Buparlisib (BKM120)

Name: Buparlisib (BKM120)
Brand: Selleck Chemicals
SKU: S2247
Rating: 5 (151 reviews)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

151 publications

Molecular Weight(MW): 410.39

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. Phase 2.

Selleck's Buparlisib (BKM120) has been cited by 151 publications

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

PubMed: 31978326 ( click the link to review the publication )

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

PubMed: 32152508 ( click the link to review the publication )

Science, 2019, 364(6441)

PubMed: 31097636 ( click the link to review the publication )

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

PubMed: 30537514 ( click the link to review the publication )

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

PubMed: 29316436 ( click the link to review the publication )

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

PubMed: 29316436 ( click the link to review the publication )

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

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

PubMed: 28619981 ( click the link to review the publication )

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

PubMed: 26735014 ( click the link to review the publication )

Nat Med, 2015, 10.1038/nm.3855

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

PubMed: 26301689 ( click the link to review the publication )

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

PubMed: 24302555 ( click the link to review the publication )

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

PubMed: 22610277 ( click the link to review the publication )

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

PubMed: 22340590 ( click the link to review the publication )

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

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

PubMed: 32127496 ( click the link to review the publication )

Mol Cancer Res, 2020, 11

PubMed: 32161139 ( click the link to review the publication )

Front Neurosci, 2020, 2;14:223

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Eur J Pharmacol, 2020, 870:172821

PubMed: 31770526 ( click the link to review the publication )

Cell Biol Int, 2020, 10.1002/cbin.11322

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

PubMed: 32123862 ( click the link to review the publication )

Mol Oncol, 2020, 10.1002/1878-0261.12673

PubMed: 32191822 ( click the link to review the publication )
Small GTPases, 2020, 10.1080/21541248

PubMed: 32043900 ( click the link to review the publication )

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

PubMed: 30692625 ( click the link to review the publication )

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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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

PubMed: 31570855 ( click the link to review the publication )

Cancer Lett, 2019, 466:23-34

PubMed: 31521695 ( click the link to review the publication )

Cancers (Basel), 2019, 11(2)

PubMed: 30736342 ( click the link to review the publication )

Mol Ther Oncolytics, 2019, 13:58-66

PubMed: 31016228 ( click the link to review the publication )

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

PubMed: 31217297 ( click the link to review the publication )

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

PubMed: 30787173 ( click the link to review the publication )

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

PubMed: 31545294 ( click the link to review the publication )

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

PubMed: 30536897 ( click the link to review the publication )

Front Oncol, 2019, 0.87569444444

PubMed: 31428587 ( click the link to review the publication )

Eur J Immunol, 2019, doi: 101002/eji201948241

PubMed: 31621069 ( click the link to review the publication )

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

PubMed: 30858165 ( click the link to review the publication )
Prostate, 2019, 79(11):1347-1359

PubMed: 31228231 ( click the link to review the publication )

Chem Biol Interact, 2019, 302:101-107

PubMed: 30703376 ( click the link to review the publication )

Eur J Pharmacol, 2019, 842:89-98

PubMed: 30401630 ( click the link to review the publication )

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

PubMed: 30981504 ( click the link to review the publication )

Leuk Lymphoma, 2019, 10.1080/10428194.2019.1594211

PubMed: 30947576 ( click the link to review the publication )

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

PubMed: 31129802 ( click the link to review the publication )

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

PubMed: 30867745 ( click the link to review the publication )

NPJ Breast Cancer, 2019, 05:31

PubMed: 31552290 ( click the link to review the publication )

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

PubMed: 30936439 ( click the link to review the publication )

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

PubMed: 30382243 ( click the link to review the publication )

Nat Commun, 2018, 9(1):4550

PubMed: 30382095 ( click the link to review the publication )

Nat Commun, 2018, 9(1):1357

PubMed: 29636477 ( click the link to review the publication )

EMBO Mol Med, 2018, 10(5)

PubMed: 29650805 ( click the link to review the publication )

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

PubMed: 29437705 ( click the link to review the publication )

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

PubMed: 29440171 ( click the link to review the publication )

NPJ Genom Med, 2018, 3:15

PubMed: 29951225 ( click the link to review the publication )

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

PubMed: 29760046 ( click the link to review the publication )

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

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

PubMed: 29996106 ( click the link to review the publication )

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

PubMed: 29582409 ( click the link to review the publication )

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

PubMed: 29210065 ( click the link to review the publication )

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

PubMed: 28945225 ( click the link to review the publication )

Cancer Lett, 2018, 439:56-65

PubMed: 30243708 ( click the link to review the publication )

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

PubMed: 28958992 ( click the link to review the publication )
Mol Cancer Res, 2018, 16(4):599-609

PubMed: 29330285 ( click the link to review the publication )

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

PubMed: 30272286 ( click the link to review the publication )

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

PubMed: 29767248 ( click the link to review the publication )

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

PubMed: 29435074 ( click the link to review the publication )

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

PubMed: 30112114 ( click the link to review the publication )

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

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

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

PubMed: 28757207 ( click the link to review the publication )

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

PubMed: 28306514 ( click the link to review the publication )

Nat Commun, 2017, 8:15623

PubMed: 28585535 ( click the link to review the publication )

Nat Commun, 2017, 8:15021

PubMed: 28443643 ( click the link to review the publication )

Nat Commun, 2017, 8(1):1278

PubMed: 29097657 ( click the link to review the publication )

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

PubMed: 29103956 ( click the link to review the publication )

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

PubMed: 28973876 ( click the link to review the publication )

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

PubMed: 28652248 ( click the link to review the publication )

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

PubMed: 28119490 ( click the link to review the publication )

Mol Cancer Ther, 2017, 10.1158/1535-7163

PubMed: 28119489 ( click the link to review the publication )

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

PubMed: 28619753 ( click the link to review the publication )

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

PubMed: 28794006 ( click the link to review the publication )

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

PubMed: 28644734 ( click the link to review the publication )

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

PubMed: 27989769 ( click the link to review the publication )

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

PubMed: 28423521 ( click the link to review the publication )

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

PubMed: 28036259 ( click the link to review the publication )

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

PubMed: 26668133 ( click the link to review the publication )

Genome Biol, 2016, 17:80

PubMed: 27139883 ( click the link to review the publication )
Clin Cancer Res, 2016, 22(3):644-56.

PubMed: 26224873 ( click the link to review the publication )

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

PubMed: 27913436 ( click the link to review the publication )

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

PubMed: 27765055 ( click the link to review the publication )

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

PubMed: 27604488 ( click the link to review the publication )

J Transl Med, 2016, 14:56

PubMed: 26912358 ( click the link to review the publication )

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

PubMed: 26735014 ( click the link to review the publication )

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

PubMed: 26272820 ( click the link to review the publication )

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

PubMed: 25977330 ( click the link to review the publication )

Oncogene, 2015, 10.1038/onc.2015.173

PubMed: 25982275 ( click the link to review the publication )

Biomed Pharmacother, 2015, 75:40-50

PubMed: 26463630 ( click the link to review the publication )

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

PubMed: 25250573 ( click the link to review the publication )

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

PubMed: 25488980 ( click the link to review the publication )

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

PubMed: 25284585 ( click the link to review the publication )

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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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

PubMed: 23918606 ( click the link to review the publication )

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

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Oncogene, 2013, 10.1038/onc.2013.509

PubMed: 24292683 ( click the link to review the publication )

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

PubMed: 23479136 ( click the link to review the publication )

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	MVvDfZRwfG:6aXOgRZN{[Xl?		NVrCd45ZPzJiaB?=	MV\EUXNQ	MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4PpcochWEl\|S3HsdIhiKEV3NEXLJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMECxOVgh\|ryP	MkPUNlQ6ODB{Nk[=
DU145	MYrDfZRwfG:6aXOgRZN{[Xl?		NUnjcFB6PzJiaB?=	NYTKd5VTTE2VTx?=	MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1?	MXOyOFkxODJ4Nh?=
A2780	NYLqR5lHS3m2b4TvfIlkKEG\|c3H5		NI[5TYs4OiCq	M3nLUWROW09?	NIe1VlFEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN	NW[xcHJbOjR7MECyOlY>
U87MG	MnPVR5l1d3SxeHnjJGF{e2G7		MoDmO\|IhcA>?	M3PXOWROW09?	M2\SXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY6QCEQvF2=	MXuyOFkxODJ4Nh?=
A2780	M{PpcGZ2dmO2aX;uJGF{e2G7		NFz4dIIyKGh?	M2HRR2ROW09?	MWXJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>?	MXWyOFkxODJ4Nh?=
DU145	MU\GeY5kfGmxbjDBd5NigQ>?		NGPNc4IyKGh?	NEjL[m5FVVOR	M3\vU2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBFXTF2NTDj[YxteyCqYYLic5JqdmdiTFvCNUBufXSjdHnvckB4cXSqIFXDOVAhd2ZiMD6wO\|Mh\|ryP	M3jLd\|I1QTByMk[2
A2780	Mn3YSpVv[3Srb36gRZN{[Xl?		M2DkeFEhcA>?	NX\yOI9lTE2VTx?=	MY\Jcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>?	NUfvfJFMOjR7MECyOlY>
MCF7	NFryOFVHfW6ldHnvckBCe3OjeR?=		NHvVRlQyKGh?	M1u0UGROW09?	MojFTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO	M3XKTVI1QTByMk[2
U87MG	NXvRS4h3TnWwY4Tpc44hSXO\|YYm=		NUHkW5BnOSCq	M13BTGROW09?	MXPJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO	MknxNlQ6ODB{Nk[=
A2780	NVHwTmNZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NEHrfo84OiCq	NGCySHNFVVOR	NX3Vb\|dYTUN3ME2wMlUzKM7:TR?=	MWGyOFkxODJ4Nh?=
SKMES-1	MlLBR5l1d3SxeHnjJGF{e2G7	NH\5WVYyKM7:TR?=	MUe3NkBp		M1rQbWlv\HWlZYOgZ4VtdCCmZXH0bC=>	NEDhUZczPjBzM{OxPC=>
H596	NWHyeFF[TnWwY4Tpc44hSXO\|YYm=	MYOxJO69VQ>?			NGW5UYRKdXCjaYLzJINmdGxibXnndoF1cW:w	NITvOHAzPjBzM{OxPC=>
HCC2450	NHTlWlBHfW6ldHnvckBCe3OjeR?=	MmDJNUDPxE1?			MorZTY1x[Wm{czDj[YxtKGmwdnHzbY9v	M3rCXFI3ODF\|M{G4
A549	MXLGeY5kfGmxbjDBd5NigQ>?	MYG1NFAhdk1?	M{C1SFQ5KGh?	NVK5e\|dsTE2VTx?=	NEX4UHNKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?=	Mmj6NlU6Ozd{OUm=
A549	MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NYq4VnBvOSEQvF2=	M4TX[FczKGh?	MojLSG1UVw>?	M13xfGlvcGmkaYTzJINmdGxiZ4Lve5Rp	NHzXUpYzPTl\|N{K5PS=>
H522	NVHmT4R1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml65NUDPxE1?	NXfnVFBGPzJiaB?=	NUPoeWFxTE2VTx?=	NGjKOXhKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	MX[yOVk{PzJ7OR?=
LNCaP	MWLGeY5kfGmxbjDBd5NigQ>?	NXHXZ3BVOSEQvF2=			MUfTeZBxemW\|c3XzJJAuSUuWIHzleoVtew>?	NXjpT3Z5OjV\|NkC3PVk>
LNCaP95	NWDpe496TnWwY4Tpc44hSXO\|YYm=	M2HaZVEh\|ryP			M2H4WHN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy\|	NV3pemszOjV\|NkC3PVk>
HCT-15	MoHNRZBwfG:\|aYOgRZN{[Xl?	NG\OZYMyOCEQvF2=	NH\K[W41QCCq	NFfySotFVVOR	MY\JcoR2[2W\|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	NWjKT5duOjVzNUKyOFU>
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UACC-732	NELwZ4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHzoToIyKM7:TR?=	NXn1SYV{PSCm	NGnjUpBFVVOR	NVv6cppyUUN3MEyxJO69VQ>?	MUKyOFg4QTd7Nh?=
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HCC202	NGrUdWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmD3NUDPxE1?	M{Dze\|Uh\A>?	MVPEUXNQ	MUXJR\|UxRDFizszN	MV6yOFg4QTd7Nh?=
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HCC1937	M4fDeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1u3R\|Eh\|ryP	M3;QcFUh\A>?	MoHTSG1UVw>?	MVzJR\|UxRDFizszN	M1WwUFI1QDd7N{m2
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BCR-ABL	M1ewUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlfDNE4zPS1zMN88US=>	NXX6eo5mPGR?		NGP6UIF{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w	NEHuZ5QzPDJ2NE[xNi=>
LC-1/SQSF	MY\GeY5kfGmxbjDBd5NigQ>?	NUK3U\|JTO87:TR?=	M1TGTVI1cA>?	MYLEUXNQ	NUnR[lV2\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt	NGfCR4EzOzl6MEC5Ny=>
Primary CLL cells	M{O5d2Fxd3C2b4Ppd{BCe3OjeR?=	NHvobHIyNTFyzszN	NWfPfYNYPDiq		NH;uVGdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{	NHfYTnczOzh3MEiwOy=>
Primary CLL cells	NX3neJJTU2mwYYPlJGF{e2G7	MnXxNu69VQ>?	NUfzPFJJOzCvaX6=		NEP4O5dl\WO{ZXHz[YQhWEl\|SzDhZ5Rqfmm2eR?=	NHO5SI0zOzh3MEiwOy=>
Primary CLL cells	M1r2bmN6fG:2b4jpZ{BCe3OjeR?=	MlPmNu69VQ>?	MVqyOIg>		NVTKW3dxcW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=>	MWOyN\|g2ODhyNx?=
human NSCLC cell lines	MX7BdI9xfG:\|aYOgRZN{[Xl?	M1r2[FAvOTJ3LUVOwG0>	MkX1NlRp	NIfpSnJFVVOR	MlnLTWM2OHNicnHu[4V{KG[{b32gNE41NTMQvF2=	MWmyN\|U3OjR5Mh?=
human HCC cell lines	M3npbWNmdGxidnnhZoltcXS7IHHzd4F6	NEixdGsxNjByNT2x{txO	M4PjN\|Q5cA>?		Mkn6TWM2OD1zzszN	M2ntV\|I{PDh7OUm5
Huh7	M1;TSWtqdmG\|ZTDBd5NigQ>?	MVWx{txO	MVi0PIg>		M{jKPZNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=>	NE\aVFQzOzR6OUm5PS=>
SK-HEP1	NFy2XnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYC4TnFkOS1{MN88US=>	M4rodlczcA>?	MUjEUXNQ	MVzJR\|Ux97zeMd88US=>	M{n0XVI{PDd7MUO2
786-0	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWCxMVIx\|ryP	NYHmR4xJPzKq	MlvoSG1UVw>?	NWnS[2NWUUN3MP-8oFHPxE1?	M4i5WlI{PDd7MUO2
JVM2	NXfDfmF4S3m2b4TvfIlkcXS7IHHzd4F6	NGrBc4QxNjJvMkFOwG0>	NUHvXpM1PzKq	M1;IbGROW09?	NYPMe4luUUN3ME2wMlnPxE1?	MV6yN\|I{QDZ\|OR?=
EHEB	NWO4RZRYS3m2b4TvfIlkcXS7IHHzd4F6	M3fXW\|AvOi1{MN88US=>	NHnpOnE4Omh?	M1fiOmROW09?	NHz0SmJKSzVyPUCuO:69VQ>?	MY[yN\|I{QDZ\|OR?=
MEC2	MmnVR5l1d3SxeHnjbZR6KGG\|c3H5	NFLXPW8xNjJvMkFOwG0>	NISzXWQ4Omh?	MmjMSG1UVw>?	Mn;qTWM2OD1yLkhOwG0>	M2rqb\|I{OjN6NkO5
primary B-CLL lymphocytes	MlPHRZBweHSxc3nzJGF{e2G7	M4DXZ2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV?	NHLj[YkzPGh?	NVq5XXRkTE2VTx?=	MnnLTWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=>	NYDOR4IyOjN{M{i2N\|k>
primary B-CLL lymphocytes	M3:4T2tqdmG\|ZTDBd5NigQ>?	MnL2TWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>?	M3OxdlI1cA>?		NXjzWWZbcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44>	M3Hje\|I{OjN6NkO5
human NSCLC	Ml31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1TYRVAvPS1{zszN	M2HHT\|czcA>?		NHeyTZNKSzVyPUJOwG0>	NFW1ZmozOjd6MUO5Ny=>
human NSCLC	NULHSVZuU2mwYYPlJGF{e2G7	Mn\2Ne69VQ>?	NYq1O2FlOjSq		MX;pcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62	NFPmOFMzOjd6MUO5Ny=>
Y1 cell line	NHGxVYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWfiWFd2OC5zzszNM\|HPxE1?	MlnxNlRp	MnzBSG1UVw>?	MXnpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>?	NXTWVGd7OjJ4OUK5NFQ>
PIK3CA-mutant MCF7	NX\nNVl6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUHnZVQ5T0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd\|bl2=	MlnPO\|Jp		NGjuNoFIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?=	MmXFNlI3PTN7Nke=
PIK3CA-mutant MCF7	MVzLbY5ie2ViQYPzZZk>	M17RdGlEPTB;MUG0xtE{dk1?	MnPGO\|Jp		MXzJR\|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:\|cHjvdplt[XSrb36gcIV3\Wy\|	M4nEUlIzPjV\|OU[3
MCF7-myr-Akt	M2PEd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NE[2ZWhIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?=	NIjtU2Y4Omh?		MYTHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>?	M4f0R\|IzPjV\|OU[3
colon cancer cell lines	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NInaOYwxNTFyzszN	NGrrNlA4Omh?	NFfTUVRFVVOR	MU\JR\|UxRTIQvF2=	NUHGdId6OjJ3NEO4OVc>
gastric cancer cell lines	M1HJUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV:wMVEx\|ryP	MnW2O\|Jp	Ml;JSG1UVw>?	MUfJR\|UxRTJvNd88US=>	Mk\ZNlI2PDN6NUe=
HCT-116/HT-29/MKN-45	MUHBdI9xfG:\|aYOgRZN{[Xl?	NGS4dIIz\|ryP	MXO0PIg>		NXrLVmVbe2irZoSgbY4hTzJicHjhd4U>	M{Hpc\|IzPTR\|OEW3
HT-29 and HCT-116	M2\5T2Nie3Cjc3WgZZN{[Xl?	Mn\VOe69VQ>?	MUSyOIg>		M1fETIlv\HWlZYOgZ4F{eGG\|ZTDhZ5Rqfmm2eR?=	MmjhNlI2PDN6NUe=
MM cell lines	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkHUNVDPxE1?	M3n0N\|I1cA>?	MULEUXNQ	MY\JR\|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U>	MVyyNlIxPzR6NR?=
ARP-1	Mn33RZBweHSxc3nzJGF{e2G7	NEjRVYoyOM7:TR?=	NEHhNGYzPGh?	NYfoS4h5TE2VTx?=	M2nTNolv\HWlZYOgUW0h[2WubDDhdI9xfG:\|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36=	NWXLV4RTOjJ{MEe0PFU>
SNU-601	NY\NcJlQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWC3Nog>	M4LnTWROW09?	Mlm0TWM2OD1yLkixOuKyOC5yNkROwG0>	NULLdJBOOjJzNUm4NVQ>
SNU-1	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NHzuUFY4Omh?	M1fhTmROW09?	NUW3ZXk5UUN3ME2xMlA5OsLzMD6wNljPxE1?	NF3PbIozOjF3OUixOC=>
SNU-668	NVjsflU3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M{X5WVczcA>?	Mo\QSG1UVw>?	MkjpTWM2OD1zLkW3PeKyOC5yN{VOwG0>	MlnmNlIyPTl6MUS=
AGS	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFny[WQ4Omh?	NEXNVFRFVVOR	NE[5T4hKSzVyPUGuO\|E1yrFyLkGxO:69VQ>?	MkHzNlIyPTl6MUS=
SNU-216	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M4DiS\|czcA>?	MXzEUXNQ	NV7oZpQ{UUN3ME2yMlY6OsLzMD6wPFLPxE1?	NYOzN3RNOjJzNUm4NVQ>
SNU-5	NVjCWIF1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NILt[XI4Omh?	Mn3MSG1UVw>?	MnzCTWM2OD1zLkO1NeKyOC5yOUJOwG0>	MWmyNlE2QThzNB?=
SNU-638	NHT4VIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkCyO\|Jp	M3XQOWROW09?	NH3ucYpKSzVyPUKuNlgzyrFyLkC1N:69VQ>?	NYnTdXFiOjJzNUm4NVQ>
SNU-16	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M4TINVczcA>?	MXrEUXNQ	MUfJR\|UxRTFwNUezxtExNjByMd88US=>	M4KxVFIzOTV7OEG0
SNU-484	MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NI[4bZU4Omh?	NH;6SZNFVVOR	NHi2OGhKSzVyPUGuO\|I5yrFyLkC0Oe69VQ>?	NV7iUXRWOjJzNUm4NVQ>
SNU-620	M{Lzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1\SV\|czcA>?	M37mNWROW09?	NVfTbo5OUUN3ME2yMlk{QcLzMD6wNFHPxE1?	NGLlfIIzOjF3OUixOC=>
SNU-719	NWHEWopST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NVf6PJNwPzKq	MWDEUXNQ	NXnmS3c6UUN3ME2zMlA{P8LzMD6wN\|LPxE1?	NIPFfYszOjF3OUixOC=>
glioma cell lines	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MWK3Nog>		NGjCbFZKSzVyPUGtNu69VQ>?	NX;rO29DOjJyNkWwPFA>
U87	MV7BdI9xfG:\|aYOgRZN{[Xl?	NV;nNY5VOs7:TR?=	MYi3Nog>		MofVbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO=	MVWyNlA3PTB6MB?=

... 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)
	Ethanol	2 mg/mL (4.87 mM)
	Water	Insoluble
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
Storage	2 years -80°C in solvent
Synonyms	NVP-BKM120
Smiles	NC1=CC(=C(C=N1)C2=NC(=NC(=C2)N3CCOCC3)N4CCOCC4)C(F)(F)F

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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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

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Calculation results:

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

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-05-15)

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.

Handling Instructions

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Selective PI3K Inhibitors

CAL-101 (Idelalisib, GS-1101) : p110δ-selective, IC50=2.5 nM.
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

VS-5584 (SB2343) ^New : Potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

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Features:A beta isoform-sparing PI3K inhibitor.
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Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
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Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
Wortmannin

Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
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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)