Buparlisib (BKM120, NVP-BKM120)

Catalog No.S2247

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.

Cited by 78 Publications

Science, 2019, 364(6441)

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

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Nat Med, 2015, 10.1038/nm.3855

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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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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):2910

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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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Mol Ther Oncolytics, 2019, 13:58-66

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

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Nat Commun, 2018, 9(1):4550

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

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

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

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

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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

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

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

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

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

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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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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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Sci Rep, 2016, 6:20189

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J Clin Invest, 2015, 10.1172/JCI78018

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

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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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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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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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Oncogene, 2013, 10.1038/onc.2013.509

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

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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	MXvDfZRwfG:6aXOgRZN{[Xl?		M4Tq[VczKGh?	NYDOR\|JbTE2VTx?=	MknIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?=	MVOyOFkxODJ4Nh?=
DU145	NHvHTGREgXSxdH;4bYMhSXO\|YYm=		NFK4fXU4OiCq	NX\V[mhYTE2VTx?=	NGjXU5BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2=	MlixNlQ6ODB{Nk[=
A2780	MoToR5l1d3SxeHnjJGF{e2G7		MVq3NkBp	MnrtSG1UVw>?	MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N\|Uh\|ryP	M2q5PVI1QTByMk[2
U87MG	MXHDfZRwfG:6aXOgRZN{[Xl?		MkPyO\|IhcA>?	NX\xc3ZpTE2VTx?=	NILCTlhEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN	NGj1UIMzPDlyMEK2Oi=>
A2780	NUXaTplkTnWwY4Tpc44hSXO\|YYm=		MUWxJIg>	M2myVmROW09?	NGPIW29KdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR\|UxKG:oIECuNFU2KM7:TR?=	MV[yOFkxODJ4Nh?=
DU145	MVXGeY5kfGmxbjDBd5NigQ>?		M{K4SFEhcA>?	MVfEUXNQ	MXfJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>?	NXvveVVsOjR7MECyOlY>
A2780	M1TnNWZ2dmO2aX;uJGF{e2G7		MV:xJIg>	MXHEUXNQ	NHnXWnRKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDFR\|UxKG:oIECuNFc1KM7:TR?=	MVWyOFkxODJ4Nh?=
MCF7	MXTGeY5kfGmxbjDBd5NigQ>?		NXLSZndROSCq	MU\EUXNQ	NFHqTlJKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR\|UxKG:oIECuNUDPxE1?	MXmyOFkxODJ4Nh?=
U87MG	MmfZSpVv[3Srb36gRZN{[Xl?		NX;ne4ZIOSCq	NYDVOmhuTE2VTx?=	MkPhTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJIlvKFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiRVO1NEBw\iByLkGzJO69VQ>?	MV:yOFkxODJ4Nh?=
A2780	NIPLPVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mn;TO\|IhcA>?	MXzEUXNQ	MmrhSWM2OD1yLkWyJO69VQ>?	NX20VIs{OjR7MECyOlY>
SKMES-1	MWTDfZRwfG:6aXOgRZN{[Xl?	M1nKdFEh\|ryP	NIfzUVc4OiCq		NWfIb45tUW6mdXPld{Bk\WyuIHTlZZRp	NIT0VnEzPjBzM{OxPC=>
H596	MnLvSpVv[3Srb36gRZN{[Xl?	NYPZVIlKOSEQvF2=			NGT0V4JKdXCjaYLzJINmdGxibXnndoF1cW:w	NF;rOZAzPjBzM{OxPC=>
HCC2450	NXTjXYRHTnWwY4Tpc44hSXO\|YYm=	NFv6R3cyKM7:TR?=			MmfiTY1x[Wm{czDj[YxtKGmwdnHzbY9v	M4WzWVI3ODF\|M{G4
A549	Ml\DSpVv[3Srb36gRZN{[Xl?	M{nLb\|UxOCCwTR?=	M3:4eVQ5KGh?	MlTLSG1UVw>?	NWKxVIl5UW6qaXLpeJMhSWu2IHHjeIl3[XSrb36=	MmO5NlU6Ozd{OUm=
A549	NYrHOIRIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV\nNm12OSEQvF2=	MnvOO\|IhcA>?	NFO5XnJFVVOR	MojSTY5pcWKrdIOgZ4VtdCCpcn;3eIg>	MonDNlU6Ozd{OUm=
H522	MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2PI[FEh\|ryP	NFzJ[5g4OiCq	NXHUNphNTE2VTx?=	Mk[xTY5pcWKrdIOgZ4VtdCCpcn;3eIg>	M2iyU\|I2QTN5Mkm5
LNCaP	M{X0W2Z2dmO2aX;uJGF{e2G7	MYixJO69VQ>?			NFjhbIRUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?=	MUGyOVM3ODd7OR?=
LNCaP95	NYjMdZBuTnWwY4Tpc44hSXO\|YYm=	MWCxJO69VQ>?			MX;TeZBxemW\|c3XzJJAuSUuWIHzleoVtew>?	M{fOelI2OzZyN{m5
HCT-15	NImzZZVCeG:2b4Ppd{BCe3OjeR?=	MmjFNVAh\|ryP	MlzlOFghcA>?	MkCySG1UVw>?	MWHJcoR2[2W\|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	MmK4NlUyPTJ{NEW=
HCT-116	M1[ySmFxd3Sxc3nzJGF{e2G7	NHSwU\|AyOCEQvF2=	MVO0PEBp	MlzsSG1UVw>?	MnfkTY5lfWOnczDhdI9xfG:\|aYOgbY4hUEOWLUGxOkBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	NIPqUpczPTF3MkK0OS=>
NCI-H460	M2LVNmFxd3Sxc3nzJGF{e2G7	MnfrNVAh\|ryP	MmnlOFghcA>?	NH;xdoRFVVOR	NHXUXopKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCQQ1mtTFQ3OCClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S\|cH;0JI12fGG2aX;u	NYP3RopUOjVzNUKyOFU>
SKOV-3	NG[wZVNCeG:2b4Ppd{BCe3OjeR?=	NGi3R3AyOCEQvF2=	MX:0PEBp	MoTrSG1UVw>?	MX;JcoR2[2W\|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	NWe0R5RPOjVzNUKyOFU>
BSY-1	NGn4c5BCeG:2b4Ppd{BCe3OjeR?=	NEHy[lUyOCEQvF2=	NX\m[4M5PDhiaB?=	NE\PZnBFVVOR	MnO3TY5lfWOnczDhdI9xfG:\|aYOgbY4hSlO\LUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	MUiyOVE2OjJ2NR?=
MKN-1	NFvjUJdCeG:2b4Ppd{BCe3OjeR?=	NEDLT4MyOCEQvF2=	NHTabFY1QCCq	M3zQWmROW09?	NFzoeFBKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	M4DqdlI2OTV{MkS1
NCI-H522	NEHB[WRCeG:2b4Ppd{BCe3OjeR?=	NHLXdIkyOCEQvF2=	NW\NdFM{PDhiaB?=	NHzOdJZFVVOR	NUWxW\|c{UW6mdXPld{BieG:ydH;zbZM>	MoGzNlUyPTJ{NEW=
OVCAR-3	MVrBdI91d3OrczDBd5NigQ>?	Mk\zNVAh\|ryP	Ml:yOFghcA>?	M2DZdGROW09?	NHjsNm5KdmS3Y3XzJIFxd3C2b4Ppdy=>	MmC5NlUyPTJ{NEW=
HBC-5	NXTrNJhrSXCxdH;zbZMhSXO\|YYm=	MX[xNEDPxE1?	M3uzUlQ5KGh?	NWT5c5BCTE2VTx?=	M2fifWlv\HWlZYOgZZBweHSxc3nz	M3fNT\|I2OTV{MkS1
RXF-631L	NIXwXHRCeG:2b4Ppd{BCe3OjeR?=	NUPvenNQOTBizszN	M4PVNlQ5KGh?	MWjEUXNQ	NWT6cXlHUW6mdXPld{BieG:ydH;zbZM>	M3yxUlI2OTV{MkS1
MKN-45	NX32cIVCSXCxdH;zbZMhSXO\|YYm=	MoW1NVAh\|ryP	NHjJWHU1QCCq	M{\sdGROW09?	MV\JcoR2[2W\|IHHwc5B1d3Orcx?=	M2rvXFI2OTV{MkS1
BON-1	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MljvOVAxKG6P	MVuxNEBl	MV\EUXNQ	NVnmT3EzUW6qaXLpeJMh[2WubDDndo94fGh?	MWKyOVAzPjJ7Mh?=
BON-1	NU\6fIhOTnWwY4Tpc44hSXO\|YYm=	NYj1eVlUPTByIH7N	NEDTSmw1KGh?	Ml;FSG1UVw>?	M3j2eGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O=	MUSyOVAzPjJ7Mh?=
QGP-1	MoPKSpVv[3Srb36gRZN{[Xl?	NX7WOmJDPTByIH7N	MWi0JIg>	NGntOFVFVVOR	NFPHV49KdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez	Mlf1NlUxOjZ{OUK=
Huh7	NHu2WWhHfW6ldHnvckBCe3OjeR?=	NUHscnZiOSEQvF2=	NVXy[FR4OSCq	M1\RVmROW09?	MlTBTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR?	MmewNlUxODR2MEO=
BNL	MkjMSpVv[3Srb36gRZN{[Xl?	NUjoWWxbOSEQvF2=	NF;nZVIyKGh?	MX\EUXNQ	NFr0OGxKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhWzZ?	M2DyPFI2ODB2NECz
MDA-MB-175	NGn4fIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlPUNUDPxE1?	M2qwfFUh\A>?	MmL2SG1UVw>?	NFHjRoRKSzVyPEGg{txO	NEizemQzPDh5OUe5Oi=>
MDA-MB-134	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV\jXG5ZOSEQvF2=	MWO1JIQ>	NGXlSINFVVOR	NGPvPW5KSzVyPEGg{txO	NISxVJIzPDh5OUe5Oi=>
HCC1500	M4HnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1vkOFEh\|ryP	NGn4bmU2KGR?	NGnWeoZFVVOR	NXq3XoFEUUN3MEyxJO69VQ>?	NHvOcpIzPDh5OUe5Oi=>
EFM-19	Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NYTP[oFLOSEQvF2=	NHrDUXY2KGR?	MmPKSG1UVw>?	NV\jTpdIUUN3MEyxJO69VQ>?	NFjMfnozPDh5OUe5Oi=>
ZR-75-30	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYGxJO69VQ>?	MWi1JIQ>	Mn3rSG1UVw>?	M4W5[mlEPTB:MTFOwG0>	MmnpNlQ5Pzl5OU[=
MDA-MB-361	NEn1WnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NF7xS2MyKM7:TR?=	NYrrSFN6PSCm	M3X0d2ROW09?	NGnIbJBKSzVyPEGg{txO	NGr2UXYzPDh5OUe5Oi=>
T-47D	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXLKVFNPOSEQvF2=	MXK1JIQ>	NYTxdnZTTE2VTx?=	MY\JR\|UxRDFizszN	NHrtUoozPDh5OUe5Oi=>
SK-BR-3	NXLrOY85T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{XYb\|Eh\|ryP	MmXOOUBl	MYTEUXNQ	M4TmN2lEPTB:MTFOwG0>	NV\IW5BzOjR6N{m3PVY>
UACC-732	NF\scW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3nwSVEh\|ryP	NXHCfGhCPSCm	MVHEUXNQ	NFLSN3NKSzVyPEGg{txO	MVqyOFg4QTd7Nh?=
BT-474	M2ruXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGrMV\|QyKM7:TR?=	NVLjcpljPSCm	MmqwSG1UVw>?	MoPMTWM2ODxzIN88US=>	MnP6NlQ5Pzl5OU[=
HCC202	Mn2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2qwXFEh\|ryP	MYm1JIQ>	MXnEUXNQ	NYDNT\|RoUUN3MEyxJO69VQ>?	M4i3eFI1QDd7N{m2
MCF7	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MV6xJO69VQ>?	M3zWTVUh\A>?	MljPSG1UVw>?	MVfJR\|UxRDFizszN	NXzkWGtSOjR6N{m3PVY>
MDA-MB-415	MkezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmPrNUDPxE1?	MX61JIQ>	NI\tVHpFVVOR	MV3JR\|UxRDFizszN	NVzmNnVkOjR6N{m3PVY>
MDA-MB-453	M{\UbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmDaNUDPxE1?	M{HPWFUh\A>?	MVrEUXNQ	MkLPTWM2ODxzIN88US=>	NGjUeo0zPDh5OUe5Oi=>
ZR-75-1	NVvReIdNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVXicYxkOSEQvF2=	M2\tRlUh\A>?	NWPrUXdHTE2VTx?=	M3u4O2lEPTB:MTFOwG0>	M33wW\|I1QDd7N{m2
HCC38	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGXhOIoyKM7:TR?=	MUO1JIQ>	MWfEUXNQ	NI\1c2pKSzVyPEGg{txO	MkPSNlQ5Pzl5OU[=
HCC1419	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlvVNUDPxE1?	MnXDOUBl	MUHEUXNQ	MkHpTWM2ODxzIN88US=>	MXqyOFg4QTd7Nh?=
UACC-812	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkH2NUDPxE1?	MoDXOUBl	NFf0eIhFVVOR	M{PKSmlEPTB:MTFOwG0>	NF7IOmYzPDh5OUe5Oi=>
HCC1187	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkLjNUDPxE1?	M4K4ZVUh\A>?	MmjTSG1UVw>?	M3rUZmlEPTB:MTFOwG0>	MX[yOFg4QTd7Nh?=
KPL-1	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mm\ENUDPxE1?	NUHi[29ZPSCm	NHPLblBFVVOR	NHPuUGdKSzVyPEGg{txO	NF:5ZW4zPDh5OUe5Oi=>
SUM-225	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWGxJO69VQ>?	MVm1JIQ>	MorWSG1UVw>?	M2LCemlEPTB:MTFOwG0>	Ml7WNlQ5Pzl5OU[=
EFM-192A	MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnrRNUDPxE1?	NGHFTVE2KGR?	NGn1ZYlFVVOR	M13QcGlEPTB:MTFOwG0>	MomzNlQ5Pzl5OU[=
JIMT-1	MoP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmnONUDPxE1?	MlXXOUBl	M4jLPGROW09?	M2LiV2lEPTB:MTFOwG0>	M3TyclI1QDd7N{m2
HCC1143	NFfmUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXWxJO69VQ>?	M4KzOlUh\A>?	M2W1c2ROW09?	MmC1TWM2ODxzIN88US=>	M4nQ[FI1QDd7N{m2
HCC2218	NV3ENFJDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYCxJO69VQ>?	M4D0XlUh\A>?	MXHEUXNQ	MXXJR\|UxRDFizszN	MlvvNlQ5Pzl5OU[=
MDA-MB-468	M2\kWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFrhRVEyKM7:TR?=	NEjhXVg2KGR?	MoXtSG1UVw>?	NHfTbGFKSzVyPEGg{txO	MWiyOFg4QTd7Nh?=
BT-20	MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHnBfnEyKM7:TR?=	MlK2OUBl	NED4S2hFVVOR	M3nQSGlEPTB:MTFOwG0>	NEDyU\|czPDh5OUe5Oi=>
MDA-MB-435	M3WxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWGxJO69VQ>?	NFvmNVU2KGR?	NH[0NGxFVVOR	M1nCUmlEPTB:MTFOwG0>	NXrx[Hp4OjR6N{m3PVY>
BT-549	MmfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NX;VPGJ5OSEQvF2=	MUS1JIQ>	MVrEUXNQ	MnfUTWM2ODxzIN88US=>	NV\FOnVKOjR6N{m3PVY>
HCC1806	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVHXXZZQOSEQvF2=	MojjOUBl	MmW1SG1UVw>?	NIC5cJhKSzVyPEGg{txO	MYCyOFg4QTd7Nh?=
HCC1937	NWPT[WJVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHvFd\|EyKM7:TR?=	M1Tv[\|Uh\A>?	NF;PfVJFVVOR	NF;oR\|dKSzVyPEGg{txO	NH3ITW4zPDh5OUe5Oi=>
Hs578T	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NELsNoMyKM7:TR?=	NVnCdI1EPSCm	NVf1OWlwTE2VTx?=	MV7JR\|UxRDFizszN	NVXhOGc2OjR6N{m3PVY>
LN18	NGK2R5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGfxTHMzOCEQvF2=	NF3UWpk4OiCq	MmrZSG1UVw>?	NX:5UmJJUUN3MEy1JO69VQ>?	Ml;ONlQ4PDFyN{S=
LN229	M{XiNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUDQOVQ6OjBizszN	M1fX[FczKGh?	MYrEUXNQ	NFvTNZlKSzVyPEWg{txO	Mk[zNlQ4PDFyN{S=
LNZ308	NXPVVpFYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWCyNEDPxE1?	M3;5[FczKGh?	M3PjfWROW09?	MnHkTWM2ODx3IN88US=>	NXTRWZRUOjR5NEGwO\|Q>
T98G	M1fCXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4fsfFIxKM7:TR?=	NGrLd5E4OiCq	NWX4bVNuTE2VTx?=	MULJR\|UxRDVizszN	Mn3aNlQ4PDFyN{S=
U87	NEjoOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV6yNEDPxE1?	M1e5c\|czKGh?	MWPEUXNQ	NXXz[YZHUUN3MEy1JO69VQ>?	MV6yOFc1OTB5NB?=
LN18	M33qTGZ2dmO2aX;uJGF{e2G7	MXq1JO69VQ>?	MWCyOEBp	NGTSRo9FVVOR	MYfJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV	NUHPc253OjR5NEGwO\|Q>
LNZ308	M4fCPWZ2dmO2aX;uJGF{e2G7	NEXBdXk2KM7:TR?=	NVzCb5NnOjRiaB?=	M2fKfWROW09?	M{jqV2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R?	MnjxNlQ4PDFyN{S=
Saos-2	MnPwSpVv[3Srb36gRZN{[Xl?	MoO0OVAh\|ryP	MkfEOFghcA>?		NHvabW9KdmirYnn0d{Bk\WyuIHnueoF{cW:w	NGH1PVAzPDd{N{[2NC=>
MG-63	MUHGeY5kfGmxbjDBd5NigQ>?	NGH1ZZc2OCEQvF2=	NX[xRm82PDhiaB?=		NVTxfI9bUW6qaXLpeJMh[2WubDDpcpZie2mxbh?=	Mn\uNlQ4Ojd4NkC=
SJSA-1	MU\GeY5kfGmxbjDBd5NigQ>?	NY\hdoxkPTBizszN	NHvncFE1QCCq		MmDaTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	Moq3NlQ4Ojd4NkC=
Saos-2	M2XIOWZ2dmO2aX;uJGF{e2G7	NH\UfnE2OCEQvF2=	NGrpSoQ1QCCq		M13Q[WlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG\|ZT2yJIV5eHKnc4Ppc44>	NFH0VZEzPDd{N{[2NC=>
MG-63	NHjydVdHfW6ldHnvckBCe3OjeR?=	NFmy[2Y2OCEQvF2=	M3vQelQ5KGh?		MWHJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	NXjJW\|FQOjR5Mke2OlA>
SJSA-1	NWO0eJdMTnWwY4Tpc44hSXO\|YYm=	NHHpcIc2OCEQvF2=	M1PnPFQ5KGh?		M1y2SWlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG\|ZT2yJIV5eHKnc4Ppc44>	MmPkNlQ4Ojd4NkC=
Saos-2	NX6xeVg4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2nicFUxKM7:TR?=	NUnZXI5oPDhiaB?=		NHrxSWRKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?=	NVnWblNHOjR5Mke2OlA>
MG-63	Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUC1NEDPxE1?	NYXqS3VHPDhiaB?=		MV;Jcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>?	M{TJ[FI1PzJ5Nk[w
SJSA-1	NHvldWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2fPSFUxKM7:TR?=	MVq0PEBp		NXjkWlNmUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	Ml;aNlQ4Ojd4NkC=
FaDu	NWfrZ\|BUTnWwY4Tpc44hSXO\|YYm=	NGHjUZo2KM7:TR?=	NEnCbnAzPCCq	M4PxVmROW09?	NGPycWFT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	MonNNlQ3OzFzNEe=
EMT6	NWTqd2xrTnWwY4Tpc44hSXO\|YYm=	NIW5U2U2KM7:TR?=	NUW3bnY3OjRiaB?=	M{PDfGROW09?	NXvT[2RvWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	MnrlNlQ3OzFzNEe=
HCT116	M{izWWZ2dmO2aX;uJGF{e2G7	MX[1JO69VQ>?	MoPTNlQhcA>?	M4jUNWROW09?	NEfxZ\|RT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	MnzmNlQ3OzFzNEe=
U87	NFjFT4lHfW6ldHnvckBCe3OjeR?=	Ml3lOUDPxE1?	NGjy[WUzPCCq	MV\EUXNQ	NXXrTFBzWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	M1XqZ\|I1PjNzMUS3
GBM	NEfk[XJCeG:ydH;zbZMhSXO\|YYm=	NXfNXplCOs7:TR?=	MVy0PIg>	NEHVelBFVVOR	MVfpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m\|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5	MWOyOFUxODR7Mh?=
BON	NHTMU4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4XvTVEuPc7:TR?=	M2PuOlczcA>?		NX30OFRH\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>?	MUSyOFQ1OzV{Mx?=
BON	NEe3fWtCeG:ydH;zbZMhSXO\|YYm=	M4TMS\|EuPc7:TR?=	Mke0NlRp		NYnVXFJucW6lcnXhd4V{KGGyb4D0c5Nqew>?	MXWyOFQ1OzV{Mx?=
H1975	NU\hUolrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkLqNE4{NTlwNt88US=>	MlPHO\|Jp	MWXEUXNQ	MWTJR\|UxRTFwM{i1{txO	Mki5NlQ{Ozd6NE[=
H1975	MnzkRZBweHSxc3nzJGF{e2G7	NFTne\|gz\|ryP	NYSwW5htOjSq	MVHEUXNQ	MWrpcoNz\WG\|ZYOgZZBweHSxc3nzJJJifGVic3nncolncWOjboTsfS=>	NHXuUGszPDN\|N{i0Oi=>
T-ALL	NV;CRo1lSXCxcITvd4l{KEG\|c3H5	MUni[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV?	NVvBd4xzOjRib4KgOFhp	NWrkSWQ4TE2VTx?=	M4jMNYFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz	M4HQd\|I1OzFyN{O2
BCR-ABL	MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUWwMlI2NTFyzszN	NF\SeWw1\A>?		MlH6d4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>?	MYCyOFI1PDZzMh?=
LC-1/SQSF	MlfJSpVv[3Srb36gRZN{[Xl?	NF\BZ20{\|ryP	NHW3b28zPGh?	NICwTpNFVVOR	MXnk[YNz\WG\|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy=	NVi3R3NYOjN7OECwPVM>
Primary CLL cells	NFPyWoFCeG:ydH;zbZMhSXO\|YYm=	NXLxeox4OS1zMN88US=>	MUS0PIg>		NH64XVVqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{	M4TqOFI{QDVyOEC3
Primary CLL cells	M1uwemtqdmG\|ZTDBd5NigQ>?	M3fz[FLPxE1?	NF7TPJM{OG2rbh?=		NXLuZXV6\GWlcnXhd4VlKFCLM1ugZYN1cX[rdIm=	MWeyN\|g2ODhyNx?=
Primary CLL cells	MWTDfZRwfG:6aXOgRZN{[Xl?	MnL1Nu69VQ>?	NWnOdYY5OjSq		MlPwbY5lfWOnczDj[YxtKGO7dH;0c5hq[2m2eR?=	NYiw[495OjN6NUC4NFc>
human NSCLC cell lines	NXfzcJRWSXCxcITvd4l{KEG\|c3H5	MmHwNE4yOjVvNN88US=>	MWeyOIg>	M4jJc2ROW09?	MVnJR\|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?=	M3\zb\|I{PTZ{NEey
human HCC cell lines	MkDPR4VtdCC4aXHibYxqfHliYYPzZZk>	NF;YPWMxNjByNT2x{txO	NV\PTWQ5PDiq		NUnK[5l{UUN3ME2x{txO	M1TtbVI{PDh7OUm5
Huh7	NWfBZXNSU2mwYYPlJGF{e2G7	M4LoZ\|HPxE1?	MVK0PIg>		Mn7td4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0	M{HMbVI{PDh7OUm5
SK-HEP1	MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIfPTIwyNTJyzszN	NF;tVFk4Omh?	MmT3SG1UVw>?	MnTFTWM2OO,:nEJOwG0>	MlL3NlM1PzlzM{[=
786-0	NH6xOGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NILNXG8yNTJyzszN	M4PRfFczcA>?	MlPFSG1UVw>?	MYDJR\|Ux97zeMd88US=>	NXnTOIRDOjN2N{mxN\|Y>
JVM2	NXvJWlNXS3m2b4TvfIlkcXS7IHHzd4F6	NIfq[mwxNjJvMkFOwG0>	MWG3Nog>	NXXMVJU2TE2VTx?=	MYfJR\|UxRTBwOd88US=>	NHjLNJAzOzJ\|OE[zPS=>
EHEB	MVLDfZRwfG:6aXPpeJkh[XO\|YYm=	NWLtVpR{OC5{LUKw{txO	MVO3Nog>	M4\oc2ROW09?	MYTJR\|UxRTBwN988US=>	Mly5NlMzOzh4M{m=
MEC2	M1jmU2N6fG:2b4jpZ4l1gSCjc4PhfS=>	NGPycZIxNjJvMkFOwG0>	NFTyOFU4Omh?	NYrUbW5kTE2VTx?=	M{OxWGlEPTB;MD63{txO	NULwXVhoOjN{M{i2N\|k>
primary B-CLL lymphocytes	M3;uVGFxd3C2b4Ppd{BCe3OjeR?=	M1jRemlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV?	NGm4emUzPGh?	NXS0XIZYTE2VTx?=	MWfJR\|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz	MYGyN\|I{QDZ\|OR?=
primary B-CLL lymphocytes	NGPlR4JMcW6jc3WgRZN{[Xl?	M2LDV2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV?	MXGyOIg>		M3LTeYlvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO\|aX;u	NXvtW2hPOjN{M{i2N\|k>
human NSCLC	MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXmwMlUuOs7:TR?=	MVK3Nog>		M{PX[2lEPTB;Md88US=>	MUGyNlc5OTN7Mx?=
human NSCLC	MojCT4lv[XOnIFHzd4F6	M1LHc\|HPxE1?	NGD3WFUzPGh?		MXnpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62	MWOyNlc5OTN7Mx?=
Y1 cell line	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1jtW\|AvOc7:TT:x{txO	NHX6cpUzPGh?	NH\CU3FFVVOR	NVLJR49QcW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO=	M4HhSFIzPjl{OUC0
PIK3CA-mutant MCF7	MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NILYOmFIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?=	MUS3Nog>		MljnS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	NEjLeZczOjZ3M{m2Oy=>
PIK3CA-mutant MCF7	Mkm3T4lv[XOnIFHzd4F6	MlXpTWM2OD1zMUVCtVNvVQ>?	NES5SJY4Omh?		NEXlOGxKSzVyPUGxOOKyO26PIHnuJJJm\HWlaX7nJGFsfCCyaH;zdIhwenmuYYTpc44hdGW4ZXzz	MoL5NlI3PTN7Nke=
MCF7-myr-Akt	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXjjW2ZRT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2=	MU[3Nog>		Ml7XS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1?	M1iyTVIzPjV\|OU[3
colon cancer cell lines	M4TaZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mom3NE0yOM7:TR?=	M1HwNVczcA>?	M{XKXGROW09?	NEnWbYJKSzVyPUJOwG0>	NWrQb2FWOjJ3NEO4OVc>
gastric cancer cell lines	NX[wTlkyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmDkNE0yOM7:TR?=	M3uwT\|czcA>?	MmXoSG1UVw>?	NXnCXoN6UUN3ME2yMVXPxE1?	MmjPNlI2PDN6NUe=
HCT-116/HT-29/MKN-45	MlPPRZBweHSxc3nzJGF{e2G7	M{XFVlLPxE1?	NULkUHpsPDiq		MU\zbIlnfCCrbjDHNkBxcGG\|ZR?=	M1L6fVIzPTR\|OEW3
HT-29 and HCT-116	NVnObnpUS2G\|cHHz[UBie3OjeR?=	M{ji[VXPxE1?	MYKyOIg>		M{Pq[Ylv\HWlZYOgZ4F{eGG\|ZTDhZ5Rqfmm2eR?=	NWTVT44zOjJ3NEO4OVc>
MM cell lines	M3r3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NITwNIsyOM7:TR?=	NEi1dngzPGh?	MYnEUXNQ	NHmxVFhKSzVyII\hdolmeyCjbX;u[{BlcW[oZYLlcpQh[2WubDDsbY5meyCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVv[2V?	NUjsb4xyOjJ{MEe0PFU>
ARP-1	NWjDPGpQSXCxcITvd4l{KEG\|c3H5	MkToNVDPxE1?	NVL3e5J3OjSq	NXvC[mZVTE2VTx?=	NYfUWFZZcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=>	MoTKNlIzODd2OEW=
SNU-601	NGrRcpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M1zW[VczcA>?	NYPs[IxFTE2VTx?=	M2TC[mlEPTB;MD64NVbDuTBwME[z{txO	NHLuW\|czOjF3OUixOC=>
SNU-1	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXrxZWZEPzKq	MoDnSG1UVw>?	MWXJR\|UxRTFwMEiyxtExNjB{ON88US=>	Mn7DNlIyPTl6MUS=
SNU-668	NWTt[Wg2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NXPVRpJYPzKq	MY\EUXNQ	NHjJNVVKSzVyPUGuOVc6yrFyLkC3OO69VQ>?	NWjyVIx4OjJzNUm4NVQ>
AGS	NYTudFVDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M4rMUFczcA>?	MWPEUXNQ	NUHhN4RjUUN3ME2xMlcyPMLzMD6xNVfPxE1?	MoPBNlIyPTl6MUS=
SNU-216	NWfoZlZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MV23Nog>	M2Pj[mROW09?	MUPJR\|UxRTJwNkmyxtExNjB6Mt88US=>	M2\HZ\|IzOTV7OEG0
SNU-5	NGfEeWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NXv3[oFoPzKq	M4\GWmROW09?	MWrJR\|UxRTFwM{WxxtExNjB7Md88US=>	NFXse3kzOjF3OUixOC=>
SNU-638	NUTLV5lST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NFX3cZM4Omh?	MnH1SG1UVw>?	MV;JR\|UxRTJwMkiyxtExNjB3M988US=>	MkO3NlIyPTl6MUS=
SNU-16	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MXu3Nog>	MVnEUXNQ	NITsTFJKSzVyPUGuOVc{yrFyLkCwNe69VQ>?	NFzjeokzOjF3OUixOC=>
SNU-484	NXn1R4k6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NULp[4xvPzKq	MVXEUXNQ	MlL1TWM2OD1zLkeyPOKyOC5yNEZOwG0>	MVqyNlE2QThzNB?=
SNU-620	NIf5OXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MmC2O\|Jp	M1;mRWROW09?	MX;JR\|UxRTJwOUO5xtExNjByMd88US=>	MV[yNlE2QThzNB?=
SNU-719	MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NULETI41PzKq	MYDEUXNQ	NV;aPVk6UUN3ME2zMlA{P8LzMD6wN\|LPxE1?	MWOyNlE2QThzNB?=
glioma cell lines	M4PrSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MXO3Nog>		MUDJR\|UxRTFvMt88US=>	NX3wbWVNOjJyNkWwPFA>
U87	M1vNXGFxd3C2b4Ppd{BCe3OjeR?=	MlzDNu69VQ>?	NXnoS\|Y5PzKq		MnS0bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO=	NHToSokzOjB4NUC4NC=>

... 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]	+ Expand 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]	+ Expand 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]	+ Expand 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.

+ Expand

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, NVP-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	N/A

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

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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PI3K Signaling Pathway Map

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Most Potent PI3K Inhibitor

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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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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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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)

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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, NVP-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.
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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, NVP-BKM120)

Cited by 78 Publications

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Solubility (25°C)

Chemical Information Download Buparlisib (BKM120, NVP-BKM120) SDF

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

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The Serial Dilution Calculator Equation

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Total Molecular Weight: g/mol

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

Molarity Calculator

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

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

Choose Your Country or Region

By Signaling Pathways

By product type

Buparlisib (BKM120, NVP-BKM120)

Cited by 78 Publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Buparlisib (BKM120, NVP-BKM120) SDF

Bio Calculators

Molarity Calculator

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

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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

Molarity Calculator

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

Tech Support

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

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