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 51 Publications

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

PubMed: 25913192 ( click the link to review the publication )

Nat Med, 2015, 10.1038/nm.3855

PubMed: 25939062 ( click the link to review the publication )

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

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

Science, 2019, 364(6441)

PubMed: 31097636 ( 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):2910

PubMed: 31266951 ( click the link to review the publication )

Mol Ther Oncolytics, 2019, 13:58-66

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

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

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

Leuk Lymphoma, 2019, 10.1080/10428194.2019.1594211

PubMed: 30947576 ( 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

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

PubMed: 29582409 ( 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 Ther, 2017, 10.1158/1535-7163

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

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

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

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

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

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

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

PLoS One, 2016, 10.1371/journal

PubMed: 27055253 ( click the link to review the publication )

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

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

J Clin Invest, 2015, 10.1172/JCI78018

PubMed: 25798617 ( click the link to review the publication )

Oncogene, 2015, 10.1038/onc.2015.173

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

Acta Pharmacol Sin, 2015, 10.1038/aps.2015.4

PubMed: 25864651 ( click the link to review the publication )
Exp Cell Res, 2015, 332(2):223-35

PubMed: 25704758 ( click the link to review the publication )

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

PubMed: ( click the link to review the publication )

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

PubMed: 25578563 ( click the link to review the publication )

PLoS One, 2015, 10(4):e0123410

PubMed: 25844720 ( click the link to review the publication )

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

PubMed: 25869396 ( click the link to review the publication )

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

PubMed: 25401474 ( click the link to review the publication )

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

PubMed: 25297634 ( click the link to review the publication )

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

PubMed: 25176649 ( click the link to review the publication )

Oncogene, 2014, 10.1038/onc.2014.328

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

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

PubMed: 24451154 ( click the link to review the publication )

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

PubMed: 25103565 ( click the link to review the publication )

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

PubMed: 25103565 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1134

PubMed: 24651437 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1013

PubMed: 24457957 ( click the link to review the publication )

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

PubMed: 25103499 ( click the link to review the publication )

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

PubMed: 24982421 ( click the link to review the publication )

PLoS One, 2014, 9(10):e108780

PubMed: 25360799 ( click the link to review the publication )

PLoS One, 2014, 9(7):e101969

PubMed: 25003333 ( click the link to review the publication )

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

PubMed: 25285632 ( click the link to review the publication )

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

PubMed: 24979463 ( click the link to review the publication )

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

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

Oncogene, 2013, 10.1038/onc.2013.509

PubMed: 24292683 ( click the link to review the publication )
Breast Cancer Res, 2013, 15(4):R55

PubMed: 23844554 ( click the link to review the publication )

BMC Cancer, 2013, 13:465

PubMed: 24103747 ( 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	M1flN2N6fG:2b4jpZ{BCe3OjeR?=		MYO3NkBp	MlT1SG1UVw>?	M3T6[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFiRUW0OWshdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFE2QCEQvF2=	NVTGb4pEOjR7MECyOlY>
DU145	MoLtR5l1d3SxeHnjJGF{e2G7		M3e0RVczKGh?	MYLEUXNQ	MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1?	NVP2[WRCOjR7MECyOlY>
A2780	NHziRWhEgXSxdH;4bYMhSXO\|YYm=		NXLKU5lZPzJiaB?=	MoDBSG1UVw>?	MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N\|Uh\|ryP	MYKyOFkxODJ4Nh?=
U87MG	MWfDfZRwfG:6aXOgRZN{[Xl?		MoHhO\|IhcA>?	MYrEUXNQ	NEPm[\|JEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN	MUGyOFkxODJ4Nh?=
A2780	NVy5SY5DTnWwY4Tpc44hSXO\|YYm=		MVGxJIg>	MVvEUXNQ	Mn;6TY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkC1OUDPxE1?	NEXWNnIzPDlyMEK2Oi=>
DU145	NXXm[JZDTnWwY4Tpc44hSXO\|YYm=		M4fzTFEhcA>?	MV7EUXNQ	NUX5XIFSUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKESXMUS1JINmdGy\|IHjhdoJwemmwZzDMT2IyKG23dHH0bY9vKHerdHigSWM2OCCxZjCwMlA4OyEQvF2=	NX7TeWc6OjR7MECyOlY>
A2780	M1TZ[2Z2dmO2aX;uJGF{e2G7		MnraNUBp	NWXsOoZwTE2VTx?=	NWTV[XZ7UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2=	M1\oU\|I1QTByMk[2
MCF7	Mn[4SpVv[3Srb36gRZN{[Xl?		MoL3NUBp	NGLDSWdFVVOR	NXXNfG1xUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh\|ryP	MYiyOFkxODJ4Nh?=
U87MG	NXTJWHBnTnWwY4Tpc44hSXO\|YYm=		MXixJIg>	MnHISG1UVw>?	MV3Jcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO	MXOyOFkxODJ4Nh?=
A2780	MorYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MXe3NkBp	NHf1OlZFVVOR	NFXTR2NGSzVyPUCuOVIh\|ryP	NHvuRYgzPDlyMEK2Oi=>
SKMES-1	NWToPZlxS3m2b4TvfIlkKEG\|c3H5	MmKzNUDPxE1?	MoryO\|IhcA>?		NXTQcWhkUW6mdXPld{Bk\WyuIHTlZZRp	NIL0N\|AzPjBzM{OxPC=>
H596	MmrISpVv[3Srb36gRZN{[Xl?	MkjTNUDPxE1?			M{D3cmlueGGrcoOgZ4VtdCCvaXfyZZRqd25?	MUeyOlAyOzNzOB?=
HCC2450	MYLGeY5kfGmxbjDBd5NigQ>?	MknaNUDPxE1?			MmXtTY1x[Wm{czDj[YxtKGmwdnHzbY9v	NV7OXnkzOjZyMUOzNVg>
A549	NWOwUG5{TnWwY4Tpc44hSXO\|YYm=	MYS1NFAhdk1?	MXG0PEBp	NHzMSWRFVVOR	NYjHOo5MUW6qaXLpeJMhSWu2IHHjeIl3[XSrb36=	NYjWepFtOjV7M{eyPVk>
A549	NHmxeWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{XMSVEh\|ryP	M1rMclczKGh?	NYPac4N1TE2VTx?=	MWXJcohq[mm2czDj[YxtKGe{b4f0bC=>	NVLMTWx3OjV7M{eyPVk>
H522	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV3yWW92OSEQvF2=	M336W\|czKGh?	MkDDSG1UVw>?	MUTJcohq[mm2czDj[YxtKGe{b4f0bC=>	NHW5bXozPTl\|N{K5PS=>
LNCaP	MlnuSpVv[3Srb36gRZN{[Xl?	NWPnVlh5OSEQvF2=			MkHLV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN?	MkTGNlU{PjB5OUm=
LNCaP95	Mn\xSpVv[3Srb36gRZN{[Xl?	NES0UIUyKM7:TR?=			NYrWOFg{W3WycILld5NmeyCyLVHLWEBt\X[nbIO=	MlP1NlU{PjB5OUm=
HCT-15	M1HOSWFxd3Sxc3nzJGF{e2G7	NVXMVZdiOTBizszN	NGHieIE1QCCq	Mon5SG1UVw>?	NGjrcFBKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVUh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	M{D4OVI2OTV{MkS1
HCT-116	M2r4V2Fxd3Sxc3nzJGF{e2G7	NID2eXkyOCEQvF2=	MVe0PEBp	MlWwSG1UVw>?	MofFTY5lfWOnczDhdI9xfG:\|aYOgbY4hUEOWLUGxOkBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	NVzLNFNTOjVzNUKyOFU>
NCI-H460	MWnBdI91d3OrczDBd5NigQ>?	MlrKNVAh\|ryP	NW\E[ZVKPDhiaB?=	NGOz[WdFVVOR	MkHuTY5lfWOnczDhdI9xfG:\|aYOgbY4hVkOLLVi0OlAh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	M2i3ZlI2OTV{MkS1
SKOV-3	MWXBdI91d3OrczDBd5NigQ>?	M{D2bVExKM7:TR?=	M4Lqe\|Q5KGh?	M4jZO2ROW09?	MWDJcoR2[2W\|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	MlHLNlUyPTJ{NEW=
BSY-1	MXfBdI91d3OrczDBd5NigQ>?	NGfhZZkyOCEQvF2=	NHnzdmk1QCCq	MkPDSG1UVw>?	NHL6WWhKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCEU2mtNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	M4Hm[FI2OTV{MkS1
MKN-1	MVXBdI91d3OrczDBd5NigQ>?	MkDCNVAh\|ryP	Mme1OFghcA>?	M2\JZWROW09?	NFjVUppKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	MnvFNlUyPTJ{NEW=
NCI-H522	MXvBdI91d3OrczDBd5NigQ>?	NXnZeVFxOTBizszN	MlTPOFghcA>?	NWnWV3JNTE2VTx?=	M4nxcGlv\HWlZYOgZZBweHSxc3nz	MWSyOVE2OjJ2NR?=
OVCAR-3	MV;BdI91d3OrczDBd5NigQ>?	M1W0T\|ExKM7:TR?=	M4CwUVQ5KGh?	MmPkSG1UVw>?	NEjkcmNKdmS3Y3XzJIFxd3C2b4Ppdy=>	M2f0d\|I2OTV{MkS1
HBC-5	NHjKPY9CeG:2b4Ppd{BCe3OjeR?=	M1eydlExKM7:TR?=	M1LIZlQ5KGh?	M3zse2ROW09?	MW\JcoR2[2W\|IHHwc5B1d3Orcx?=	NYLrU2t4OjVzNUKyOFU>
RXF-631L	MoTjRZBwfG:\|aYOgRZN{[Xl?	MoPMNVAh\|ryP	M4HRT\|Q5KGh?	NWG1WFJqTE2VTx?=	NWnnXFVUUW6mdXPld{BieG:ydH;zbZM>	M{LJdlI2OTV{MkS1
MKN-45	M2jpd2Fxd3Sxc3nzJGF{e2G7	MX2xNEDPxE1?	Mn\pOFghcA>?	M3XrV2ROW09?	NF60NW1KdmS3Y3XzJIFxd3C2b4Ppdy=>	MnG2NlUyPTJ{NEW=
BON-1	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2GwTFUxOCCwTR?=	MonONVAh\A>?	M2rtVGROW09?	M4q4VGlvcGmkaYTzJINmdGxiZ4Lve5Rp	M2fST\|I2ODJ4Mkmy
BON-1	M4\IfWZ2dmO2aX;uJGF{e2G7	NUfoc4REPTByIH7N	M1rYOFQhcA>?	NV3nW3puTE2VTx?=	NWHtd3NrUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ\|MEigZY5lKFOnckS3Ny=>	NFvYUpgzPTB{NkK5Ni=>
QGP-1	MYrGeY5kfGmxbjDBd5NigQ>?	M{fCO\|UxOCCwTR?=	M4rMT\|QhcA>?	M{\RVGROW09?	MYPJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd\|	MUmyOVAzPjJ7Mh?=
Huh7	MX7GeY5kfGmxbjDBd5NigQ>?	MXKxJO69VQ>?	Mln4NUBp	NXzlPVVHTE2VTx?=	MYjJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGPldlQ4PA>?	Mn;MNlUxODR2MEO=
BNL	M4\lZWZ2dmO2aX;uJGF{e2G7	NGK5[WQyKM7:TR?=	Mor3NUBp	NIDV[IJFVVOR	NFfqZVdKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhWzZ?	MUSyOVAxPDRyMx?=
MDA-MB-175	NYPMXnVFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnzoNUDPxE1?	MkT4OUBl	MVjEUXNQ	NG\2THdKSzVyPEGg{txO	NEfWUmUzPDh5OUe5Oi=>
MDA-MB-134	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV;XUFBPOSEQvF2=	MljiOUBl	M3m0N2ROW09?	MXvJR\|UxRDFizszN	NHWzO2QzPDh5OUe5Oi=>
HCC1500	Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mo\lNUDPxE1?	MoTlOUBl	M3raUGROW09?	NFfSdGJKSzVyPEGg{txO	M4jCeFI1QDd7N{m2
EFM-19	NXz4[4N3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MUGxJO69VQ>?	MlzlOUBl	NHGz[3pFVVOR	NHrkNmdKSzVyPEGg{txO	M17HO\|I1QDd7N{m2
ZR-75-30	M2PoN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnPsNUDPxE1?	M374WlUh\A>?	MoDySG1UVw>?	NFyy[HRKSzVyPEGg{txO	NXrMbGNROjR6N{m3PVY>
MDA-MB-361	NIrDVIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVexJO69VQ>?	NH7FeVg2KGR?	MVLEUXNQ	NYT0[ohmUUN3MEyxJO69VQ>?	M{\h[FI1QDd7N{m2
T-47D	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVuxJO69VQ>?	M2LpelUh\A>?	MmDrSG1UVw>?	M1nsOmlEPTB:MTFOwG0>	NWfvWphXOjR6N{m3PVY>
SK-BR-3	NFjJc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUD0fXdtOSEQvF2=	MnP5OUBl	MnvWSG1UVw>?	NF3neI9KSzVyPEGg{txO	NHewTY8zPDh5OUe5Oi=>
UACC-732	MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4TT[VEh\|ryP	MnPiOUBl	MoLDSG1UVw>?	NXfrRXo{UUN3MEyxJO69VQ>?	MYCyOFg4QTd7Nh?=
BT-474	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFu2SGIyKM7:TR?=	NUHOcFRPPSCm	NFz3RZdFVVOR	MUXJR\|UxRDFizszN	NXW2VpNqOjR6N{m3PVY>
HCC202	NVrlSpROT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmPINUDPxE1?	MWS1JIQ>	NH;EbnhFVVOR	M{H3UmlEPTB:MTFOwG0>	MWCyOFg4QTd7Nh?=
MCF7	M4\h[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlzYNUDPxE1?	NX\6PJJpPSCm	MULEUXNQ	NIHLPWNKSzVyPEGg{txO	M2jWelI1QDd7N{m2
MDA-MB-415	NYXzNG9UT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MX2xJO69VQ>?	NFvFWoU2KGR?	NVuxWnpvTE2VTx?=	NHSxWnlKSzVyPEGg{txO	NGn5O4ozPDh5OUe5Oi=>
MDA-MB-453	M3PzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWKxJO69VQ>?	NHLtRmY2KGR?	M4GwTGROW09?	M{KwRWlEPTB:MTFOwG0>	NXnPb5lFOjR6N{m3PVY>
ZR-75-1	M1PZe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2Lv[VEh\|ryP	M4TrTVUh\A>?	NFX5eXFFVVOR	NXHzc2xNUUN3MEyxJO69VQ>?	Mny1NlQ5Pzl5OU[=
HCC38	NXLHZ41ZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV7NUpZZOSEQvF2=	NFfCWI82KGR?	MmTzSG1UVw>?	M1PMTWlEPTB:MTFOwG0>	M{nleVI1QDd7N{m2
HCC1419	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4O5NlEh\|ryP	MWm1JIQ>	MUPEUXNQ	NInwTIlKSzVyPEGg{txO	MnTWNlQ5Pzl5OU[=
UACC-812	NFjDSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUfrOZpCOSEQvF2=	MlyxOUBl	NHniWlFFVVOR	NX;jSohmUUN3MEyxJO69VQ>?	NGnaR5IzPDh5OUe5Oi=>
HCC1187	Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGnvNGQyKM7:TR?=	MoTLOUBl	MXXEUXNQ	NUTqfGRPUUN3MEyxJO69VQ>?	MUOyOFg4QTd7Nh?=
KPL-1	Mnv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3;QclEh\|ryP	M3LDNFUh\A>?	MlfCSG1UVw>?	M3r5cWlEPTB:MTFOwG0>	NUK1emlPOjR6N{m3PVY>
SUM-225	Mny0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGX2[XIyKM7:TR?=	MYm1JIQ>	NEmwNoJFVVOR	NHfmZoZKSzVyPEGg{txO	NVvaUXFmOjR6N{m3PVY>
EFM-192A	NYLlTIM3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYCxJO69VQ>?	MoLPOUBl	NUP3cIg1TE2VTx?=	NWnzOIh7UUN3MEyxJO69VQ>?	NFXr[okzPDh5OUe5Oi=>
JIMT-1	MkX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{juWVEh\|ryP	MXK1JIQ>	M1GxbWROW09?	NYTHW\|BqUUN3MEyxJO69VQ>?	MknXNlQ5Pzl5OU[=
HCC1143	NHzXUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUCxJO69VQ>?	M3y1eVUh\A>?	M1j0RmROW09?	NGPROnVKSzVyPEGg{txO	MmDINlQ5Pzl5OU[=
HCC2218	NYnsRWl6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYfMTIh7OSEQvF2=	Mny3OUBl	M3LhWmROW09?	M2PYUGlEPTB:MTFOwG0>	NIfQTYszPDh5OUe5Oi=>
MDA-MB-468	NIXkcmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV6xJO69VQ>?	MWC1JIQ>	Mo[3SG1UVw>?	M2j2[mlEPTB:MTFOwG0>	MY[yOFg4QTd7Nh?=
BT-20	NHj1XYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGe2W2syKM7:TR?=	M3TmZVUh\A>?	M4DEe2ROW09?	NFXsS5ZKSzVyPEGg{txO	NFzJfpkzPDh5OUe5Oi=>
MDA-MB-435	NYG2XoQxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1zqSVEh\|ryP	M2jvPFUh\A>?	NInXbGVFVVOR	NYf1NY9pUUN3MEyxJO69VQ>?	NFT2OZIzPDh5OUe5Oi=>
BT-549	NGP4XXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NX\p[oNFOSEQvF2=	MV[1JIQ>	NWP5U5NrTE2VTx?=	NXLlWItMUUN3MEyxJO69VQ>?	MWCyOFg4QTd7Nh?=
HCC1806	MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NG\wT\|AyKM7:TR?=	Mly2OUBl	NEGzN4NFVVOR	M3;x[GlEPTB:MTFOwG0>	MYWyOFg4QTd7Nh?=
HCC1937	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlzwNUDPxE1?	NUDPOo1zPSCm	M2DJNGROW09?	MmTETWM2ODxzIN88US=>	NEPTUYozPDh5OUe5Oi=>
Hs578T	NH\zXHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4DseFEh\|ryP	NEPqTYs2KGR?	MoHxSG1UVw>?	NUDaTIFWUUN3MEyxJO69VQ>?	Ml7hNlQ5Pzl5OU[=
LN18	MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkfMNlAh\|ryP	NF\PZlg4OiCq	MVfEUXNQ	M3e3fWlEPTB:NTFOwG0>	M3;ublI1PzRzMEe0
LN229	NYm0SJB5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MUKyNEDPxE1?	NHTr[pQ4OiCq	MWXEUXNQ	MWPJR\|UxRDVizszN	M{\xPVI1PzRzMEe0
LNZ308	MofSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MViyNEDPxE1?	M3HzdFczKGh?	Mk\XSG1UVw>?	NVn6fotmUUN3MEy1JO69VQ>?	MkPPNlQ4PDFyN{S=
T98G	NHjoW4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M17UcVIxKM7:TR?=	MofiO\|IhcA>?	M4H1RmROW09?	MknhTWM2ODx3IN88US=>	MXiyOFc1OTB5NB?=
U87	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3eyPVIxKM7:TR?=	MX63NkBp	NInjNWlFVVOR	NGD5OGRKSzVyPEWg{txO	Mn;wNlQ4PDFyN{S=
LN18	MnvESpVv[3Srb36gRZN{[Xl?	NFLpU482KM7:TR?=	MUSyOEBp	Mnm5SG1UVw>?	MUjJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV	MXGyOFc1OTB5NB?=
LNZ308	M4raPGZ2dmO2aX;uJGF{e2G7	NHjXNoE2KM7:TR?=	NEP6XZozPCCq	M2DCbmROW09?	M3ewN2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R?	NWLpeWVQOjR5NEGwO\|Q>
Saos-2	NXHw[XlETnWwY4Tpc44hSXO\|YYm=	M3;nS\|UxKM7:TR?=	Ml\nOFghcA>?		MVvJcohq[mm2czDj[YxtKGmwdnHzbY9v	MkDVNlQ4Ojd4NkC=
MG-63	NV3RSIxsTnWwY4Tpc44hSXO\|YYm=	NUXvdmNqPTBizszN	NV;BZW9WPDhiaB?=		M4rFbmlvcGmkaYTzJINmdGxiaX72ZZNqd25?	NEfUU5UzPDd{N{[2NC=>
SJSA-1	M1v5fGZ2dmO2aX;uJGF{e2G7	NHHUdZI2OCEQvF2=	M2rZOVQ5KGh?		NX7mfY9nUW6qaXLpeJMh[2WubDDpcpZie2mxbh?=	NXTZ[I1wOjR5Mke2OlA>
Saos-2	Mk[0SpVv[3Srb36gRZN{[Xl?	MmHaOVAh\|ryP	NWPab25xPDhiaB?=		MXXJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	M3TjcVI1PzJ5Nk[w
MG-63	MoHlSpVv[3Srb36gRZN{[Xl?	MkHyOVAh\|ryP	M37qWFQ5KGh?		NETFR\|dKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v	M4rVUlI1PzJ5Nk[w
SJSA-1	MkDhSpVv[3Srb36gRZN{[Xl?	MoPIOVAh\|ryP	MmTJOFghcA>?		NX;4bXg2UW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>?	MViyOFczPzZ4MB?=
Saos-2	M1PUTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkXYOVAh\|ryP	MofDOFghcA>?		MY\Jcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>?	NV;FOoVMOjR5Mke2OlA>
MG-63	M2PzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGDxfnA2OCEQvF2=	NHfKV4Y1QCCq		NV\FfWhbUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	MVmyOFczPzZ4MB?=
SJSA-1	NXO5TJVOT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWXIUHFpPTBizszN	NH3leZc1QCCq		MnLaTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl?	NEfieGgzPDd{N{[2NC=>
FaDu	MmL2SpVv[3Srb36gRZN{[Xl?	M3PZPFUh\|ryP	NGjuXpIzPCCq	MWTEUXNQ	MkjYVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36=	M3HvRVI1PjNzMUS3
EMT6	NHvmelVHfW6ldHnvckBCe3OjeR?=	M17ENlUh\|ryP	NXrsb2s3OjRiaB?=	MorxSG1UVw>?	M2P4N3Jm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	NH;kdW8zPDZ\|MUG0Oy=>
HCT116	MXPGeY5kfGmxbjDBd5NigQ>?	NUHWUI0{PSEQvF2=	MmPyNlQhcA>?	MXLEUXNQ	NIjyRlRT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	MVWyOFY{OTF2Nx?=
U87	MY\GeY5kfGmxbjDBd5NigQ>?	NYDaPXlFPSEQvF2=	NHnvdpQzPCCq	NXz2W5JlTE2VTx?=	NEC0Rm1T\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	MljzNlQ3OzFzNEe=
GBM	MmXBRZBweHSxc3nzJGF{e2G7	M1nEfFLPxE1?	MY[0PIg>	M4r0dmROW09?	NHrvd2ZqdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6	NWrhXZBSOjR3MEC0PVI>
BON	NWnCc4EzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnvmNU02\|ryP	MofpO\|Jp		NWX6XFZy\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>?	M1LLbVI1PDR\|NUKz
BON	NEjGV49CeG:ydH;zbZMhSXO\|YYm=	NX\0W4tFOS13zszN	M4ruS\|I1cA>?		M2DoWolv[3KnYYPld{BieG:ydH;zbZM>	NGjWb3EzPDR2M{WyNy=>
H1975	NI\DfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1L5fFAvOy17LkdOwG0>	MmTzO\|Jp	MVHEUXNQ	MlX2TWM2OD1zLkO4Oe69VQ>?	MnqyNlQ{Ozd6NE[=
H1975	MnH0RZBweHSxc3nzJGF{e2G7	MWiy{txO	NEfVSVEzPGh?	M{\EVWROW09?	MnXPbY5kemWjc3XzJIFxd3C2b4Ppd{Bz[XSnIIPp[45q\mmlYX70cJk>	MnTyNlQ{Ozd6NE[=
T-ALL	NInKWldCeG:ydH;zbZMhSXO\|YYm=	NGm3TXNj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW=	M2j3d\|I1KG:{IES4bC=>	MYLEUXNQ	NH;CWGdi\m[nY4TzJJRp\SCSSUPLJJBifGi5YYmgbY4hXC2DTFygZ4VtdCCuaX7ldy=>	M3HKOVI1OzFyN{O2
BCR-ABL	MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHywUlYxNjJ3LUGw{txO	M3;pPVRl		NULWUY4ye2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?=	M4D3R\|I1OjR2NkGy
LC-1/SQSF	M4OxR2Z2dmO2aX;uJGF{e2G7	NEnFUYY{\|ryP	NGrTfGwzPGh?	M{\Y[GROW09?	M{nJS4Rm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=>	MkDsNlM6QDByOUO=
Primary CLL cells	NYHROYd7SXCxcITvd4l{KEG\|c3H5	NUTINnpTOS1zMN88US=>	NVTVTnN3PDiq		MUfpcoR2[2W\|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz	M1vqSFI{QDVyOEC3
Primary CLL cells	MmHJT4lv[XOnIFHzd4F6	MmPTNu69VQ>?	NGXS[2c{OG2rbh?=		NUPQe5c4\GWlcnXhd4VlKFCLM1ugZYN1cX[rdIm=	MWqyN\|g2ODhyNx?=
Primary CLL cells	MVPDfZRwfG:6aXOgRZN{[Xl?	NVvEXodxOs7:TR?=	MVeyOIg>		NIPqUVlqdmS3Y3XzJINmdGxiY4n0c5RwgGmlaYT5	MVWyN\|g2ODhyNx?=
human NSCLC cell lines	M4nWOmFxd3C2b4Ppd{BCe3OjeR?=	Mlu1NE4yOjVvNN88US=>	M4XM[FI1cA>?	MlrNSG1UVw>?	NIX4S41KSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=>	MWqyN\|U3OjR5Mh?=
human HCC cell lines	NHrt[GFE\WyuII\pZYJqdGm2eTDhd5NigQ>?	NXrvW4w6OC5yMEWtNe69VQ>?	NILhXYw1QGh?		MXTJR\|UxRTIQvF2=	NGfZepgzOzR6OUm5PS=>
Huh7	M1;6NGtqdmG\|ZTDBd5NigQ>?	NE\SO2sy\|ryP	MXy0PIg>		NYqyfVJSe2mpbnpvsKFk[W62bImgdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gRYt1	MUKyN\|Q5QTl7OR?=
SK-HEP1	NXvsWJI4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXvpdppDOS1{MN88US=>	NYDuem9TPzKq	NXi3[opJTE2VTx?=	M{\GcmlEPTExvKyx{txO	Mn7FNlM1PzlzM{[=
786-0	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2jVZ\|EuOjEQvF2=	MnL4O\|Jp	MYLEUXNQ	MV3JR\|Ux97zeMd88US=>	M36ydlI{PDd7MUO2
JVM2	MlPZR5l1d3SxeHnjbZR6KGG\|c3H5	M{LKUVAvOi1{MN88US=>	MXK3Nog>	M4DxPGROW09?	MojoTWM2OD1yLkpOwG0>	NGPFSYgzOzJ\|OE[zPS=>
EHEB	MlfMR5l1d3SxeHnjbZR6KGG\|c3H5	MUSwMlIuOjEQvF2=	NYLqbYlnPzKq	NXrpUJhPTE2VTx?=	MmTkTWM2OD1yLkhOwG0>	MkHwNlMzOzh4M{m=
MEC2	NEnsVo5EgXSxdH;4bYNqfHliYYPzZZk>	NFT5Z4wxNjJvMkFOwG0>	MnnkO\|Jp	MYnEUXNQ	M4PZU2lEPTB;MD63{txO	NYDQenNnOjN{M{i2N\|k>
primary B-CLL lymphocytes	M2\JVGFxd3C2b4Ppd{BCe3OjeR?=	NHHwXVRKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n	M2D1e\|I1cA>?	M{PLfWROW09?	NFnGTXBKSzVy78{cN:69VSCob4KgZYxtKHCjdHnlcpR{	Mny1NlMzOzh4M{m=
primary B-CLL lymphocytes	MYLLbY5ie2ViQYPzZZk>	NIexeXpKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n	MlnYNlRp		MkD5bY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36=	NFLpNFEzOzJ\|OE[zPS=>
human NSCLC	NWjte2FCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF[0cVYxNjVvMt88US=>	M3rBS\|czcA>?		MVjJR\|UxRTIQvF2=	NU\WcpF5OjJ5OEGzPVM>
human NSCLC	NX7WbppNU2mwYYPlJGF{e2G7	NYC4WZNzOc7:TR?=	NWPDcpJDOjSq		M2nuOolvcGmkaYTzJJRp\SCDa4SvcXRQWiC\|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS=	MViyNlc5OTN7Mx?=
Y1 cell line	M3rlXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV:0fHhKOC5zzszNM\|HPxE1?	MUWyOIg>	NYPibJdwTE2VTx?=	Mn7rbY5pcWKrdIOgOlDwxIViY3XscEB3cWGkaXzpeJkhcW5iTYnjMXNkfHJvdILhcpNn\WO2ZXSgZ4VtdHN?	M4fkTVIzPjl{OUC0
PIK3CA-mutant MCF7	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUHHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO\|NvVQ>?	MlfiO\|Jp		NW\QVoY{T0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd\|bl2=	NV3teIN6OjJ4NUO5Olc>
PIK3CA-mutant MCF7	NFm3[GFMcW6jc3WgRZN{[Xl?	MVrJR\|UxRTFzNNMxN45O	NXuwVZFPPzKq		NWnSTpBFUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=>	MY[yNlY2Ozl4Nx?=
MCF7-myr-Akt	MoTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NYTjdJJ2T0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2=	M1yzVFczcA>?		NWrDeFM1T0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2=	NYnSSG1bOjJ4NUO5Olc>
colon cancer cell lines	NWPZfJdsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1KwO\|AuOTEQvF2=	NHXp[HU4Omh?	NIjGVmtFVVOR	NUPwfI1zUUN3ME2x{txO	NIft[IEzOjV2M{i1Oy=>
gastric cancer cell lines	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2P1PFAuOTEQvF2=	MlPXO\|Jp	NX[3No5FTE2VTx?=	MkP2TWM2OD1{LUZOwG0>	NVnaNFEyOjJ3NEO4OVc>
HCT-116/HT-29/MKN-45	NXfs[GM{SXCxcITvd4l{KEG\|c3H5	MlTLNu69VQ>?	M{LEV\|Q5cA>?		NUPEVGVue2irZoSgbY4hTzJicHjhd4U>	NWPaN\|JCOjJ3NEO4OVc>
HT-29 and HCT-116	M2PrT2Nie3Cjc3WgZZN{[Xl?	MWW1{txO	NX7Sc29KOjSq		NWDBUYJVcW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5	M17tN\|IzPTR\|OEW3
MM cell lines	NHPTPZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnrjNVDPxE1?	M4n1elI1cA>?	NEnmc41FVVOR	M{TNfWlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>?	M3TvR\|IzOjB5NEi1
ARP-1	MnPiRZBweHSxc3nzJGF{e2G7	NF3rVVIyOM7:TR?=	M4LNZ\|I1cA>?	M2LBR2ROW09?	NYTTWYM5cW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=>	MVqyNlIxPzR6NR?=
SNU-601	NUnYRXNxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NUPLRpNqPzKq	NYDLWmdTTE2VTx?=	NXS5[HhKUUN3ME2wMlgyPsLzMD6wOlPPxE1?	M1f4clIzOTV7OEG0
SNU-1	MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NEDhZm44Omh?	MWnEUXNQ	MV7JR\|UxRTFwMEiyxtExNjB{ON88US=>	M{DheFIzOTV7OEG0
SNU-668	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M1XWd\|czcA>?	MmXVSG1UVw>?	NV3kOpNYUUN3ME2xMlU4QcLzMD6wO\|TPxE1?	NYmz[XdDOjJzNUm4NVQ>
AGS	NWfBZ2RET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MkLiO\|Jp	NEm5NIRFVVOR	NHvveFVKSzVyPUGuO\|E1yrFyLkGxO:69VQ>?	NHLINmQzOjF3OUixOC=>
SNU-216	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXuxNGE6PzKq	NHzjWVBFVVOR	NFrKUINKSzVyPUKuOlkzyrFyLkC4Nu69VQ>?	Mn\2NlIyPTl6MUS=
SNU-5	M3S0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MnfKO\|Jp	NVLmNYV7TE2VTx?=	MXnJR\|UxRTFwM{WxxtExNjB7Md88US=>	NYT0U4Y5OjJzNUm4NVQ>
SNU-638	Ml;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M2HoS\|czcA>?	MVXEUXNQ	M3HG[GlEPTB;Mj6yPFLDuTBwMEWz{txO	NV\sdItCOjJzNUm4NVQ>
SNU-16	M2mx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NHvSfVA4Omh?	MnXkSG1UVw>?	NUGxb41VUUN3ME2xMlU4O8LzMD6wNFHPxE1?	M3LSRVIzOTV7OEG0
SNU-484	NGr0[ZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MX63Nog>	NG\PXGFFVVOR	MWPJR\|UxRTFwN{K4xtExNjB2Nd88US=>	MWCyNlE2QThzNB?=
SNU-620	M1zOd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MYC3Nog>	M1jGcmROW09?	MVjJR\|UxRTJwOUO5xtExNjByMd88US=>	MojhNlIyPTl6MUS=
SNU-719	MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYPqcVVFPzKq	M3z5UmROW09?	NXzxPFVzUUN3ME2zMlA{P8LzMD6wN\|LPxE1?	NEW4dlkzOjF3OUixOC=>
glioma cell lines	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M176SFczcA>?		MnzCTWM2OD1zLUNOwG0>	NH24dWQzOjB4NUC4NC=>
U87	M2HUbWFxd3C2b4Ppd{BCe3OjeR?=	MmX2Nu69VQ>?	M{WxZlczcA>?		NHO2do5qdmS3Y3XzJINmdGxiYYDvdJRwe2m\|IHHu[EBkdGWjdnXkJHBCWlBiYX7kJINie3Cjc3WtNy=>	NFH3XZAzOjB4NUC4NC=>

... 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 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02756247	Active not recruiting	Lymphoma\|Mantle Cell Lymphoma\|Follicular Lymphoma\|Diffuse Large B Cell Lymphoma	Memorial Sloan Kettering Cancer Center\|Janssen Scientific Affairs LLC\|Novartis Pharmaceuticals	May 2016	Phase 1
NCT02756247	Active not recruiting	Lymphoma\|Mantle Cell Lymphoma\|Follicular Lymphoma\|Diffuse Large B Cell Lymphoma	Memorial Sloan Kettering Cancer Center\|Janssen Scientific Affairs LLC\|Novartis Pharmaceuticals	May 2016	Phase 1
NCT02614508	Active not recruiting	Recurrent Chronic Lymphocytic Leukemia\|Recurrent Small Lymphocytic Lymphoma\|Refractory Chronic Lymphocytic Leukemia\|Refractory Small Lymphocytic Lymphoma	Emory University\|Novartis	January 2016	Phase 1
NCT02614508	Active not recruiting	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	Treatment for Metastatic or Locally Advanced Cervical Cancer	Novartis Pharmaceuticals\|Novartis	November 2015	Phase 2
NCT01613677	Withdrawn	Treatment for Metastatic or Locally Advanced Cervical Cancer	Novartis Pharmaceuticals\|Novartis	November 2015	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

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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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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, 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.
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, NVP-BKM120)

Cited by 51 Publications

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Protocol

References

Solubility (25°C)

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

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

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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 2019-03-27)

Tech Support

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products5

Choose Your Country or Region

By Signaling Pathways

By product type

Buparlisib (BKM120, NVP-BKM120)

Cited by 51 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 (g) = Concentration (mol/L) × Volume (L) × 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 2019-03-27)

Tech Support

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products5

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