cell Signal. 2026 Aug:144:112506. [Abstract]
- Oncol Rep. 2026 May;55(5):94. [Abstract]
- Cell Signal. 2025 Nov:135:112077. [Abstract]
- Cell Signal. 2025 Nov:135:112068. [Abstract]
- Biomedicines. 2022 Aug 16;10(8):1988. [Abstract]
- J Endocr Soc. 2021 Jun 1;5(8):bvab102. [Abstract]
- J Biol Chem. 2026 Jun;302(6):111461. [Abstract]
- J Cell Sci. 2025 May 15;138(10):jcs263688. [Abstract]
- Carcinogenesis. 2025 Aug 21:bgaf048. [Abstract]
- Endocrinology. 2023 Aug 28;164(10):bqad135. [Abstract]
- Analyst. 2026 Feb 16;151(4):1058-1070. [Abstract]
- Mol Carcinog. 2024 Jul;63(7):1334-1348. [Abstract]
- Mol Carcinog. 2022 Jul;61(7):664-676. [Abstract]
- BMC Anesthesiol. 2021 Aug 30;21(1):210. [Abstract]
- Brain Behav. 2018 Nov;8(11):e01123. [Abstract]
- PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]
- PLoS One. 2016 Jan 28;11(1):e0147682. [Abstract]
- Prostate. 2018 Feb;78(3):166-177. [Abstract]
- Clin Med Insights Oncol. 2024 Oct 16:18:11795549241285387. [Abstract]
- Mol Genet Genomics. 2026 Jan 31;301(1):26. [Abstract]
- In Vitro Cell Dev Biol Anim. 2021 May;57(5):510-518. [Abstract]
- Am J Transl Res. 2019 Sep 15;11(9):6055-6065. [Abstract]
- Anticancer Res. 2018 Jun;38(6):3375-3385. [Abstract]
- bioRxiv. 2025 Apr 9:2025.04.04.647273. [Abstract]
- bioRxiv. 2025 February 23.
- bioRxiv. 2024 Dec 10:2024.12.09.627542. [Abstract]
- Biomed Pharmacother. 2024 Nov:180:117569. [Abstract]
- bioRxiv. 2022 Aug 02.
- Patent. US20210236501A1.
- bioRxiv. 2023 Aug 13.
- bioRxiv. 2023 Jul 24:2023.07.23.550235. [Abstract]
- University of Gothenburg. 2023 Jun 27.
- Res Sq. 2023 Jan 10:rs.3.rs-2320717. [Abstract]
- Research Square Print. November 7th, 2022
- Medizinische Hochschule Hannover. 2020 Oct.
- Universidad de Granada. 2020 Sep.
- Cold Spring Harb Mol Case Stud. 2020 Jun 12;6(3):a004853. [Abstract]
- Patent. US20160215053A1.
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Biological Activity
|
p110α 52 nM (IC50) |
p110α-H1047R 58 nM (IC50) |
p110α-E545K 99 nM (IC50) |
p110δ 116 nM (IC50) |
p110β 166 nM (IC50) |
p110γ 262 nM (IC50) |
Vps34 2.4 μM (IC50) |
mTOR 4.6 μM (IC50) |
Buparlisib (BKM120) exhibits 50-300 nM activity for class I PI3K’s, including the most common p110α mutants. Additionally, NVP-BKM120 exhibits lower potency against class III and class IV PI3K's, where 2, 5, >5, and >25 μM biochemical activity is observed for inhibition of VPS34, mTOR, DNAPK, and PI4K, respectively[1]. Buparlisib (BKM120) induces multiple myeloma (MM) cell apoptosis in both dose- and time-dependent manners. Buparlisib (BKM120) at concentrations ≥10 μM induces significant apoptosis in all tested MM cell lines at 24 h (P<0.05, compares with control). Therefore, 10 μM Buparlisib (BKM120) and 24-h treatment are chose in in the following experiments if not stated otherwise. Buparlisib (BKM120) treatment results in a dose-dependent growth inhibition in all tested MM cell lines. Buparlisib (BKM120) IC50 varies among tested MM cells. At 24 h treatment, IC50 for ARP-1, ARK, and MM.1R is between 1 and 10 μM, while IC50 for MM.1S is <1 μM, and IC50 for U266 is between 10 and 100 μM. In summary, Buparlisib (BKM120) treatment results in MM cell growth inhibition and apoptosis in dose- and time-dependent manners[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1312445-63-8
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Appearance Solid
-
Molecular Weight 446.85
-
Formula C18H22ClF3N6O2
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Color White to yellow
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SMILES
NC(N=C1)=CC(C(F)(F)F)=C1C2=NC(N3CCOCC3)=NC(N4CCOCC4)=C2.[H]Cl
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Synonyms
BKM120 Hydrochloride; NVP-BKM120 Hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (90)
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Journal Impact Factor
-
Most Recent
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Nature
2024 Sep;633(8031):895-904. PMID: 39169180 -
Nature
2022 Dec;612(7940):555-563. PMID: 36450983 -
Nature
2018 Aug;560(7719):499-503. PMID: 30051890 -
Nat Med
Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. [Abstract]2016 Jul;22(7):723-6. PMID: 27270588
Buparlisib Hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Med. 2016 Jul;22(7):723-6. [Abstract]
Selective response of HER2-positive PDX DF-BM355 to the combination of BKM120/RAD001. Western blot analysis of lysates from vehicle-treated or BKM120-treated DF-BM355 in vivo.
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Science
2025 Mar 14;387(6739):eadm9805. PMID: 40080571 -
Cell
2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455 -
Cell
Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]2025 May 29;188(11):3065-3080.e21. PMID: 40393457 -
Cancer Discov
The INPP4B Tumor Suppressor Modulates EGFR Trafficking and Promotes Triple-Negative Breast Cancer. [Abstract]2020 Aug;10(8):1226-1239. PMID: 32513774 -
Cancer Discov
2019 Sep;9(9):1306-1323. PMID: 31217297 -
Cancer Discov
Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple-Negative Breast Cancer. [Abstract]2018 Mar;8(3):354-369. PMID: 29203461 -
Cancer Commun (Lond)
Aberrant translation regulated by METTL1/WDR4-mediated tRNA N7-methylguanosine modification drives head and neck squamous cell carcinoma progression. [Abstract]2022 Mar;42(3):223-244. PMID: 35179319 -
Nat Cancer
A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. [Abstract]2024 Aug;5(8):1250-1266. PMID: 38992135 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Cancer Res
GOT2 Silencing Promotes Reprogramming of Glutamine Metabolism and Sensitizes Hepatocellular Carcinoma to Glutaminase Inhibitors. [Abstract]2022 Sep 16;82(18):3223-3235. PMID: 35895805 -
Autophagy
Lysosomal targetomics of ghr KO mice shows chaperone-mediated autophagy degrades nucleocytosolic acetyl-coA enzymes. [Abstract]2022 Jul;18(7):1551-1571. PMID: 34704522 -
Nat Commun
Proteomic characterization of gastric cancer response to chemotherapy and targeted therapy reveals new therapeutic strategies. [Abstract]2022 Sep 29;13(1):5723. PMID: 36175412 -
Nat Commun
2021 Jun 8;12(1):3444. PMID: 34103528 -
Nat Commun
SH3RF3 promotes breast cancer stem-like properties via JNK activation and PTX3 upregulation. [Abstract]2020 May 19;11(1):2487. PMID: 32427938 -
Sci Transl Med
Obesity promotes breast epithelium DNA damage in women carrying a germline mutation in BRCA1 or BRCA2. [Abstract]2023 Feb 22;15(684):eade1857. PMID: 36812344 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Sci Adv
2025 Apr 25;11(17):eads6385. PMID: 40279411 -
Sci Adv
Fasting improves therapeutic response in hepatocellular carcinoma through p53-dependent metabolic synergism. [Abstract]2022 Jan 21;8(3):eabh2635. PMID: 35061544 -
Cancer Lett
Inhibition of BTF3 sensitizes luminal breast cancer cells to PI3Kα inhibition through the transcriptional regulation of ERα. [Abstract]2019 Jan:440-441:54-63. PMID: 30315845
Buparlisib Hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2019 Jan:440-441:54-63. [Abstract]
The cells are transfected with either the negative control (siNC) or BTF3 siRNA for 12 hours followed by BKM-120 or AZD-6482 treatment for 48 hours. The protein abundance is determined by an immunoblotting analysis.
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J Exp Med
2023 Nov 6;220(11):e20211743. PMID: 37642941 -
Cell Commun Signal
MIIP inhibits the growth of prostate cancer via interaction with PP1α and negative modulation of AKT signaling. [Abstract]2019 May 15;17(1):44. PMID: 31092266 -
Diabetologia
Saturated fatty acids entrap PDX1 in stress granules and impede islet beta cell function. [Abstract]2021 May;64(5):1144-1157. PMID: 33569632 -
J Transl Med
SLC38A5 suppresses ferroptosis through glutamine-mediated activation of the PI3K/AKT/mTOR signaling in osteosarcoma. [Abstract]2024 Nov 7;22(1):1004. PMID: 39511570 -
Proc Natl Acad Sci U S A
Role for ERK1/2-dependent activation of FCHSD2 in cancer cell-selective regulation of clathrin-mediated endocytosis. [Abstract]2018 Oct 9;115(41):E9570-E9579. PMID: 30249660 -
Dev Cell
2026 Apr 29:S1534-5807(26)00150-4. PMID: 42061405 -
Oncogene
Targeting glutamine metabolism network for the treatment of therapy-resistant prostate cancer. [Abstract]2022 Feb;41(8):1140-1154. PMID: 35046532 -
Oncogene
PI3K-p110α mediates resistance to HER2-targeted therapy in HER2+, PTEN-deficient breast cancers. [Abstract]2016 Jul 7;35(27):3607-12. PMID: 26500061
Buparlisib 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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NPJ Breast Cancer
SIMD: Synergistic integration mutualistic platform based on single-cell and proteotranscriptomics for drug repositioning. [Abstract]2025 Dec 24;12(1):4. PMID: 41444222 -
ACS Appl Mater Interfaces
Micellar Formulation of Talazoparib and Buparlisib for Enhanced DNA Damage in Breast Cancer Chemoradiotherapy. [Abstract]2019 Apr 3;11(13):12342-12356. PMID: 30860347 -
Cell Rep
Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect. [Abstract]2024 Apr 23;43(5):114132. PMID: 38656871 -
World J Gastroenterol
Roles of phosphatidylinositol-3-kinases signaling pathway in inflammation-related cancer: Impact of rs10889677 variant and buparlisib in colitis-associated cancer. [Abstract]2023 Oct 28;29(40):5543-5556. PMID: 37970476 -
Cell Rep
2020 Sep 29;32(13):108196. PMID: 32997991 -
Cell Syst
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]2020 Jan 22;10(1):66-81.e11. PMID: 31812693 -
Cancer Cell Int
Breast cancer organoids from a patient with giant papillary carcinoma as a high-fidelity model. [Abstract]2020 Mar 18:20:86. PMID: 32206037 -
Sci Signal
2019 May 28;12(583):eaaw9450. PMID: 31138768 -
JCI Insight
YAP/TAZ mediates resistance to KRAS inhibitors through inhibiting proapoptosis and activating the SLC7A5/mTOR axis. [Abstract]2024 Dec 20;9(24):e178535. PMID: 39704172 -
Oncoimmunology
Inhibition of PI3K pathway increases immune infiltrate in muscle-invasive bladder cancer. [Abstract]2019 Mar 16;8(5):e1581556. PMID: 31069145 -
J Cell Biol
2023 Sep 4;222(9):e202208150. PMID: 37418003 -
J Cell Biol
2020 Dec 7;219(12):e202001031. PMID: 33048163 -
Hepatol Commun
Murine Liver Organoids as a Genetically Flexible System to Study Liver Cancer In Vivo and In Vitro. [Abstract]2019 Feb 5;3(3):423-436. PMID: 30859153 -
Cancer Immunol Immunother
Dual roles of HK3 in regulating the network between tumor cells and tumor-associated macrophages in neuroblastoma. [Abstract]2024 May 7;73(7):122. PMID: 38714539 -
Eur J Pharmacol
BKM120 inhibits malignant rhabdoid tumor of the kidney through induction of apoptosis and G0/G1 phase arrest. [Abstract]2023 Jul 15:951:175747. PMID: 37142086 -
J Clin Endocrinol Metab
2021 Jan 1;106(1):e232-e246. PMID: 33000123 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
Sci Rep
Establishment of novel cholangiocarcinoma cell lines with ARID1A deficiency and preclinical validation of synthetic lethality therapies. [Abstract]2025 Nov 18;15(1):40619. PMID: 41254205 -
Sci Rep
Solid stress-induced migration is mediated by GDF15 through Akt pathway activation in pancreatic cancer cells. [Abstract]2019 Jan 30;9(1):978. PMID: 30700740 -
Cancers (Basel)
Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]2024 Aug 7;16(16):2785. PMID: 39199558 -
Cancers (Basel)
Combined Targeting of Pathogenetic Mechanisms in Pancreatic Neuroendocrine Tumors Elicits Synergistic Antitumor Effects. [Abstract]2022 Nov 8;14(22):5481. PMID: 36428573 -
Cell Signal
RNF130 inhibits the proliferation, migration and invasion of osteosarcoma through DAB1 mediated suppression of the PI3K/AKT signaling pathway. [Abstract]2026 Aug:144:112506. PMID: 41933674 -
Oncol Rep
Depleting HIF‑1α attenuates the progression of osteosarcoma, but tumorigenicity is sustained through HIF‑independent pathways. [Abstract]2026 May;55(5):94. PMID: 41823542 -
Cell Signal
ABLIM1 promotes the proliferation, migration and invasion of osteosarcoma through DCC mediated activation of PI3K/AKT signaling pathway. [Abstract]2025 Nov:135:112077. PMID: 40846275 -
Cell Signal
IRF2BPL inhibits proliferation, migration and invasion of osteosarcoma cells by inhibiting FOSL2-mediated PI3K/AKT pathway activation. [Abstract]2025 Nov:135:112068. PMID: 40834975 -
Biomedicines
A Drug Screening Reveals Minocycline Hydrochloride as a Therapeutic Option to Prevent Breast Cancer Cells Extravasation across the Blood-Brain Barrier. [Abstract]2022 Aug 16;10(8):1988. PMID: 36009536 -
J Endocr Soc
Thyroid Hormone Receptor Beta Inhibits PI3K-Akt-mTOR Signaling Axis in Anaplastic Thyroid Cancer via Genomic Mechanisms. [Abstract]2021 Jun 1;5(8):bvab102. PMID: 34258492 -
J Biol Chem
2026 Jun;302(6):111461. PMID: 41999888 -
J Cell Sci
Tumor acidosis supports cancer cell lipid uptake via a rapid transporter-independent mechanism. [Abstract]2025 May 15;138(10):jcs263688. PMID: 40190115 -
Carcinogenesis
HECTD3 E3 ligase mediates ubiquitination of AKT-phosphorylated CMTM3 in HER2-overexpressed breast cancer cells. [Abstract]2025 Aug 21:bgaf048. PMID: 40836897 -
Endocrinology
TRβ Agonism Induces Tumor Suppression and Enhances Drug Efficacy in Anaplastic Thyroid Cancer in Female Mice. [Abstract]2023 Aug 28;164(10):bqad135. PMID: 37702560 -
Analyst
Quantification of buparlisib in human liver microsomes employing an ultra-fast, sensitive UPLC-MS/MS method: in vitro and in silico metabolic stability evaluation. [Abstract]2026 Feb 16;151(4):1058-1070. PMID: 41589698 -
Mol Carcinog
Four and a half LIM domains 2 (FHL2) attenuates tumorigenesis of gastrointestinal stromal tumors (GISTs) by negatively regulating KIT signaling. [Abstract]2024 Jul;63(7):1334-1348. PMID: 38629424 -
Mol Carcinog
Epidermal growth factor receptor signaling in precancerous keratinocytes promotes neighboring head and neck cancer squamous cell carcinoma cancer stem cell-like properties and phosphoinositide 3-kinase inhibitor insensitivity. [Abstract]2022 Jul;61(7):664-676. PMID: 35417043 -
BMC Anesthesiol
The expression of kappa-opioid receptor promotes the migration of breast cancer cells in vitro. [Abstract]2021 Aug 30;21(1):210. PMID: 34461834 -
Brain Behav
Protective effect of docosahexaenoic acid on lipotoxicity-mediated cell death in Schwann cells: Implication of PI3K/AKT and mTORC2 pathways. [Abstract]2018 Nov;8(11):e01123. PMID: 30264903
Buparlisib Hydrochloride purchased from MedChemExpress. Usage Cited in: Brain Behav. 2018 Nov;8(11):e01123. [Abstract]
The effect of BKM120 on AKT phosphorylation is examined by Western blot.
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PLoS One
PIK3CA missense mutations promote glioblastoma pathogenesis, but do not enhance targeted PI3K inhibition. [Abstract]2018 Jul 5;13(7):e0200014. PMID: 29975751
Buparlisib Hydrochloride purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]
Representative immunoblots of control and NHARAS treated with Buparlisib for 24 h.
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PLoS One
2016 Jan 28;11(1):e0147682. PMID: 26821351 -
Prostate
2018 Feb;78(3):166-177. PMID: 29181846
Buparlisib Hydrochloride purchased from MedChemExpress. Usage Cited in: Prostate. 2018 Feb;78(3):166-177. [Abstract]
Western blot analysis of p-AKT (Ser473) in stable cell lines (Vector-DU145 and GOLM1-DU145) treated with 200 nM, 500 nM or 1 μM BKM120.
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Clin Med Insights Oncol
Exploring the Clinical Implications of RPL3 Presence in BRCA-Associated Cancers: Unraveling the Interplay With Cancer Immunity. [Abstract]2024 Oct 16:18:11795549241285387. PMID: 39429685 -
Mol Genet Genomics
Buparlisib induces eukaryotic elongation factor-2 expression to cause treatment failure for lung cancer cells. [Abstract]2026 Jan 31;301(1):26. PMID: 41619002 -
In Vitro Cell Dev Biol Anim
Breast cancer organoids from malignant pleural effusion-derived tumor cells as an individualized medicine platform. [Abstract]2021 May;57(5):510-518. PMID: 33950403 -
Am J Transl Res
2019 Sep 15;11(9):6055-6065. PMID: 31632573 -
Anticancer Res
Broad-spectrum Preclinical Antitumor Activity of Eribulin (Halaven®): Combination with Anticancer Agents of Differing Mechanisms. [Abstract]2018 Jun;38(6):3375-3385. PMID: 29848686 -
bioRxiv
Genome-wide profiling identifies the genetic dependencies of cell death following EGFR inhibition. [Abstract]2025 Apr 9:2025.04.04.647273. PMID: 40291701 -
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bioRxiv
2024 Dec 10:2024.12.09.627542. PMID: 39713309 -
Biomed Pharmacother
Buparlisib and ponatinib inhibit aggressiveness of cholangiocarcinoma cells via suppression of IRS1-related pathway by targeting oxidative stress resistance. [Abstract]2024 Nov:180:117569. PMID: 39418964 -
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bioRxiv
Endocytic vesicles act as vehicles for glucose uptake in response to growth factor stimulation. [Abstract]2023 Jul 24:2023.07.23.550235. PMID: 37546742 -
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Res Sq
Post-fast refeeding enhances intestinal stem cell-mediated regeneration and tumourigenesis through mTORC1-dependent polyamine synthesis. [Abstract]2023 Jan 10:rs.3.rs-2320717. PMID: 36711807 -
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Cold Spring Harb Mol Case Stud
2020 Jun 12;6(3):a004853. PMID: 32532875 -
Solvent & Solubility
DMSO : ≥ 50 mg/mL (111.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
A2780 cells are cultured in DMEM supplemented with 10% FBS. L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 1000 cells per well, 100 uL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. Buparlisib (BKM120) supplied in DMSO (20 mM) are diluted further into DMSO (7.5 uL of 20 mM NVP-BKM120 in 22.5 uL DMSO. Mix well, transfer 10 uL to 20 uL DMSO, repeat until 9 concentrations have been made). The diluted Buparlisib (BKM120) solution (2 uL), is then added to cell medium (500 uL) cell medium. Equal volumes of this solution (100 uL) are added to the cells in 96 well plates and incubated at 37ºC for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Six- to eight-week-old female severe combined immunodeficiency (SCID) mice are used. SCID mice are subcutaneously inoculated in the right flank with 1 million ARP-1 or MM.1S cells suspended in 50 μL phosphate-buffered saline (PBS). After palpable tumor developed (tumor diameter ≥5 mm), mice are treated with intraperitoneal injection of DMSO/PBS or Buparlisib (BKM120) (5 μM per kg per day) for 15 days. Tumor sizes are measured every 5 days, and blood samples are collected at the same period. Tumor burdens are evaluated by measuring tumor size and detecting circulating human kappa chain or lambda chain.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (584 KB)
- English - EN (584 KB)
- Français - FR (584 KB)
- Deutsch - DE (584 KB)
- Norwegian - NO (584 KB)
- Español - ES (584 KB)
- Swedish - SV (584 KB)
- Italian - IT (584 KB)
- Korean - KR (584 KB)
- Portuguese - PT (584 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Zheng Y, et al. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone. J Mol Med (Berl). 2012 Jun;90(6):695-706. [Content Brief]
[3]. de Gooijer MC, et al. Buparlisib is a brain penetrable pan-PI3K inhibitor. Sci Rep. 2018 Jul 17;8(1):10784. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2379 mL | 11.1894 mL | 22.3789 mL | 55.9472 mL |
| 5 mM | 0.4476 mL | 2.2379 mL | 4.4758 mL | 11.1894 mL | |
| 10 mM | 0.2238 mL | 1.1189 mL | 2.2379 mL | 5.5947 mL | |
| 15 mM | 0.1492 mL | 0.7460 mL | 1.4919 mL | 3.7298 mL | |
| 20 mM | 0.1119 mL | 0.5595 mL | 1.1189 mL | 2.7974 mL | |
| 25 mM | 0.0895 mL | 0.4476 mL | 0.8952 mL | 2.2379 mL | |
| 30 mM | 0.0746 mL | 0.3730 mL | 0.7460 mL | 1.8649 mL | |
| 40 mM | 0.0559 mL | 0.2797 mL | 0.5595 mL | 1.3987 mL | |
| 50 mM | 0.0448 mL | 0.2238 mL | 0.4476 mL | 1.1189 mL | |
| 60 mM | 0.0373 mL | 0.1865 mL | 0.3730 mL | 0.9325 mL | |
| 80 mM | 0.0280 mL | 0.1399 mL | 0.2797 mL | 0.6993 mL | |
| 100 mM | 0.0224 mL | 0.1119 mL | 0.2238 mL | 0.5595 mL |