Buparlisib (BKM120)

Name: Buparlisib (BKM120)
Brand: Selleck Chemicals
SKU: S2247
Rating: 5 (157 reviews)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

157 publications

CAS No. 944396-07-0

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.

Selleck's Buparlisib (BKM120) has been cited by 157 publications

Cell, 2020, 25;181(7):1596-1611.e27.

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Cancer Cell, 2020, 37(2):183-199

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Nat Immunol, 2020, 21(4):442-454

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Science, 2019, 364(6441)

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Cancer Cell, 2018, 34(6):922-938

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Cancer Cell, 2018, 33(1):91-107

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Cell, 2017, 161(4):803-16

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Cancer Discov, 2017, 7(9):1018-1029

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Nature, 2016, 529(7586):413-417

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Nat Med, 2015, 10.1038/nm.3855

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Nat Med, 2015, 21(9):1038-47

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Cancer Discov, 2014, 4(1):69-79

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Cancer Discov, 2013, 4(2):232-45

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Cancer Discov, 2013, 4(2):186-99

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Cell, 2012, 27;149(3):656-70.

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Nat Med, 2012, 18(6):892-901

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Cancer Cell, 2012, 21(2):155-67

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Genome Med, 2020, 18;12(1):17

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Cell Rep, 2020, 31(12):107800

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Sci Signal, 2020, 3;13(621) pii: eaax2364

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Mol Cancer Res, 2020, 11

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Front Neurosci, 2020, 2;14:223

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Eur J Pharmacol, 2020, 870:172821

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Cell Biol Int, 2020, 10.1002/cbin.11322

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BMC Cancer, 2020, 20(1):724

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FASEB Bioadv, 2020, 2(2):126-144

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NPJ Breast Cancer, 2020, 6:30

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Mol Oncol, 2020, 10.1002/1878-0261.12673

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Cancer, 2020, 10.1002/cncr.33071

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Small GTPases, 2020, 10.1080/21541248

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Nat Cell Biol, 2019, 21(2):226-237

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Nat Commun, 2019, 10(1):259

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Nat Commun, 2019, 10(1):2910

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Nat Commun, 2019, 10(1):1515

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J Thorac Oncol, 2019, 14(6):1061-1076

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Leukemia, 2019, 10.1038/s41375-019-0556-z

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Cell Syst, 2019, 8(2):97-108

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Theranostics, 2019, 9(8):2380-2394

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Cell Rep, 2019, 27(1):294-306

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Cell Rep, 2019, 27(2):631-647

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Cell Rep, 2019, 28(9):2317-2330

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Cell Death Differ, 2019, 10.1038/s41418-019-0422-6

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Cancer Lett, 2019, 466:23-34

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Cancers (Basel), 2019, 11(2)

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Mol Ther Oncolytics, 2019, 13:58-66

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Cancer Discov, 2019, 9(9):1306-1323

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Mol Cancer Ther, 2019, 18(4):834-844

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Aging (Albany NY), 2019, 11(18):7780-7795

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J Cell Physiol, 2019, 234(7):10907-10917

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Front Oncol, 2019, 0.87569444444

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Eur J Immunol, 2019, doi: 101002/eji201948241

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Mol Pharmacol, 2019, 95(5):528-536

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Prostate, 2019, 79(11):1347-1359

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Chem Biol Interact, 2019, 302:101-107

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Eur J Pharmacol, 2019, 842:89-98

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Biochem Biophys Res Commun, 2019, 513(3):546-552

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Leuk Lymphoma, 2019, 10.1080/10428194.2019.1594211

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Int J Hematol, 2019, 110(2):213-227

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Oncol Lett, 2019, 17(3-:3151-3162

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NPJ Breast Cancer, 2019, 05:31

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Nat Biomed Eng, 2018, 2(8):578-588

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Nat Biomed Eng, 2018, 2(4):239-253

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Nat Protoc, 2018, 13(12):2827-2843

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Nat Commun, 2018, 9(1):4550

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Nat Commun, 2018, 9(1):1357

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EMBO Mol Med, 2018, 10(5)

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Cancer Res, 2018, 78(8):2000-2013

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Cancer Res, 2018, 78(9):2383-2395

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NPJ Genom Med, 2018, 3:15

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Cancer Res, 2018, 78(14):4007-4021

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Cell Rep, 2018, 24(8):2155-2166

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Cell Rep, 2018, 24(2):463-478

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Int J Cancer, 2018, 143(5):1188-1201

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Int J Cancer, 2018, 142(9):1926-1937

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Oncogene, 2018, 37(3):363-376

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Cancer Lett, 2018, 439:56-65

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Mol Cancer Ther, 2018, 17(2):347-354

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Mol Cancer Res, 2018, 16(4):599-609

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Oncol Rep, 2018, 40(6):3223-3234

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Oncol Rep, 2018, 40(1):479-487

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Oncol Lett, 2018, 15(3):3321-3328

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Oncotarget, 2018, 9(56):30869-30882

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J Exp Med, 2018, 215(1):159-175

PubMed: 29141866 ( click the link to review the publication )

Mol Cell, 2017, 67(3):512-527

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Mol Cell, 2017, 65(6):999-1013

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Nat Commun, 2017, 8:15623

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Nat Commun, 2017, 8;8:15617

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Nat Commun, 2017, 8:15021

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Nat Commun, 2017, 8(1):1278

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Dev Cell, 2017, 43(6):673-688

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Proc Natl Acad Sci U S A, 2017, 114(41):E8628-E8636

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Cancer Res, 2017, 77(16):4448-4459

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Mol Cancer Ther, 2017, 16(4):729-738

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Mol Cancer Ther, 2017, 10.1158/1535-7163

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Mol Cancer Ther, 2017, 16(9):1779-1790

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Mol Cell Proteomics, 2017, 16(10):1864-1888

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SLAS Discov, 2017, 22(8):974-984

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Cell Stem Cell, 2017, 20(2):233-246

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Oncotarget, 2017, 8(13):21806-21817

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Oncotarget, 2017, 8(4):6608-6622

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Nat Cell Biol, 2016, 18(12):1324-1335

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Blood, 2016, 127(10):1325-35

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Genome Biol, 2016, 17:80

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Clin Cancer Res, 2016, 22(3):644-56.

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Cancer Res, 2016, 76(24):7168-7180

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J Hematol Oncol, 2016, 9(1):113

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Cancer Discov, 2016, 6(10):1134-1147

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J Transl Med, 2016, 14:56

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Int J Biochem Cell Biol, 2016, 79:308-317

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PLoS One, 2016, 11(1):e0147682

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PLoS One, 2016, 10.1371/journal

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Oncotarget, 2016, 7(41):67277-67287

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Nature, 2016, 529(7586):413-417

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Oncotarget, 2016, 7(26):40398-40417

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Sci Rep, 2016, 6:20189

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Oncotarget, 2016, 7(45):72608-72621

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J Clin Invest, 2015, 10.1172/JCI78018

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J Clin Invest, 2015, 125(12):4559-71

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Genes Dev, 2015, 29(16):1677-82

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Cancer Res, 2015, 75(14):2851-62

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Oncogene, 2015, 10.1038/onc.2015.173

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Biomed Pharmacother, 2015, 75:40-50

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Acta Pharmacol Sin, 2015, 10.1038/aps.2015.4

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Exp Cell Res, 2015, 332(2):223-35

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Exp Cell Res, 2015, 332(2):223-35

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Int J Biochem Cell Biol, 2015, 60C:34-42

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Int Immunopharmacol, 2015, 28(1):675-85

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PLoS One, 2015, 10(9):e0133610

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PLoS One, 2015, 10(4):e0123410

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Immunol Res, 2015, 10.1007/s12026-015-8648-y

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Oncotarget, 2015, 6(31):31792-804

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J Clin Invest, 2014, 124(12):5490-502

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J Clin Invest, 2014, 124(11):4737-52

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J Exp Med, 2014, 211(13):2497-2505

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Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1392

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Cell Rep, 2014, 8(5):1265-70

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Oncogene, 2014, 10.1038/onc.2014.328

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PLoS Pathog, 2014, 10(6):e1004196

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Breast Cancer Res, 2014, 16(1):R9

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Breast Cancer Res, 2014, 16(4):406

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Cell Death Dis, 2014, 5:e1134

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Cell Death Dis, 2014, 5:e1013

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Mol Cancer Res, 2014, 12(10):1520-31

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J Biol Chem, 2014, 289(33):22785-97

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PLoS One, 2014, 9(10):e108780

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PLoS One, 2014, 9(7):e101969

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Biochem Biophys Res Commun, 2014, 10.1016/j.bbrc.2014.09.129

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Oncotarget, 2014, 5(14):5295-303

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Clin Cancer Res, 2013, 19(21):5940-51

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Cancer Res, 2013, 73(17):5459-72

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Oncogene, 2013, 10.1038/onc.2013.509

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Breast Cancer Res, 2013, 15(4):R55

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Cell Commun Signal, 2013, 11(1):3

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Mol Cancer Res, 2013, 11(10):1269-78

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BMC Cancer, 2013, 13:465

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Cancer Chemother Pharmacol, 2013, 71(5):1297-307

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University Gattingen, 2013, Elisabeth Hand

PubMed: ( click the link to review the publication )

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description

Targets

p110α ^[1] (Cell-free assay)	p110δ ^[1] (Cell-free assay)	p110β ^[1] (Cell-free assay)	p110γ ^[1] (Cell-free assay)	Vps34 ^[1] (Cell-free assay)	View More
52 nM	116 nM	166 nM	262 nM	2.4 μM	View More

In vitro

BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. ^[1] BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. ^[2] BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. ^[3] A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
MCF7	MVHDfZRwfG:6aXOgRZN{[Xl?		NIPuV2Y4OiCq	M2XvNGROW09?	M4PmOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFiRUW0OWshdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFE2QCEQvF2=	M2XkVVI1QTByMk[2
DU145	MVnDfZRwfG:6aXOgRZN{[Xl?		NHvZ[Gk4OiCq	MlnmSG1UVw>?	M1PIOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiTFvCNUBufXSjboSge4l1cCCJSUWwJI9nKDBwMECwOFM2KM7:TR?=	MlPJNlQ6ODB{Nk[=
A2780	NYfIWGhtS3m2b4TvfIlkKEG\|c3H5		NYfoNZhRPzJiaB?=	NYDKemJmTE2VTx?=	M4PvXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO\|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2=	MlTnNlQ6ODB{Nk[=
U87MG	MVLDfZRwfG:6aXOgRZN{[Xl?		MmDRO\|IhcA>?	NYPWWoR4TE2VTx?=	MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh\|ryP	NYHkTo94OjR7MECyOlY>
A2780	MXLGeY5kfGmxbjDBd5NigQ>?		MWixJIg>	MXrEUXNQ	MmqyTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkC1OUDPxE1?	MlvBNlQ6ODB{Nk[=
DU145	M{LXd2Z2dmO2aX;uJGF{e2G7		NVXGS\|lzOSCq	NIq1c2dFVVOR	MmL0TY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1?	MlX0NlQ6ODB{Nk[=
A2780	M1:1S2Z2dmO2aX;uJGF{e2G7		MXGxJIg>	NUfofHVITE2VTx?=	M3\HZ2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO\|Qh\|ryP	MnqzNlQ6ODB{Nk[=
MCF7	MYTGeY5kfGmxbjDBd5NigQ>?		MnT2NUBp	NVO3VWdLTE2VTx?=	M4PyemlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFW1OFVMKG23dHHueE1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6xJO69VQ>?	M{H0R\|I1QTByMk[2
U87MG	Mo\hSpVv[3Srb36gRZN{[Xl?		MUSxJIg>	M4TSVmROW09?	NVvGWYw2UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJHU5P02JIHPlcIx{KHerdHigSWM2OCCxZjCwMlE{KM7:TR?=	NI\5Rm4zPDlyMEK2Oi=>
A2780	NIjpfJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NUXI[nhOPzJiaB?=	MYLEUXNQ	MnTySWM2OD1yLkWyJO69VQ>?	MVuyOFkxODJ4Nh?=
SKMES-1	MWjDfZRwfG:6aXOgRZN{[Xl?	MoLSNUDPxE1?	NF7xVWY4OiCq		NUPidGhNUW6mdXPld{Bk\WyuIHTlZZRp	MWCyOlAyOzNzOB?=
H596	MkjlSpVv[3Srb36gRZN{[Xl?	M{j0dVEh\|ryP			NXvF[XA6UW2yYXnyd{Bk\WyuIH3p[5JifGmxbh?=	MUKyOlAyOzNzOB?=
HCC2450	MljrSpVv[3Srb36gRZN{[Xl?	MXexJO69VQ>?			NWmwfHF6UW2yYXnyd{Bk\WyuIHnueoF{cW:w	NH:4PYMzPjBzM{OxPC=>
A549	M{D5NGZ2dmO2aX;uJGF{e2G7	NYX3Z3lDPTByIH7N	NI\6cVk1QCCq	NH7RZoNFVVOR	M{LMcGlvcGmkaYTzJGFsfCCjY4TpeoF1cW:w	MYGyOVk{PzJ7OR?=
A549	NIPtVHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NIO0SJYyKM7:TR?=	MlzZO\|IhcA>?	Ml\YSG1UVw>?	M2LlemlvcGmkaYTzJINmdGxiZ4Lve5Rp	NX3GbVRVOjV7M{eyPVk>
H522	NETHR5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NH[3dY0yKM7:TR?=	MnTmO\|IhcA>?	M4XvbGROW09?	MVzJcohq[mm2czDj[YxtKGe{b4f0bC=>	MWKyOVk{PzJ7OR?=
LNCaP	M1TncmZ2dmO2aX;uJGF{e2G7	NU\j[W91OSEQvF2=			NUPhSGw3W3WycILld5NmeyCyLVHLWEBt\X[nbIO=	NITSUVEzPTN4MEe5PS=>
LNCaP95	M4X5PGZ2dmO2aX;uJGF{e2G7	MVqxJO69VQ>?			MYXTeZBxemW\|c3XzJJAuSUuWIHzleoVtew>?	NYG4WVF5OjV\|NkC3PVk>
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BCR-ABL	NX3wdVlZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml;BNE4zPS1zMN88US=>	M4[3W\|Rl		M4nCSJNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25?	M1\oelI1OjR2NkGy
LC-1/SQSF	MXvGeY5kfGmxbjDBd5NigQ>?	NXHiT2VOO87:TR?=	NHPGcXkzPGh?	NHXtR5JFVVOR	NFjYVGJl\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw>	MUSyN\|k5ODB7Mx?=
Primary CLL cells	MUjBdI9xfG:\|aYOgRZN{[Xl?	NYnuT3VZOS1zMN88US=>	NW[3V2NTPDiq		MnzhbY5lfWOnczDhdI9xfG:\|aYOgbY4hS0yOIHPlcIx{KGmwZHXw[Y5l\W62IH;mJJBzd2ewb4P0bYMhdWG{a3Xydy=>	NUPoelJHOjN6NUC4NFc>
Primary CLL cells	M3TLeWtqdmG\|ZTDBd5NigQ>?	MlW4Nu69VQ>?	Mm\1N\|BucW5?		M1[yTYRm[3KnYYPl[EBRUTONIHHjeIl3cXS7	NUHh[WF4OjN6NUC4NFc>
Primary CLL cells	NXLZb3M3S3m2b4TvfIlkKEG\|c3H5	NHjlXm8z\|ryP	NIDMbGUzPGh?		MY\pcoR2[2W\|IHPlcIwh[3m2b4TvfIlkcXS7	MoP0NlM5PTB6MEe=
human NSCLC cell lines	MV3BdI9xfG:\|aYOgRZN{[Xl?	MnL0NE4yOjVvNN88US=>	M2TNWVI1cA>?	NXjDWW14TE2VTx?=	MYDJR\|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?=	NH\zc5ozOzV4MkS3Ni=>
human HCC cell lines	NH:3VJhE\WyuII\pZYJqdGm2eTDhd5NigQ>?	NIDjRowxNjByNT2x{txO	M3TLR\|Q5cA>?		NFHzbXZKSzVyPUJOwG0>	MYKyN\|Q5QTl7OR?=
Huh7	MnXYT4lv[XOnIFHzd4F6	NUfhVY11Oc7:TR?=	NYfKToxnPDiq		Mmfjd4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0	NHW0cFMzOzR6OUm5PS=>
SK-HEP1	NIL2TJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXuxMVIx\|ryP	MWe3Nog>	MYTEUXNQ	NULscpl2UUN3MP-8oFHPxE1?	MnO0NlM1PzlzM{[=
786-0	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmfTNU0zOM7:TR?=	Mn;DO\|Jp	NY[5T3B[TE2VTx?=	MlyzTWM2OO,:nEJOwG0>	MkXvNlM1PzlzM{[=
JVM2	NUjCVFZDS3m2b4TvfIlkcXS7IHHzd4F6	NIXFS5QxNjJvMkFOwG0>	NF3NUmI4Omh?	NIPuN\|lFVVOR	Mmn4TWM2OD1yLkpOwG0>	NV3nPItrOjN{M{i2N\|k>
EHEB	M{CwTmN6fG:2b4jpZ4l1gSCjc4PhfS=>	MVGwMlIuOjEQvF2=	M4\ld\|czcA>?	MkjOSG1UVw>?	MmC2TWM2OD1yLkhOwG0>	MorCNlMzOzh4M{m=
MEC2	NFjFZXpEgXSxdH;4bYNqfHliYYPzZZk>	NEnWeYcxNjJvMkFOwG0>	NVr5UWNpPzKq	NXWwVoZPTE2VTx?=	MmDWTWM2OD1yLkhOwG0>	M4nNV\|I{OjN6NkO5
primary B-CLL lymphocytes	MULBdI9xfG:\|aYOgRZN{[Xl?	MmPYTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>?	MorPNlRp	Mn3BSG1UVw>?	NXvVdJJYUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>?	NX\wemFyOjN{M{i2N\|k>
primary B-CLL lymphocytes	Ml7DT4lv[XOnIFHzd4F6	MUjJR\|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m	MX[yOIg>		MVLpcohq[mm2czDwO\|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?=	NVj5SoNQOjN{M{i2N\|k>
human NSCLC	NXPjVnduT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmnYNE42NTMQvF2=	M4m2NVczcA>?		NWjCNWFGUUN3ME2x{txO	NITlXoozOjd6MUO5Ny=>
human NSCLC	NXK0TJV6U2mwYYPlJGF{e2G7	NITBO4Ey\|ryP	M1n4dlI1cA>?		NYi1TVNEcW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=>	MWiyNlc5OTN7Mx?=
Y1 cell line	MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVjLcG9UOC5zzszNM\|HPxE1?	MWWyOIg>	MkLSSG1UVw>?	M2GwdYlvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy\|	NEfYUmIzOjZ7MkmwOC=>
PIK3CA-mutant MCF7	NFX4SnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHzFV5VIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?=	M{TPW\|czcA>?		M1n2bmdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P	NGXMZVIzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7	MVfLbY5ie2ViQYPzZZk>	NIXsSHdKSzVyPUGxOOKyO26P	MVO3Nog>		NG\KN3dKSzVyPUGxOOKyO26PIHnuJJJm\HWlaX7nJGFsfCCyaH;zdIhwenmuYYTpc44hdGW4ZXzz	M1TCVVIzPjV\|OU[3
MCF7-myr-Akt	NFG1OlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYnHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>?	MmjVO\|Jp		NFzsZ4dIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?=	NU\JZWE4OjJ4NUO5Olc>
colon cancer cell lines	NHvMbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml3FNE0yOM7:TR?=	MX[3Nog>	M4jZSWROW09?	NITUZVZKSzVyPUJOwG0>	MmPBNlI2PDN6NUe=
gastric cancer cell lines	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYL2dFhROC1zMN88US=>	MVG3Nog>	MX;EUXNQ	M2HhRWlEPTB;Mj21{txO	NYTQ[5lqOjJ3NEO4OVc>
HCT-116/HT-29/MKN-45	MlyzRZBweHSxc3nzJGF{e2G7	NXrO[2M2Os7:TR?=	MUK0PIg>		M2\UO5NpcW[2IHnuJGczKHCqYYPl	NVzHUXJSOjJ3NEO4OVc>
HT-29 and HCT-116	MXjDZZNx[XOnIHHzd4F6	M3XNOlXPxE1?	MmDjNlRp		MlTobY5lfWOnczDjZZNx[XOnIHHjeIl3cXS7	MY[yNlU1Ozh3Nx?=
MM cell lines	M4KxOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M36zc\|Ex\|ryP	NVj0WnpLOjSq	MXfEUXNQ	NYjxc5dYUUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn	MkS0NlIzODd2OEW=
ARP-1	MV\BdI9xfG:\|aYOgRZN{[Xl?	NWTyeXBKOTEQvF2=	MlfjNlRp	M2r6eWROW09?	NGPXSIlqdmS3Y3XzJG1OKGOnbHygZZBweHSxc3nzJJRpem:3Z3igZ4F{eGG\|ZTDhZ5RqfmG2aX;u	MXKyNlIxPzR6NR?=
SNU-601	MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MluzO\|Jp	NIfodlNFVVOR	M{nMXmlEPTB;MD64NVbDuTBwME[z{txO	MlHhNlIyPTl6MUS=
SNU-1	Mlf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M4HTb\|czcA>?	NILMVo1FVVOR	M17LWWlEPTB;MT6wPFLDuTBwMEK4{txO	MmWyNlIyPTl6MUS=
SNU-668	NFO2T\|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MVO3Nog>	MWXEUXNQ	MojKTWM2OD1zLkW3PeKyOC5yN{VOwG0>	NW\4eFJ4OjJzNUm4NVQ>
AGS	M1naVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NVnQR29mPzKq	NUnwSno{TE2VTx?=	NH;1bnFKSzVyPUGuO\|E1yrFyLkGxO:69VQ>?	NX\1SGRuOjJzNUm4NVQ>
SNU-216	M4raPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M{WzO\|czcA>?	M321b2ROW09?	MoOwTWM2OD1{Lk[5NuKyOC5yOENOwG0>	NWPhb\|dTOjJzNUm4NVQ>
SNU-5	M2\0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1vXWlczcA>?	NHfrb\|dFVVOR	NXzENpRvUUN3ME2xMlM2OcLzMD6wPVHPxE1?	Ml;3NlIyPTl6MUS=
SNU-638	NI\yZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkTNO\|Jp	MmHzSG1UVw>?	M4L2N2lEPTB;Mj6yPFLDuTBwMEWz{txO	NHPWcpAzOjF3OUixOC=>
SNU-16	NHK1WHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Moj5O\|Jp	NEPhUVFFVVOR	M1TvZWlEPTB;MT61O\|PDuTBwMECx{txO	NGrVRZYzOjF3OUixOC=>
SNU-484	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NUD2cnV4PzKq	NXTSWWk6TE2VTx?=	M2CwcWlEPTB;MT63NljDuTBwMES1{txO	MXGyNlE2QThzNB?=
SNU-620	MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MX[3Nog>	M4DH[mROW09?	NEn5XFFKSzVyPUKuPVM6yrFyLkCwNe69VQ>?	Mnr3NlIyPTl6MUS=
SNU-719	NXmzTZp4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MYK3Nog>	M2m2PGROW09?	NYW1VGFpUUN3ME2zMlA{P8LzMD6wN\|LPxE1?	MmC0NlIyPTl6MUS=
glioma cell lines	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NH70PI44Omh?		MUXJR\|UxRTFvMt88US=>	M4DkUlIzODZ3MEiw
U87	MXXBdI9xfG:\|aYOgRZN{[Xl?	MojiNu69VQ>?	NUP4b2YzPzKq		MorvbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO=	NHT4UY0zOjB4NUC4NC=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AKT (T308) / p-AKT (S473) / AKT; PubMed: 27283525 J Neurooncol Left western blots showing levels of pAkt (T308), pAkt (S473) and total Akt in U87 cells exposed to buparlisib for 72 h. Right densitometric assessment of western blots, showing relative changes in phosphorylation. p-FOXO3a (S253) / FOXO3a; PubMed: 28036259 Oncotarget Cells were treated with 0.5 μM BKM120 for 24 h and cell lysates were immunoblotted with the indicated antibodies. Actin was used as the loading control. Nuclear NF-κB p65 / NF-κB p65; PubMed: 26673665 Cell Death Dis Western blots show BKM120 downregulating pAKT, nuclear NF-κB p65 and total NF-κB p65 in MDR and their parental cells. β-actin was used as a loading control for pAKT, AKT and total NF-κB p65. Lamin B was used as a loading control for nuclear NF-κB p65. p-ERK / ERK / LC3; PubMed: 27572309 Oncotarget The indicated cell lines were exposed to different concentrations of BKM120 as indicated for 8 h A. or with 2 μM BKM120 for the indicated times B. The cells were then harvested for preparation of whole-cell protein lysates and subsequent Western blot analysis to detect the given proteins. p-STAT3 / STAT3 / p-ERK / ERK / p-S6; PubMed: 29928341 Oncol Lett Western blot analysis of H460 and H2126 cell lysates using specific antibodies to phosphorylated or total proteins of STAT3, ERK1/2, AKT, S6 or GAPDH (loading control). The cells were treated with increasing concentrations of BKM120 for 24 h. p-MET / MET; PubMed: 29928341 Oncol Lett The expression of phosphorylated or total forms of MET protein was analyzed by western blotting.	27283525 28036259 26673665 27572309 29928341
Immunofluorescence	FOXO3a; PubMed: 28036259 Oncotarget Cells were cultured on coverslips to approximately 60% confluency and then treated with 1 μM BKM120 for an additional 24 h. Immunofluorescence staining was performed using an anti-FOXO3a antibody and the nuclei were stained with DAPI. Scale bar, 20 μm.	28036259
Growth inhibition assay	Cell viability; PubMed: 26673665 Cell Death Dis Dose-response curves were used to calculate the IC50 of BKM120 for MCs of MCF-7/A02 cells (upper) and CALDOX cells (lower).	26673665

In vivo

BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. ^[1] BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival. ^[2]

Protocol

Kinase Assay:^[1]	- Collapse PI3K biochemical assay (ATP depletion assay): BKM120 is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 µL per well. To start the reaction, 25 µL of 10 nM PI3 kinase and 5 µg/mL 1-α-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl₂, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 µL of 2 µM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted and then stopped by the addition of 25 µL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence.
Cell Research:^[1]	- Collapse Cell lines: A2780 cells. Concentrations: 0-6.6 μM Incubation Time: 3 days. Method: 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 10³ cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux. (Only for Reference)
Animal Research:^[1]	- Collapse Animal Models: U87MG and A2780 xenografts are established in female nu/nu mice. Dosages: ~60 mg/kg. Administration: Dosed orally daily (q.d.). (Only for Reference)

References

[4] Koul D, et al. Clin Cancer Res, 2012, 18(1), 184-195.

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Solubility (25°C)

In vitro	DMSO	82 mg/mL (199.8 mM)
	Water	Insoluble
	Ethanol	'2 mg/mL
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing.	15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Buparlisib (BKM120) SDF

Molecular Weight	410.39
Formula	C₁₈H₂₁F₃N₆O₂
CAS No.	944396-07-0
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	NVP-BKM120
Smiles	C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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The Serial Dilution Calculator Equation

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Computed Result

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Molecular Weight Calculator

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04338399	Not yet recruiting	Drug: Buparlisib & Paclitaxel	Head and Neck Cancer	Adlai Nortye Biopharma Co. Ltd.	July 31 2020	Phase 3
NCT02614508	Terminated	Drug: Buparlisib\|Drug: Ibrutinib\|Biological: Ofatumumab	Recurrent Chronic Lymphocytic Leukemia\|Recurrent Small Lymphocytic Lymphoma\|Refractory Chronic Lymphocytic Leukemia\|Refractory Small Lymphocytic Lymphoma	Emory University\|Novartis	January 2016	Phase 1
NCT01613677	Withdrawn	Drug: BKM120	Treatment for Metastatic or Locally Advanced Cervical Cancer	Novartis Pharmaceuticals\|Novartis	November 2015	Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PI3K Signaling Pathway Map

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Selective PI3K Inhibitors

TGX-221 : p110β-specific, IC50=5 nM.
Most Potent PI3K Inhibitor

BEZ235 (NVP-BEZ235, Dactolisib) : p110α/γ/δ/β, IC50=4 nM/5 nM/7 nM/75 nM.
FDA-approved PI3K Inhibitor

CAL-101 (Idelalisib, GS-1101) : Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.
Newest PI3K Inhibitor

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Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Alpelisib (BYL719)

Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

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Buparlisib (BKM120)