Buparlisib (BKM120)

Name: Buparlisib (BKM120)
Brand: Selleck Chemicals
SKU: S2247
Rating: 5 (137 reviews)

For research use only. Not for use in humans.

Catalog No.S2247 Synonyms: NVP-BKM120

137 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 137 publications

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

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

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

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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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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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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

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

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

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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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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, 8:15021

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

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

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

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

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

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

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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	M2D0OmN6fG:2b4jpZ{BCe3OjeR?=		M4PxTVczKGh?	MVnEUXNQ	NXL5b2ZqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=>	M4rkVFI1QTByMk[2
DU145	MUTDfZRwfG:6aXOgRZN{[Xl?		MoPYO\|IhcA>?	NILFfI5FVVOR	NHjRNphEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2=	MXOyOFkxODJ4Nh?=
A2780	NXHv[FFjS3m2b4TvfIlkKEG\|c3H5		NYThRYdEPzJiaB?=	M2jVR2ROW09?	NYfEc4dFS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjN3IN88US=>	M{e1d\|I1QTByMk[2
U87MG	NUjsO\|FFS3m2b4TvfIlkKEG\|c3H5		M37WWlczKGh?	MnfCSG1UVw>?	NVS5cVRlS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjl6IN88US=>	NH7s[pEzPDlyMEK2Oi=>
A2780	M{XteGZ2dmO2aX;uJGF{e2G7		MXuxJIg>	NGfmTItFVVOR	MXvJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>?	NYXkdpltOjR7MECyOlY>
DU145	Mm\uSpVv[3Srb36gRZN{[Xl?		M1zxW\|EhcA>?	NXvEXm5RTE2VTx?=	M4O4cGlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBFXTF2NTDj[YxteyCqYYLic5JqdmdiTFvCNUBufXSjdHnvckB4cXSqIFXDOVAhd2ZiMD6wO\|Mh\|ryP	MU[yOFkxODJ4Nh?=
A2780	NWfib4tPTnWwY4Tpc44hSXO\|YYm=		MVWxJIg>	M{jyPWROW09?	NIDMeGxKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDFR\|UxKG:oIECuNFc1KM7:TR?=	MnzUNlQ6ODB{Nk[=
MCF7	NFLlflZHfW6ldHnvckBCe3OjeR?=		MUexJIg>	Ml3jSG1UVw>?	M2jOWWlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFW1OFVMKG23dHHueE1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6xJO69VQ>?	MlTqNlQ6ODB{Nk[=
U87MG	MVjGeY5kfGmxbjDBd5NigQ>?		MVmxJIg>	NW\WPYR6TE2VTx?=	M3;Uc2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1?	Mnm0NlQ6ODB{Nk[=
A2780	MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NUDE[ZlHPzJiaB?=	MkTqSG1UVw>?	NYXZc3hVTUN3ME2wMlUzKM7:TR?=	M2Hld\|I1QTByMk[2
SKMES-1	M1THWGN6fG:2b4jpZ{BCe3OjeR?=	NUfWRXl[OSEQvF2=	NVv2WpJ6PzJiaB?=		M3:yXmlv\HWlZYOgZ4VtdCCmZXH0bC=>	M37KWFI3ODF\|M{G4
H596	M4DxVGZ2dmO2aX;uJGF{e2G7	Mmq1NUDPxE1?			MnzBTY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>?	NFfV[4ozPjBzM{OxPC=>
HCC2450	NGe1NXdHfW6ldHnvckBCe3OjeR?=	NUHiVnJjOSEQvF2=			MofvTY1x[Wm{czDj[YxtKGmwdnHzbY9v	NHjLXGszPjBzM{OxPC=>
A549	MX7GeY5kfGmxbjDBd5NigQ>?	MVK1NFAhdk1?	M17IXVQ5KGh?	MlvBSG1UVw>?	M3n5S2lvcGmkaYTzJGFsfCCjY4TpeoF1cW:w	MV:yOVk{PzJ7OR?=
A549	NHrQSHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX:xJO69VQ>?	MkCwO\|IhcA>?	Mo\FSG1UVw>?	NF;4SGdKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	MWmyOVk{PzJ7OR?=
H522	NH7veHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlHvNUDPxE1?	NEOydmY4OiCq	MWLEUXNQ	NYWwUFY6UW6qaXLpeJMh[2WubDDndo94fGh?	NEHqdmszPTl\|N{K5PS=>
LNCaP	MXnGeY5kfGmxbjDBd5NigQ>?	NEnCboQyKM7:TR?=			M2npUnN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy\|	Mlz1NlU{PjB5OUm=
LNCaP95	NInaWVVHfW6ldHnvckBCe3OjeR?=	M2GwWFEh\|ryP			M1e5NHN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy\|	MmL4NlU{PjB5OUm=
HCT-15	Mk\ZRZBwfG:\|aYOgRZN{[Xl?	NIHjSmgyOCEQvF2=	NFLoboo1QCCq	MWfEUXNQ	NVLVcFQxUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVE2KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36=	NYjDV5JwOjVzNUKyOFU>
HCT-116	NYDlS2NESXCxdH;zbZMhSXO\|YYm=	MofZNVAh\|ryP	MXW0PEBp	MXnEUXNQ	M{T4Zmlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	NHHQN3kzPTF3MkK0OS=>
NCI-H460	NXP5PJkzSXCxdH;zbZMhSXO\|YYm=	Mn60NVAh\|ryP	Mmi3OFghcA>?	NVHwXoRxTE2VTx?=	MUfJcoR2[2W\|IHHwc5B1d3OrczDpckBPS0lvSES2NEBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	M3XGUlI2OTV{MkS1
SKOV-3	NGTVSmhCeG:2b4Ppd{BCe3OjeR?=	MX:xNEDPxE1?	NGXIUIM1QCCq	NUf6O5dsTE2VTx?=	NIP4cpdKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCVS1;WMVMh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	MkjmNlUyPTJ{NEW=
BSY-1	NV3kWXpjSXCxdH;zbZMhSXO\|YYm=	NEfnS5UyOCEQvF2=	MVe0PEBp	M1PyOGROW09?	M3izb2lv\HWlZYOgZZBweHSxc3nzJIlvKEKVWT2xJINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	NVvwRldMOjVzNUKyOFU>
MKN-1	Ml7SRZBwfG:\|aYOgRZN{[Xl?	MlS3NVAh\|ryP	MVO0PEBp	MkTMSG1UVw>?	MUPJcoR2[2W\|IHHwc5B1d3OrczDpckBOU05vMTDj[YxteyCqYYLic5VzcW6pIGDJT\|NESSCqb4TzdI91KG23dHH0bY9v	NVLIeVFROjVzNUKyOFU>
NCI-H522	MoKzRZBwfG:\|aYOgRZN{[Xl?	NIjQfGMyOCEQvF2=	Mn7YOFghcA>?	M2nIVGROW09?	MX3JcoR2[2W\|IHHwc5B1d3Orcx?=	NUO4bFM6OjVzNUKyOFU>
OVCAR-3	MX\BdI91d3OrczDBd5NigQ>?	M4HqZlExKM7:TR?=	MVi0PEBp	NFv2SppFVVOR	NIrjN2VKdmS3Y3XzJIFxd3C2b4Ppdy=>	M{Xw[\|I2OTV{MkS1
HBC-5	NXLnNnhWSXCxdH;zbZMhSXO\|YYm=	MkjFNVAh\|ryP	NGPmZ2I1QCCq	MVrEUXNQ	NILHd3JKdmS3Y3XzJIFxd3C2b4Ppdy=>	MV2yOVE2OjJ2NR?=
RXF-631L	NFj1TWRCeG:2b4Ppd{BCe3OjeR?=	MV:xNEDPxE1?	NGPhXnQ1QCCq	MoX4SG1UVw>?	NE\TdGtKdmS3Y3XzJIFxd3C2b4Ppdy=>	NWXtWZJIOjVzNUKyOFU>
MKN-45	NWi5bnRQSXCxdH;zbZMhSXO\|YYm=	M2jMZlExKM7:TR?=	M4PlVVQ5KGh?	M3LmUWROW09?	MmTSTY5lfWOnczDhdI9xfG:\|aYO=	M3y3UVI2OTV{MkS1
BON-1	NIjNc5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV;RflFpPTByIH7N	MVKxNEBl	MVnEUXNQ	M4TkSmlvcGmkaYTzJINmdGxiZ4Lve5Rp	MknBNlUxOjZ{OUK=
BON-1	MnPRSpVv[3Srb36gRZN{[Xl?	M4fvfVUxOCCwTR?=	NW[5N\|hmPCCq	MknGSG1UVw>?	NInWWpBKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez	MUeyOVAzPjJ7Mh?=
QGP-1	M{HndmZ2dmO2aX;uJGF{e2G7	NIjTPFA2ODBibl2=	M3G1T\|QhcA>?	NWDTfXJCTE2VTx?=	NGXyV\|hKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez	Ml7yNlUxOjZ{OUK=
Huh7	Ml7SSpVv[3Srb36gRZN{[Xl?	M3zZN\|Eh\|ryP	MkPrNUBp	NWjzO2dKTE2VTx?=	NVLzVYlsUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S=	M{X0dlI2ODB2NECz
BNL	MnjTSpVv[3Srb36gRZN{[Xl?	MX[xJO69VQ>?	NXfuUFh3OSCq	MlfESG1UVw>?	NVvyTVVSUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4	M333TlI2ODB2NECz
MDA-MB-175	NUfIVoVCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXuxJO69VQ>?	NV7I[mJXPSCm	MmO1SG1UVw>?	NX\2OpRvUUN3MEyxJO69VQ>?	MVqyOFg4QTd7Nh?=
MDA-MB-134	M2nFcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWrK[4JpOSEQvF2=	Mn3JOUBl	MXXEUXNQ	Ml36TWM2ODxzIN88US=>	M1T1SFI1QDd7N{m2
HCC1500	NFLyOYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1nXPVEh\|ryP	NYS5WI5GPSCm	MXLEUXNQ	MlfQTWM2ODxzIN88US=>	NFLWS2ozPDh5OUe5Oi=>
EFM-19	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV;JPHdiOSEQvF2=	M3\2XlUh\A>?	NW[2NHdrTE2VTx?=	M{jvTWlEPTB:MTFOwG0>	NHfrepgzPDh5OUe5Oi=>
ZR-75-30	NGjqWW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFHKe\|AyKM7:TR?=	MWW1JIQ>	NYTDPXdPTE2VTx?=	MkXzTWM2ODxzIN88US=>	Mk\kNlQ5Pzl5OU[=
MDA-MB-361	NUfqfWtUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{O4V\|Eh\|ryP	MY[1JIQ>	M1nuT2ROW09?	Mof5TWM2ODxzIN88US=>	Mnq3NlQ5Pzl5OU[=
T-47D	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1nlZ\|Eh\|ryP	Mon5OUBl	MWHEUXNQ	MnzHTWM2ODxzIN88US=>	MoW2NlQ5Pzl5OU[=
SK-BR-3	MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoL1NUDPxE1?	M2e0RlUh\A>?	NGDQSnBFVVOR	NInwVmpKSzVyPEGg{txO	MoPwNlQ5Pzl5OU[=
UACC-732	Ml70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUexJO69VQ>?	MlPmOUBl	NXLjcll5TE2VTx?=	MV7JR\|UxRDFizszN	M3zPWVI1QDd7N{m2
BT-474	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXLmZ2o6OSEQvF2=	MWe1JIQ>	MWrEUXNQ	MV;JR\|UxRDFizszN	MmTSNlQ5Pzl5OU[=
HCC202	NUHxVXVFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnKzNUDPxE1?	NFPoOZQ2KGR?	M2DoTGROW09?	Mk\0TWM2ODxzIN88US=>	NHfzVY4zPDh5OUe5Oi=>
MCF7	NF:zSYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVfvbo5oOSEQvF2=	M4j4RVUh\A>?	MYjEUXNQ	M4XlfmlEPTB:MTFOwG0>	NHniPVQzPDh5OUe5Oi=>
MDA-MB-415	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXXtRol{OSEQvF2=	NEfVRVQ2KGR?	MkXSSG1UVw>?	NV23WmFrUUN3MEyxJO69VQ>?	M325ZlI1QDd7N{m2
MDA-MB-453	NVXpTW83T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnfPNUDPxE1?	NVO5V5BLPSCm	MkHvSG1UVw>?	NYf1VHlqUUN3MEyxJO69VQ>?	MoHHNlQ5Pzl5OU[=
ZR-75-1	NW\JbYl{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4nwe\|Eh\|ryP	Mn20OUBl	MlTiSG1UVw>?	NH;TZmhKSzVyPEGg{txO	MkTpNlQ5Pzl5OU[=
HCC38	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnLMNUDPxE1?	NV;iW4lbPSCm	M33aSWROW09?	NWrJboxmUUN3MEyxJO69VQ>?	MUWyOFg4QTd7Nh?=
HCC1419	NF3RflhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYXEZYE{OSEQvF2=	M4KzRVUh\A>?	MWXEUXNQ	Mn;zTWM2ODxzIN88US=>	NV;FVItmOjR6N{m3PVY>
UACC-812	NHHVS\|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4\iRlEh\|ryP	M2DDelUh\A>?	MoDLSG1UVw>?	MlXmTWM2ODxzIN88US=>	Mnf4NlQ5Pzl5OU[=
HCC1187	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4TNbFEh\|ryP	MX:1JIQ>	MXrEUXNQ	NFy3WWxKSzVyPEGg{txO	MVeyOFg4QTd7Nh?=
KPL-1	MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXqxJO69VQ>?	MUK1JIQ>	M17UV2ROW09?	NYLz[246UUN3MEyxJO69VQ>?	M1i0U\|I1QDd7N{m2
SUM-225	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYDOcoZzOSEQvF2=	M13DXVUh\A>?	NHXjNIxFVVOR	MXzJR\|UxRDFizszN	M3u1O\|I1QDd7N{m2
EFM-192A	MmfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmTwNUDPxE1?	Ml7OOUBl	NIH4eIJFVVOR	M3LwWWlEPTB:MTFOwG0>	M{T1cFI1QDd7N{m2
JIMT-1	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{\O[FEh\|ryP	NWXIUoZQPSCm	NXnVOIgyTE2VTx?=	M3jIcmlEPTB:MTFOwG0>	MV:yOFg4QTd7Nh?=
HCC1143	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnHiNUDPxE1?	MkjtOUBl	MUPEUXNQ	M3e3NmlEPTB:MTFOwG0>	NIXUPVczPDh5OUe5Oi=>
HCC2218	NXzRZ2R4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4WwcVEh\|ryP	M2HDeFUh\A>?	NVHyOHl5TE2VTx?=	NHXBVYJKSzVyPEGg{txO	MVSyOFg4QTd7Nh?=
MDA-MB-468	NFj5Tm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXuxJO69VQ>?	NFfHRnY2KGR?	M4XCUWROW09?	NW\scG5NUUN3MEyxJO69VQ>?	M4XYPVI1QDd7N{m2
BT-20	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mnj0NUDPxE1?	NGPRRZY2KGR?	M2G3WmROW09?	M4jP[mlEPTB:MTFOwG0>	MVKyOFg4QTd7Nh?=
MDA-MB-435	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGnOc4UyKM7:TR?=	M{Xoc\|Uh\A>?	NVG3eJNOTE2VTx?=	NILIe21KSzVyPEGg{txO	MonjNlQ5Pzl5OU[=
BT-549	NGjzW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVGxJO69VQ>?	M1HqXlUh\A>?	NXLoXnM3TE2VTx?=	NFKzUWVKSzVyPEGg{txO	NVLDOm1rOjR6N{m3PVY>
HCC1806	M2DLNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXz6WG1QOSEQvF2=	NH3ndHg2KGR?	NULvc2JZTE2VTx?=	MV7JR\|UxRDFizszN	NFOwRpEzPDh5OUe5Oi=>
HCC1937	NFTRbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXixJO69VQ>?	NV3nSHNVPSCm	Mn7iSG1UVw>?	NWXoSYZHUUN3MEyxJO69VQ>?	NXL4Vo1ZOjR6N{m3PVY>
Hs578T	M2DlV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmLYNUDPxE1?	M4SzeVUh\A>?	NGTvTlhFVVOR	M364SmlEPTB:MTFOwG0>	M4P3eVI1QDd7N{m2
LN18	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVP1PJpoOjBizszN	Mli4O\|IhcA>?	NXL2TpNXTE2VTx?=	NH[4ZmdKSzVyPEWg{txO	NXewR3p1OjR5NEGwO\|Q>
LN229	NEjadGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmXYNlAh\|ryP	MXK3NkBp	M3fGbGROW09?	MnTtTWM2ODx3IN88US=>	MUiyOFc1OTB5NB?=
LNZ308	NI\xdnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVqyNEDPxE1?	M1zpNFczKGh?	MVjEUXNQ	M{fnVmlEPTB:NTFOwG0>	NYHiUWdlOjR5NEGwO\|Q>
T98G	NED4bHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXnyOG11OjBizszN	NEXwd3Y4OiCq	MlXFSG1UVw>?	MWrJR\|UxRDVizszN	MmLzNlQ4PDFyN{S=
U87	M2rCVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXvWNVl3OjBizszN	NHfzdlM4OiCq	M4PEPWROW09?	NYK4XZN2UUN3MEy1JO69VQ>?	MoOxNlQ4PDFyN{S=
LN18	NEnPbIJHfW6ldHnvckBCe3OjeR?=	MUi1JO69VQ>?	MnTXNlQhcA>?	M1TGUGROW09?	MYnJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV	NVLycIZkOjR5NEGwO\|Q>
LNZ308	NYDaW3lxTnWwY4Tpc44hSXO\|YYm=	NUjq[Y9WPSEQvF2=	M1m5WlI1KGh?	NWnwT4hzTE2VTx?=	M1;N[WlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R?	MVGyOFc1OTB5NB?=
Saos-2	MY\GeY5kfGmxbjDBd5NigQ>?	MW[1NEDPxE1?	MmexOFghcA>?		NInJdFlKdmirYnn0d{Bk\WyuIHnueoF{cW:w	MW[yOFczPzZ4MB?=
MG-63	M1LjW2Z2dmO2aX;uJGF{e2G7	NEK3SWk2OCEQvF2=	Mlr2OFghcA>?		NHvLWpVKdmirYnn0d{Bk\WyuIHnueoF{cW:w	NYnSTZYzOjR5Mke2OlA>
SJSA-1	Mny2SpVv[3Srb36gRZN{[Xl?	NVLyT5BPPTBizszN	MWC0PEBp		MYfJcohq[mm2czDj[YxtKGmwdnHzbY9v	M1LBU\|I1PzJ5Nk[w
Saos-2	MnX3SpVv[3Srb36gRZN{[Xl?	M3XBN\|UxKM7:TR?=	MW[0PEBp		M{ThNGlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG\|ZT2yJIV5eHKnc4Ppc44>	MoHVNlQ4Ojd4NkC=
MG-63	MVHGeY5kfGmxbjDBd5NigQ>?	M3HxWVUxKM7:TR?=	M175NFQ5KGh?		MXXJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	NWjy[W9jOjR5Mke2OlA>
SJSA-1	M33RbWZ2dmO2aX;uJGF{e2G7	NYXNXndRPTBizszN	NI\6Wok1QCCq		MlvKTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW\|c3nvci=>	M4\IRlI1PzJ5Nk[w
Saos-2	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV;JfnA2PTBizszN	M{ftUlQ5KGh?		M3LofWlvcGmkaYTzJINmdGxidnnhZoltcXS7	MUmyOFczPzZ4MB?=
MG-63	MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIjNTGU2OCEQvF2=	MVq0PEBp		NUPzVJlZUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	NHXZSHIzPDd{N{[2NC=>
SJSA-1	MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGT2cVg2OCEQvF2=	NWTOSYMxPDhiaB?=		NYnkXHZUUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	Mn;oNlQ4Ojd4NkC=
FaDu	M3vkTWZ2dmO2aX;uJGF{e2G7	NVztfoRUPSEQvF2=	M1jTZ\|I1KGh?	NIW2dotFVVOR	NVvFOXJVWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	M1zoZ\|I1PjNzMUS3
EMT6	NGTPU5RHfW6ldHnvckBCe3OjeR?=	NFr6Z4U2KM7:TR?=	NGnzUFYzPCCq	MWPEUXNQ	Mn\6VoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36=	NYP4fWdiOjR4M{GxOFc>
HCT116	NUfmbm1kTnWwY4Tpc44hSXO\|YYm=	Moq1OUDPxE1?	NWLDZoh5OjRiaB?=	MkG1SG1UVw>?	NVjNOlRsWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	NFmxZnMzPDZ\|MUG0Oy=>
U87	NFjyS2FHfW6ldHnvckBCe3OjeR?=	MlexOUDPxE1?	NYW4bHlzOjRiaB?=	Ml3GSG1UVw>?	M1XwcXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	MYGyOFY{OTF2Nx?=
GBM	MnjrRZBweHSxc3nzJGF{e2G7	NInyT28z\|ryP	NXjsU2dHPDiq	NEKxUFJFVVOR	NFrHboVqdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6	M3LJ[FI1PTByNEmy
BON	MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUixMVXPxE1?	NWnZRY1uPzKq		NYDu[pFo\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>?	NGjKco4zPDR2M{WyNy=>
BON	MXXBdI9xfG:\|aYOgRZN{[Xl?	M2nWdlEuPc7:TR?=	Mmi0NlRp		NIO3TXFqdmO{ZXHz[ZMh[XCxcITvd4l{	NWPkUFZnOjR2NEO1NlM>
H1975	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3zPUlAvOy17LkdOwG0>	MUe3Nog>	MVHEUXNQ	MVjJR\|UxRTFwM{i1{txO	NXTDZ\|VJOjR\|M{e4OFY>
H1975	MWHBdI9xfG:\|aYOgRZN{[Xl?	NFvZOIYz\|ryP	NYjEcml2OjSq	NEKxdXZFVVOR	NWjMVHBicW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl?	MWeyOFM{Pzh2Nh?=
T-ALL	NV3XZXNnSXCxcITvd4l{KEG\|c3H5	M3:z[oJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?=	NFLUbo8zPCCxcjC0PIg>	MkfDSG1UVw>?	NYexZW1i[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM>	M4XjRVI1OzFyN{O2
BCR-ABL	M3P2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlvxNE4zPS1zMN88US=>	NUG0PZlSPGR?		M3f1e5Nq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25?	MlPFNlQzPDR4MUK=
LC-1/SQSF	M2\tV2Z2dmO2aX;uJGF{e2G7	MmnWN:69VQ>?	MorpNlRp	M3PzdWROW09?	M3TjUIRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=>	MVqyN\|k5ODB7Mx?=
Primary CLL cells	MXnBdI9xfG:\|aYOgRZN{[Xl?	NXPPXXZOOS1zMN88US=>	NV\kRWlCPDiq		MVTpcoR2[2W\|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz	MVSyN\|g2ODhyNx?=
Primary CLL cells	NH;jTXNMcW6jc3WgRZN{[Xl?	NFjqe44z\|ryP	MU[zNI1qdg>?		Mlvm[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl?	MlXJNlM5PTB6MEe=
Primary CLL cells	MX7DfZRwfG:6aXOgRZN{[Xl?	NVH5bnA1Os7:TR?=	MoCzNlRp		M3H0WIlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm=	M2S4ZVI{QDVyOEC3
human NSCLC cell lines	NW\Ke5p{SXCxcITvd4l{KEG\|c3H5	NYTjcYtQOC5zMkWtOO69VQ>?	Ml7hNlRp	MmfwSG1UVw>?	M1qxRmlEPTC\|IILhcodmeyCocn;tJFAvPC1{zszN	NYrZWZRKOjN3NkK0O\|I>
human HCC cell lines	NUDZZoFJS2WubDD2bYFjcWyrdImgZZN{[Xl?	MXGwMlAxPS1zzszN	MXi0PIg>		M4PSdWlEPTB;Md88US=>	M37yV\|I{PDh7OUm5
Huh7	MUnLbY5ie2ViQYPzZZk>	M1mweVHPxE1?	M{HEOlQ5cA>?		M2ewZpNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=>	NXfyR\|hYOjN2OEm5PVk>
SK-HEP1	NITqXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHTaXlIyNTJyzszN	MXe3Nog>	NGfNV\|RFVVOR	NH;TOYFKSzVy78{cNe69VQ>?	NFrJOIozOzR5OUGzOi=>
786-0	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mn3RNU0zOM7:TR?=	MU[3Nog>	MUPEUXNQ	MlfhTWM2OO,:nEJOwG0>	Mo\GNlM1PzlzM{[=
JVM2	NU[wO5FmS3m2b4TvfIlkcXS7IHHzd4F6	MlXmNE4zNTJyzszN	MVe3Nog>	MlnQSG1UVw>?	NITWW\|VKSzVyPUCuPe69VQ>?	NUDvOIJLOjN{M{i2N\|k>
EHEB	MX\DfZRwfG:6aXPpeJkh[XO\|YYm=	NH\0d3IxNjJvMkFOwG0>	MW[3Nog>	MlTuSG1UVw>?	M2LRdGlEPTB;MD63{txO	NWnPU\|BIOjN{M{i2N\|k>
MEC2	MUXDfZRwfG:6aXPpeJkh[XO\|YYm=	NXnLcpc4OC5{LUKw{txO	NHjBUVE4Omh?	NVe1fnZWTE2VTx?=	MYTJR\|UxRTBwN988US=>	MYeyN\|I{QDZ\|OR?=
primary B-CLL lymphocytes	MXXBdI9xfG:\|aYOgRZN{[Xl?	NYDHRZc5UUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?=	M1L5TFI1cA>?	MkDvSG1UVw>?	MlT0TWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=>	M{fkRVI{OjN6NkO5
primary B-CLL lymphocytes	MXTLbY5ie2ViQYPzZZk>	NWT5VWQ4UUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?=	NIfSO4QzPGh?		M1jsfolvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO\|aX;u	M3LDSFI{OjN6NkO5
human NSCLC	MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NUnRRWVyOC53LUNOwG0>	NHuyOXI4Omh?		NXzpOWNkUUN3ME2x{txO	MYCyNlc5OTN7Mx?=
human NSCLC	M2TycmtqdmG\|ZTDBd5NigQ>?	M3nXVVHPxE1?	M2LweVI1cA>?		M{fmcIlvcGmkaYTzJJRp\SCDa4SvcXRQWiC\|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS=	NVvMflJiOjJ5OEGzPVM>
Y1 cell line	M1TIUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlvGNE4y\|ryPL{JOwG0>	Mn6wNlRp	NUPBeWxOTE2VTx?=	MWDpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>?	NWDr[JNZOjJ4OUK5NFQ>
PIK3CA-mutant MCF7	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVHHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO\|NvVQ>?	NUf1eXM6PzKq		M2SyWmdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P	NIjifo8zOjZ3M{m2Oy=>
PIK3CA-mutant MCF7	MXjLbY5ie2ViQYPzZZk>	NYjhdHhyUUN3ME2xNVTDuTOwTR?=	M{nsV\|czcA>?		Mnq2TWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?=	M3j4dFIzPjV\|OU[3
MCF7-myr-Akt	NVz5eYZUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEnXdHFIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?=	Mo\qO\|Jp		NVjvboVXT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2=	NHey[2UzOjZ3M{m2Oy=>
colon cancer cell lines	NG\jTo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGDmU3IxNTFyzszN	Mmj6O\|Jp	MmHWSG1UVw>?	MY\JR\|UxRTIQvF2=	MVmyNlU1Ozh3Nx?=
gastric cancer cell lines	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXrzU5F1OC1zMN88US=>	MWO3Nog>	NXzsZmJoTE2VTx?=	NGriUmdKSzVyPUKtOe69VQ>?	MoHPNlI2PDN6NUe=
HCT-116/HT-29/MKN-45	M1:xPGFxd3C2b4Ppd{BCe3OjeR?=	MVGy{txO	Ml\oOFhp		NVzLPXhye2irZoSgbY4hTzJicHjhd4U>	M3Ts[VIzPTR\|OEW3
HT-29 and HCT-116	MmTsR4F{eGG\|ZTDhd5NigQ>?	MXu1{txO	NYrBToMzOjSq		NIT6fmVqdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm=	M{njPVIzPTR\|OEW3
MM cell lines	M3PpSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MonvNVDPxE1?	MmXXNlRp	MWjEUXNQ	M3vmcGlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>?	M3O3VVIzOjB5NEi1
ARP-1	NF2yc5pCeG:ydH;zbZMhSXO\|YYm=	NYfhNotHOTEQvF2=	NULLO3BoOjSq	MX;EUXNQ	M4LEbolv\HWlZYOgUW0h[2WubDDhdI9xfG:\|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36=	MVGyNlIxPzR6NR?=
SNU-601	M17JeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M2i0ZVczcA>?	NYTDT2Z{TE2VTx?=	NX73NZY3UUN3ME2wMlgyPsLzMD6wOlPPxE1?	MkDpNlIyPTl6MUS=
SNU-1	M1HpOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NIe5cJA4Omh?	Ml7PSG1UVw>?	M{XNOGlEPTB;MT6wPFLDuTBwMEK4{txO	NV3kcnp4OjJzNUm4NVQ>
SNU-668	M3Lhe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NE\sd2M4Omh?	NHvZ[3lFVVOR	MlPMTWM2OD1zLkW3PeKyOC5yN{VOwG0>	NIm5SnkzOjF3OUixOC=>
AGS	NYO3c2NjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MYW3Nog>	MonHSG1UVw>?	Moe0TWM2OD1zLkexOOKyOC5zMUhOwG0>	M1zEflIzOTV7OEG0
SNU-216	NVLwVWw5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MnjXO\|Jp	NYXNdoVVTE2VTx?=	NHr5V2tKSzVyPUKuOlkzyrFyLkC4Nu69VQ>?	MWSyNlE2QThzNB?=
SNU-5	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NWK0TIg4PzKq	NGrib3BFVVOR	M3LKeGlEPTB;MT6zOVHDuTBwMEmx{txO	NXrVO\|Z1OjJzNUm4NVQ>
SNU-638	MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MWC3Nog>	NVnKN5A3TE2VTx?=	NVL3NnZbUUN3ME2yMlI5OsLzMD6wOVPPxE1?	MorvNlIyPTl6MUS=
SNU-16	NHfqZ\|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NEnENGs4Omh?	M4LI[2ROW09?	Ml7RTWM2OD1zLkW3N:KyOC5yMEJOwG0>	NILVPHUzOjF3OUixOC=>
SNU-484	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NV3PSHdxPzKq	MUXEUXNQ	NWWxeZZtUUN3ME2xMlczQMLzMD6wOFXPxE1?	MnrqNlIyPTl6MUS=
SNU-620	M{DqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NUnJXIhvPzKq	MULEUXNQ	NHLzVYpKSzVyPUKuPVM6yrFyLkCwNe69VQ>?	NInJXnQzOjF3OUixOC=>
SNU-719	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MVS3Nog>	NYPGcXZKTE2VTx?=	NGW2c4xKSzVyPUOuNFM4yrFyLkCzNu69VQ>?	MY[yNlE2QThzNB?=
glioma cell lines	NXf2Z25LT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWK3Nog>		NVrvSJRzUUN3ME2xMVLPxE1?	M1vOfFIzODZ3MEiw
U87	NH3XbVVCeG:ydH;zbZMhSXO\|YYm=	NHvpbIUz\|ryP	MX:3Nog>		MYTpcoR2[2W\|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?=	MlniNlIxPjVyOEC=

... 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. Formulation: In 15% Captisol. 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

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
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
NCT01953445	Withdrawn	Drug: paclitaxel\|Drug: BKM120	Breast Neoplasms	Washington University School of Medicine	August 2014	Phase 2

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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

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.

Related PI3K Products

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Taselisib (GDC 0032) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with K_i of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

Features:A beta isoform-sparing PI3K inhibitor.
Pilaralisib (XL147) ^New

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.
GNE-317 ^New

GNE-317 is a potent, brain-penetrant PI3K inhibitor.
LY294002

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family.
3-Methyladenine (3-MA)

3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions of 3-MA are best fresh-prepared by heating.
Idelalisib (CAL-101, GS-1101)

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.
Dactolisib (BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3^TopBP1-ER cell.
Pictilisib (GDC-0941)

Pictilisib (GDC-0941) 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). 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)