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 41 Publications

Nat Med, 2015, 10.1038/nm.3855

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

Nat Commun, 2018, 9(1):4550

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

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

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

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

PubMed: 24356096 ( click the link to review the publication )

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

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

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

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

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

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

J Clin Invest, 2015, 10.1172/JCI78018

PubMed: 25798617 ( 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 )

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

PubMed: 26224873 ( click the link to review the publication )
Clin Cancer Res, 2013, 19(21):5940-51

PubMed: 23918606 ( 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 )

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

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

Oncogene, 2015, 10.1038/onc.2015.173

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

Oncogene, 2014, 10.1038/onc.2014.328

PubMed: 25284585 ( 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, 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 )

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

PubMed: 23844554 ( 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 Ther, 2017, 10.1158/1535-7163

PubMed: 28119489 ( 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 )

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 )

BMC Cancer, 2013, 13:465

PubMed: 24103747 ( 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, 2016, 10.1371/journal

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

PLoS One, 2015, 10(4):e0123410

PubMed: 25844720 ( 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 )

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

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

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

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

University Gattingen, 2013, Elisabeth Hand

PubMed: ( click the link to review the publication )

6 Customer Reviews

NLGN3 mRNA expression in SU-pcGBM2 cells after 12 hr exposure to vehicle, 50 nM NLGN3, 100 nM BKM120, or 50 nM NLGN3 + 100 nM BKM120.

Cell, 2017, 161(4):803-16. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

Western blot analysis of cleaved caspase 3 in T cell-enriched PBMCs.

J Hematol Oncol, 2016, 9(1):113. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.
AN3CA (A) and JHUEM2 (B) cells were treated for the indicated times with DMSO, 0.3 μM BGJ398 (BGJ), 0.3 μM GDC-0941 (GDC), 0.6 μM BYL719 (BYL) and 0.6 μM BKM120 (BKM) alone or in combination. Cell lysates were immunoblotted with antibodies for phospho-AKT (Ser473), total AKT, phospho-ERK (Thr202/Tyr204), ERK2, phospho-S6 (Ser240/244), total S6, phospho-4EBP1 (Thr37/46), total 4EBP1, total PARP and cleaved PARP. Tubulin was detected as the loading control. Western blot analysis of AN3CA and JHUEM2.

Mol Cancer Ther, 2017, 16(4):637-648. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of BKM120 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.

Dr. Zhang of Tianjin Medical University. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.
One customer. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

Dr. Pilar Eroles of INCLIVA Biomedical Research Institute.. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

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	Mn7RR5l1d3SxeHnjJGF{e2G7		NUnkfVN[PzJiaB?=	MY\EUXNQ	NUj6Vpl2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=>	NFnEUJAzPDlyMEK2Oi=>
DU145	MWLDfZRwfG:6aXOgRZN{[Xl?		MmDDO\|IhcA>?	NXTifYVFTE2VTx?=	MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1?	MXeyOFkxODJ4Nh?=
A2780	MnHER5l1d3SxeHnjJGF{e2G7		NHr5N4E4OiCq	NFXXb\|RFVVOR	M{DpdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO\|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2=	M{fCO\|I1QTByMk[2
U87MG	M{LtRmN6fG:2b4jpZ{BCe3OjeR?=		NV7IPZJoPzJiaB?=	NWq3boVTTE2VTx?=	MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh\|ryP	NXziT3RkOjR7MECyOlY>
A2780	NVq5SWpwTnWwY4Tpc44hSXO\|YYm=		M1PZOFEhcA>?	NFnENWVFVVOR	M4fhcmlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6wOVUh\|ryP	NGfLTpUzPDlyMEK2Oi=>
DU145	NI\DXZNHfW6ldHnvckBCe3OjeR?=		M3;WXlEhcA>?	M{fPW2ROW09?	MofPTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1?	MmHlNlQ6ODB{Nk[=
A2780	MVLGeY5kfGmxbjDBd5NigQ>?		NHX1epcyKGh?	NGHrR\|BFVVOR	MUfJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>?	Mn:4NlQ6ODB{Nk[=
MCF7	MV7GeY5kfGmxbjDBd5NigQ>?		NHnTSpYyKGh?	NU\XT\|hLTE2VTx?=	NXHPUnhjUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh\|ryP	NHLhbZYzPDlyMEK2Oi=>
U87MG	MYTGeY5kfGmxbjDBd5NigQ>?		M3vu[\|EhcA>?	MkfxSG1UVw>?	MmjGTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJIlvKFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiRVO1NEBw\iByLkGzJO69VQ>?	M1rnWVI1QTByMk[2
A2780	NEfYRXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MVe3NkBp	M4noRmROW09?	MYjFR\|UxRTBwNUKg{txO	MYqyOFkxODJ4Nh?=
SKMES-1	NULIO\|JCS3m2b4TvfIlkKEG\|c3H5	Mn\0NUDPxE1?	Mkf0O\|IhcA>?		NGHPOGZKdmS3Y3XzJINmdGxiZHXheIg>	M2iyRlI3ODF\|M{G4
H596	M{TyfmZ2dmO2aX;uJGF{e2G7	MXixJO69VQ>?			NGXhV4lKdXCjaYLzJINmdGxibXnndoF1cW:w	NFy5W3QzPjBzM{OxPC=>
HCC2450	NUjtN21RTnWwY4Tpc44hSXO\|YYm=	Mn;vNUDPxE1?			NHX6e3VKdXCjaYLzJINmdGxiaX72ZZNqd25?	MUGyOlAyOzNzOB?=
A549	MYPGeY5kfGmxbjDBd5NigQ>?	MmjpOVAxKG6P	M2TtXlQ5KGh?	NHXzdm1FVVOR	MlzMTY5pcWKrdIOgRYt1KGGldHn2ZZRqd25?	NEPNVHMzPTl\|N{K5PS=>
A549	Mn;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGTEWZUyKM7:TR?=	MXy3NkBp	NGG3eJVFVVOR	NGXMU\|VKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	M2PFWFI2QTN5Mkm5
H522	NEDJV5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MWexJO69VQ>?	NGD0Tm84OiCq	MV;EUXNQ	M{HoXWlvcGmkaYTzJINmdGxiZ4Lve5Rp	NUnYW5VnOjV7M{eyPVk>
LNCaP	NVKzVIxjTnWwY4Tpc44hSXO\|YYm=	Mlu2NUDPxE1?			M3;V[XN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy\|	NIrrWVAzPTN4MEe5PS=>
LNCaP95	NUTWfoZwTnWwY4Tpc44hSXO\|YYm=	NUXlWFZrOSEQvF2=			MmL0V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN?	M135dVI2OzZyN{m5
HCT-15	M1e0UmFxd3Sxc3nzJGF{e2G7	M17KT\|ExKM7:TR?=	NYnO[3pWPDhiaB?=	MoTpSG1UVw>?	M4fnSGlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xOUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	NFH5ZVczPTF3MkK0OS=>
HCT-116	M2fldmFxd3Sxc3nzJGF{e2G7	NYjoeJVXOTBizszN	NFntZ241QCCq	M3z3d2ROW09?	M{TsPGlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	NEPYdJUzPTF3MkK0OS=>
NCI-H460	NUnMOWZRSXCxdH;zbZMhSXO\|YYm=	MlXZNVAh\|ryP	M{fVNVQ5KGh?	NXzkZ5M2TE2VTx?=	M4TvWGlv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36=	NHjCco4zPTF3MkK0OS=>
SKOV-3	NFTQR3FCeG:2b4Ppd{BCe3OjeR?=	NVvhcGpjOTBizszN	NUPG[plDPDhiaB?=	M2jSfGROW09?	MljkTY5lfWOnczDhdI9xfG:\|aYOgbY4hW0uRVj2zJINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	NXqyWlZTOjVzNUKyOFU>
BSY-1	NVThVmNYSXCxdH;zbZMhSXO\|YYm=	NEXjfmUyOCEQvF2=	MoHFOFghcA>?	NGnld4pFVVOR	MYPJcoR2[2W\|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT\|NESSCqb4TzdI91KG23dHH0bY9v	NFHZeFEzPTF3MkK0OS=>
MKN-1	MX7BdI91d3OrczDBd5NigQ>?	NUXBU4xOOTBizszN	NUHsV4liPDhiaB?=	MVHEUXNQ	NVqxc2Q6UW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	M4\nOFI2OTV{MkS1
NCI-H522	NFLCUZBCeG:2b4Ppd{BCe3OjeR?=	NUTkS\|kyOTBizszN	MlXmOFghcA>?	MYXEUXNQ	NG\aXJVKdmS3Y3XzJIFxd3C2b4Ppdy=>	MX:yOVE2OjJ2NR?=
OVCAR-3	NUTBbZlWSXCxdH;zbZMhSXO\|YYm=	MnnYNVAh\|ryP	NH35V401QCCq	MXrEUXNQ	MXnJcoR2[2W\|IHHwc5B1d3Orcx?=	NYrweHpQOjVzNUKyOFU>
HBC-5	M3y4R2Fxd3Sxc3nzJGF{e2G7	NGWyVGUyOCEQvF2=	MorpOFghcA>?	M4GyWGROW09?	MmqwTY5lfWOnczDhdI9xfG:\|aYO=	NYjUbWtHOjVzNUKyOFU>
RXF-631L	NFjMSIZCeG:2b4Ppd{BCe3OjeR?=	NHPZfpYyOCEQvF2=	M3:2XlQ5KGh?	M2[0c2ROW09?	NEewR5lKdmS3Y3XzJIFxd3C2b4Ppdy=>	NEDNcoEzPTF3MkK0OS=>
MKN-45	M1zwO2Fxd3Sxc3nzJGF{e2G7	MmfBNVAh\|ryP	MUi0PEBp	MVHEUXNQ	NXLPPIU3UW6mdXPld{BieG:ydH;zbZM>	NIjtcIUzPTF3MkK0OS=>
BON-1	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{C2dVUxOCCwTR?=	NGjqS2gyOCCm	MX7EUXNQ	MnnsTY5pcWKrdIOgZ4VtdCCpcn;3eIg>	NXLPXJRUOjVyMk[yPVI>
BON-1	MXnGeY5kfGmxbjDBd5NigQ>?	NF\QVpI2ODBibl2=	MV[0JIg>	MYTEUXNQ	NV7uNHZRUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ\|MEigZY5lKFOnckS3Ny=>	MlPYNlUxOjZ{OUK=
QGP-1	M{XCXGZ2dmO2aX;uJGF{e2G7	NVW3cXNCPTByIH7N	NIL3RWw1KGh?	MnzGSG1UVw>?	MojpTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?=	MWSyOVAzPjJ7Mh?=
Huh7	NF;MRY1HfW6ldHnvckBCe3OjeR?=	MXexJO69VQ>?	M3TxUlEhcA>?	MUDEUXNQ	MlnMTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR?	MYWyOVAxPDRyMx?=
BNL	NWjnUGNvTnWwY4Tpc44hSXO\|YYm=	MVWxJO69VQ>?	NV7ZN4dGOSCq	M1nLZmROW09?	M{DtWmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>?	NXr4NpREOjVyMES0NFM>
MDA-MB-175	NUexPYJWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXTVfpdVOSEQvF2=	MUC1JIQ>	M1fYPWROW09?	NUHhSIlXUUN3MEyxJO69VQ>?	M4P2ZlI1QDd7N{m2
MDA-MB-134	NGTaTm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml3XNUDPxE1?	MWq1JIQ>	NEjON41FVVOR	NFvJW\|BKSzVyPEGg{txO	NHfEPVMzPDh5OUe5Oi=>
HCC1500	NGq1N5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkDYNUDPxE1?	MYe1JIQ>	MWLEUXNQ	NHqxZ3hKSzVyPEGg{txO	MUOyOFg4QTd7Nh?=
EFM-19	MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4PKZVEh\|ryP	MmHqOUBl	Mki0SG1UVw>?	NWTtSmZ6UUN3MEyxJO69VQ>?	NFKyNo0zPDh5OUe5Oi=>
ZR-75-30	NV[ycGt[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2nrUFEh\|ryP	MnPOOUBl	M3zZbmROW09?	NWDYWG9FUUN3MEyxJO69VQ>?	MYqyOFg4QTd7Nh?=
MDA-MB-361	MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWWySYtZOSEQvF2=	Ml;mOUBl	NWn1Zm9TTE2VTx?=	NVKyRmtlUUN3MEyxJO69VQ>?	NXvzbJdOOjR6N{m3PVY>
T-47D	NIPtfXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFi0ZlkyKM7:TR?=	MnzJOUBl	M3\ldGROW09?	NGm2bXVKSzVyPEGg{txO	NIO5ZXMzPDh5OUe5Oi=>
SK-BR-3	M1zNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUWxJO69VQ>?	NGLRS4U2KGR?	NYrKfGp{TE2VTx?=	M4DKVmlEPTB:MTFOwG0>	NYXYcIxNOjR6N{m3PVY>
UACC-732	Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NYL4bnR5OSEQvF2=	M2mzc\|Uh\A>?	M1TWWGROW09?	M1LxOmlEPTB:MTFOwG0>	MUKyOFg4QTd7Nh?=
BT-474	NUjvcGhNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmLiNUDPxE1?	MX21JIQ>	MWnEUXNQ	NV[xN5pTUUN3MEyxJO69VQ>?	NWrTdZdyOjR6N{m3PVY>
HCC202	MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGThbYEyKM7:TR?=	MX:1JIQ>	MXvEUXNQ	M1KyTmlEPTB:MTFOwG0>	MXGyOFg4QTd7Nh?=
MCF7	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHG4VlkyKM7:TR?=	NFm5Smo2KGR?	Mnm1SG1UVw>?	M{nuO2lEPTB:MTFOwG0>	NVTKV3NlOjR6N{m3PVY>
MDA-MB-415	NHPPUphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlK2NUDPxE1?	Ml\4OUBl	MUXEUXNQ	NIrZfnJKSzVyPEGg{txO	NGXLTpUzPDh5OUe5Oi=>
MDA-MB-453	NEDod\|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NIXsWpEyKM7:TR?=	MoPnOUBl	MlzYSG1UVw>?	MlvvTWM2ODxzIN88US=>	NYLscVV5OjR6N{m3PVY>
ZR-75-1	Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEe3RmcyKM7:TR?=	NIfk[2o2KGR?	Mkj3SG1UVw>?	M3HH[2lEPTB:MTFOwG0>	MWiyOFg4QTd7Nh?=
HCC38	M3fpc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4nnXVEh\|ryP	MX:1JIQ>	M1n2bmROW09?	Mn;FTWM2ODxzIN88US=>	NGexSJYzPDh5OUe5Oi=>
HCC1419	MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF:3b4oyKM7:TR?=	Mn3TOUBl	MVrEUXNQ	NVT6b2FVUUN3MEyxJO69VQ>?	NFn5RoYzPDh5OUe5Oi=>
UACC-812	MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnHGNUDPxE1?	MUO1JIQ>	Mmj5SG1UVw>?	MnrpTWM2ODxzIN88US=>	NUHBS5FyOjR6N{m3PVY>
HCC1187	NFzPXm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mo[yNUDPxE1?	MUi1JIQ>	M{fzSmROW09?	NF[wNohKSzVyPEGg{txO	M4\nNVI1QDd7N{m2
KPL-1	NHXRSIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3LaUVEh\|ryP	M37kSFUh\A>?	M1HKW2ROW09?	MkK0TWM2ODxzIN88US=>	M33mUVI1QDd7N{m2
SUM-225	NFznfXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHPBc4cyKM7:TR?=	MXG1JIQ>	M33wT2ROW09?	M{DJfGlEPTB:MTFOwG0>	M33BT\|I1QDd7N{m2
EFM-192A	M4PqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHvyNGwyKM7:TR?=	M{TkSlUh\A>?	M{KxNGROW09?	MkjCTWM2ODxzIN88US=>	M3\zflI1QDd7N{m2
JIMT-1	NFfkUWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXT0cY1OOSEQvF2=	NV\JcWREPSCm	M1PLWWROW09?	Mlv0TWM2ODxzIN88US=>	MUKyOFg4QTd7Nh?=
HCC1143	M1jFfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NG\pdnoyKM7:TR?=	M2PHclUh\A>?	NGPkWJRFVVOR	NH22WY5KSzVyPEGg{txO	NI\4bI0zPDh5OUe5Oi=>
HCC2218	MlHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWHXNol4OSEQvF2=	M3;jOlUh\A>?	NWf5R\|ZzTE2VTx?=	NHq1fXlKSzVyPEGg{txO	NIG2UWszPDh5OUe5Oi=>
MDA-MB-468	M1i0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NH;yR2EyKM7:TR?=	M{DlelUh\A>?	MorZSG1UVw>?	MWDJR\|UxRDFizszN	NHLGNmQzPDh5OUe5Oi=>
BT-20	NGrnUlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWTEUYRlOSEQvF2=	MYi1JIQ>	NXXqbI11TE2VTx?=	MnXtTWM2ODxzIN88US=>	M4\mVlI1QDd7N{m2
MDA-MB-435	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3jUZ\|Eh\|ryP	Mk\kOUBl	M17wWmROW09?	MlHVTWM2ODxzIN88US=>	MWGyOFg4QTd7Nh?=
BT-549	NFLRUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHmzT2MyKM7:TR?=	NF;nVoQ2KGR?	Mn7zSG1UVw>?	MWXJR\|UxRDFizszN	NYPXNW1vOjR6N{m3PVY>
HCC1806	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHjldpIyKM7:TR?=	NVe5VFd5PSCm	NFHmdY9FVVOR	NVzOO2tmUUN3MEyxJO69VQ>?	MnvWNlQ5Pzl5OU[=
HCC1937	MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlPBNUDPxE1?	MmHjOUBl	MUHEUXNQ	NV;vcpl1UUN3MEyxJO69VQ>?	M1Syc\|I1QDd7N{m2
Hs578T	MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXqxJO69VQ>?	NIOzUJA2KGR?	NVq2ZnF6TE2VTx?=	M1n2emlEPTB:MTFOwG0>	MVGyOFg4QTd7Nh?=
LN18	M{PvdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUeyNEDPxE1?	NVTYUYJUPzJiaB?=	NHrpZ3dFVVOR	NIDDe5NKSzVyPEWg{txO	M4PnOVI1PzRzMEe0
LN229	M{\ZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXmyNEDPxE1?	MYe3NkBp	NY\lfVdCTE2VTx?=	NHnPWWtKSzVyPEWg{txO	MnfsNlQ4PDFyN{S=
LNZ308	NHvDeGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlXENlAh\|ryP	Mn;6O\|IhcA>?	NETyV\|NFVVOR	MWDJR\|UxRDVizszN	M3jE[\|I1PzRzMEe0
T98G	NIXqOlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml3pNlAh\|ryP	NFjs[HU4OiCq	NU[1OWNZTE2VTx?=	MlL1TWM2ODx3IN88US=>	NGfJXpczPDd2MUC3OC=>
U87	NFzmeVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{DKTFIxKM7:TR?=	MVG3NkBp	MlPSSG1UVw>?	Mn;2TWM2ODx3IN88US=>	MVmyOFc1OTB5NB?=
LN18	M13sWGZ2dmO2aX;uJGF{e2G7	NV;6TI9nPSEQvF2=	MoLoNlQhcA>?	NX\iXohWTE2VTx?=	MmG5TY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>?	M2XN[\|I1PzRzMEe0
LNZ308	MonZSpVv[3Srb36gRZN{[Xl?	MnftOUDPxE1?	MWeyOEBp	MlPuSG1UVw>?	NFvsR2VKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuW	M{jSdFI1PzRzMEe0
Saos-2	MV;GeY5kfGmxbjDBd5NigQ>?	M{X4UFUxKM7:TR?=	NGjm[Gc1QCCq		MnHOTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	MX:yOFczPzZ4MB?=
MG-63	NH7Hb\|ZHfW6ldHnvckBCe3OjeR?=	NYCyeYZXPTBizszN	NHzlcoE1QCCq		NETXe5lKdmirYnn0d{Bk\WyuIHnueoF{cW:w	NH;XVJYzPDd{N{[2NC=>
SJSA-1	NXPTVGVKTnWwY4Tpc44hSXO\|YYm=	M17xdFUxKM7:TR?=	NU\TPJl2PDhiaB?=		MlrZTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	M3fzV\|I1PzJ5Nk[w
Saos-2	NWLVfYc{TnWwY4Tpc44hSXO\|YYm=	MXG1NEDPxE1?	NVXGXmpPPDhiaB?=		NVG0eFlvUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>?	MX[yOFczPzZ4MB?=
MG-63	MkexSpVv[3Srb36gRZN{[Xl?	NV;YPG04PTBizszN	MnHkOFghcA>?		MXzJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	NHHtbVAzPDd{N{[2NC=>
SJSA-1	MonWSpVv[3Srb36gRZN{[Xl?	MnfyOVAh\|ryP	NE\nPG81QCCq		MV7Jcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	MkPlNlQ4Ojd4NkC=
Saos-2	MlvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mn:zOVAh\|ryP	MmXjOFghcA>?		MYXJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>?	NXrod3R6OjR5Mke2OlA>
MG-63	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHLBb4M2OCEQvF2=	MkP5OFghcA>?		M4roT2lvcGmkaYTzJINmdGxidnnhZoltcXS7	NVu5W2xiOjR5Mke2OlA>
SJSA-1	NHrLPINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVv5W4szPTBizszN	M2TYUFQ5KGh?		NXTzR\|c2UW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	M3vaZVI1PzJ5Nk[w
FaDu	Mlz2SpVv[3Srb36gRZN{[Xl?	MV61JO69VQ>?	NXi1eJFZOjRiaB?=	NFPyPWFFVVOR	NXHEVGo4WmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	MlLjNlQ3OzFzNEe=
EMT6	MWfGeY5kfGmxbjDBd5NigQ>?	NUfub5poPSEQvF2=	M2nud\|I1KGh?	NIrQNIZFVVOR	M4r0THJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	NYnRZYUyOjR4M{GxOFc>
HCT116	NYr2e\|JWTnWwY4Tpc44hSXO\|YYm=	NXzPVJlIPSEQvF2=	NULK[\|FEOjRiaB?=	M3\JeWROW09?	M4HUTnJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	NFfIRmUzPDZ\|MUG0Oy=>
U87	NVHaZ\|NmTnWwY4Tpc44hSXO\|YYm=	MWC1JO69VQ>?	M3P0VFI1KGh?	NXzaTIdwTE2VTx?=	MY\S[YR2[2W\|IH;4fYdmdiClb37zeY1xfGmxbh?=	NEm1ZmEzPDZ\|MUG0Oy=>
GBM	NHjKdGJCeG:ydH;zbZMhSXO\|YYm=	NEXVUIUz\|ryP	NF;HVpo1QGh?	M2XMb2ROW09?	M{\nS4lv\HWlZXSgbIlocGW{IHzleoVteyCxZjDhdI9xfG:\|aYOsJIFv\CCmZXPy[YF{\WRiY3XscEB3cWGkaXzpeJk>	MXGyOFUxODR7Mh?=
BON	MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mnr3NU02\|ryP	NXniTJd5PzKq		MkXi[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=>	NXjKcnNYOjR2NEO1NlM>
BON	M4rONWFxd3C2b4Ppd{BCe3OjeR?=	NH7XNVMyNTYQvF2=	NGiyVIszPGh?		NUfUfm9RcW6lcnXhd4V{KGGyb4D0c5Nqew>?	NXW1fZJwOjR2NEO1NlM>
H1975	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYqwMlMuQS54zszN	MkjyO\|Jp	M{nEdWROW09?	MXrJR\|UxRTFwM{i1{txO	MoGzNlQ{Ozd6NE[=
H1975	NF\mbJNCeG:ydH;zbZMhSXO\|YYm=	M{TLUVLPxE1?	MV[yOIg>	NUfqdpVZTE2VTx?=	M4fZfYlv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6	NYn5OmRmOjR\|M{e4OFY>
T-ALL	MnPtRZBweHSxc3nzJGF{e2G7	MoTBZoV1f2WnbjCxMlQh[W6mIEWuN{BuVSCjdDCyOIgh[W6mIECuPUBidmRiNT61JI1OKGG2IES4bEBqdiCmaX\m[ZJmdnRiY3XscEBtcW6n	MnfCNlQhd3JiNEjo	MWnEUXNQ	NWPafYJz[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM>	NFLOboszPDNzMEezOi=>
BCR-ABL	NWTOcmtLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4\6NVAvOjVvMUFOwG0>	Mkn1OIQ>		MUnzbYdvcW[rY3HueIx6KGmwaHnibZQh[2WubDDwdo9tcW[ncnH0bY9v	MUWyOFI1PDZzMh?=
LC-1/SQSF	MnLnSpVv[3Srb36gRZN{[Xl?	MVez{txO	NH:0SHAzPGh?	M3vsR2ROW09?	M37s[oRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=>	NH3lb2QzOzl6MEC5Ny=>
Primary CLL cells	MXHBdI9xfG:\|aYOgRZN{[Xl?	MV:xMVEx\|ryP	MlXPOFhp		M1TCTIlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM>	NWLPdFV1OjN6NUC4NFc>
Primary CLL cells	M4iyRmtqdmG\|ZTDBd5NigQ>?	MUiy{txO	NHziXHQ{OG2rbh?=		NGPK[Zdl\WO{ZXHz[YQhWEl\|SzDhZ5Rqfmm2eR?=	MVmyN\|g2ODhyNx?=
Primary CLL cells	M3ruS2N6fG:2b4jpZ{BCe3OjeR?=	NYi0coZXOs7:TR?=	M1X1UVI1cA>?		M2DXTIlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm=	MY[yN\|g2ODhyNx?=
human NSCLC cell lines	MYrBdI9xfG:\|aYOgRZN{[Xl?	NIf4fFAxNjF{NT20{txO	NXq5NVhKOjSq	M4DVfmROW09?	NH2zb2pKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=>	NH[1[XkzOzV4MkS3Ni=>
human HCC cell lines	M1jJSWNmdGxidnnhZoltcXS7IHHzd4F6	NXmzc45kOC5yMEWtNe69VQ>?	MVu0PIg>		MWXJR\|UxRTIQvF2=	M1:3[FI{PDh7OUm5
Huh7	MofkT4lv[XOnIFHzd4F6	MkjYNe69VQ>?	MknuOFhp		M1PBWJNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=>	NVXVe2x5OjN2OEm5PVk>
SK-HEP1	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NF3SZXAyNTJyzszN	MlnLO\|Jp	MYjEUXNQ	MV7JR\|Ux97zeMd88US=>	NWW0eJl4OjN2N{mxN\|Y>
786-0	MkfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NH3sNogyNTJyzszN	MYi3Nog>	NFT3cpBFVVOR	MlLMTWM2OO,:nEJOwG0>	MnewNlM1PzlzM{[=
JVM2	MXjDfZRwfG:6aXPpeJkh[XO\|YYm=	NU\4S5RxOC5{LUKw{txO	NIXoSZU4Omh?	M33ZUWROW09?	MUXJR\|UxRTBwOd88US=>	M3TaO\|I{OjN6NkO5
EHEB	NGewOVNEgXSxdH;4bYNqfHliYYPzZZk>	M1zZW\|AvOi1{MN88US=>	MnGxO\|Jp	NX;CTIdwTE2VTx?=	NXj6R\|NSUUN3ME2wMlfPxE1?	MofaNlMzOzh4M{m=
MEC2	NIXyUXVEgXSxdH;4bYNqfHliYYPzZZk>	M2XxU\|AvOi1{MN88US=>	Mnz3O\|Jp	MYjEUXNQ	M2jldGlEPTB;MD63{txO	MlK1NlMzOzh4M{m=
primary B-CLL lymphocytes	NXvGZo5VSXCxcITvd4l{KEG\|c3H5	M1ThdGlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV?	NH7KbYozPGh?	MX\EUXNQ	NFTOVohKSzVy78{cN:69VSCob4KgZYxtKHCjdHnlcpR{	M2ja[lI{OjN6NkO5
primary B-CLL lymphocytes	M{HodmtqdmG\|ZTDBd5NigQ>?	NGTuOo9KSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n	MmjCNlRp		NWnVS2RpcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44>	NFrnOoYzOzJ\|OE[zPS=>
human NSCLC	NIPpXZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MljqNE42NTMQvF2=	M3j5VlczcA>?		M3TJN2lEPTB;Md88US=>	MliwNlI4QDF\|OUO=
human NSCLC	NX;vUmtPU2mwYYPlJGF{e2G7	NI\QbXky\|ryP	NVmxXGNuOjSq		M4iwTIlvcGmkaYTzJJRp\SCDa4SvcXRQWiC\|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS=	NH:2T3ozOjd6MUO5Ny=>
Y1 cell line	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXHyZZd5OC5zzszNM\|HPxE1?	NX35Z2NzOjSq	NEXOZ4lFVVOR	NFXnPWRqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?=	Mm\nNlI3QTJ7MES=
PIK3CA-mutant MCF7	NYLhbIJxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MoC5S2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	NHzSPXo4Omh?		M2\SfWdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P	Mo\vNlI3PTN7Nke=
PIK3CA-mutant MCF7	NYnI[W0{U2mwYYPlJGF{e2G7	M3fs[2lEPTB;MUG0xtE{dk1?	NEnjPVY4Omh?		NXzsXpJNUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=>	NWTiSG16OjJ4NUO5Olc>
MCF7-myr-Akt	NGr0bZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFSyXVJIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?=	MXu3Nog>		MWjHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>?	NXy2dIlxOjJ4NUO5Olc>
colon cancer cell lines	NInTcnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYWwMVEx\|ryP	MkLmO\|Jp	MmfWSG1UVw>?	NHvSclJKSzVyPUJOwG0>	MlzwNlI2PDN6NUe=
gastric cancer cell lines	M2T3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MX6wMVEx\|ryP	MYm3Nog>	NGfZU3pFVVOR	Ml\qTWM2OD1{LUZOwG0>	NUL2RmNOOjJ3NEO4OVc>
HCT-116/HT-29/MKN-45	MmjLRZBweHSxc3nzJGF{e2G7	M3\TNFLPxE1?	NH73Zpc1QGh?		M2rtPZNpcW[2IHnuJGczKHCqYYPl	Ml2xNlI2PDN6NUe=
HT-29 and HCT-116	NWrWdYJVS2G\|cHHz[UBie3OjeR?=	M4rHU\|XPxE1?	MljzNlRp		MXfpcoR2[2W\|IHPhd5Bie2ViYXP0bZZqfHl?	MlPoNlI2PDN6NUe=
MM cell lines	MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXixNO69VQ>?	NUXmToc1OjSq	NIW0Z\|hFVVOR	M4W4TGlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>?	MnTTNlIzODd2OEW=
ARP-1	M{[xfWFxd3C2b4Ppd{BCe3OjeR?=	NHrZb3AyOM7:TR?=	NUDsNYNMOjSq	NIG4V\|lFVVOR	NF\UVHJqdmS3Y3XzJG1OKGOnbHygZZBweHSxc3nzJJRpem:3Z3igZ4F{eGG\|ZTDhZ5RqfmG2aX;u	NYDCR3E4OjJ{MEe0PFU>
SNU-601	NFzUbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NInrNHQ4Omh?	MYDEUXNQ	NXTxe\|R4UUN3ME2wMlgyPsLzMD6wOlPPxE1?	MofXNlIyPTl6MUS=
SNU-1	NW\HV\|RnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MXi3Nog>	NWLNcIx[TE2VTx?=	MVXJR\|UxRTFwMEiyxtExNjB{ON88US=>	NHzsdm4zOjF3OUixOC=>
SNU-668	MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NGjpc5E4Omh?	NFfKWmJFVVOR	NXP4bnE1UUN3ME2xMlU4QcLzMD6wO\|TPxE1?	MWCyNlE2QThzNB?=
AGS	NYfLOWRqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MnyyO\|Jp	MWHEUXNQ	MmL2TWM2OD1zLkexOOKyOC5zMUhOwG0>	MYiyNlE2QThzNB?=
SNU-216	M{[2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MnGxO\|Jp	MXrEUXNQ	NWrsNlNIUUN3ME2yMlY6OsLzMD6wPFLPxE1?	M3HyR\|IzOTV7OEG0
SNU-5	NYD4SHlMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MnvkO\|Jp	Ml\qSG1UVw>?	NFq2dFZKSzVyPUGuN\|UyyrFyLkC5Ne69VQ>?	MnOwNlIyPTl6MUS=
SNU-638	MoTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MX[3Nog>	MWLEUXNQ	Mmr4TWM2OD1{LkK4NuKyOC5yNUROwG0>	NXK5VHZOOjJzNUm4NVQ>
SNU-16	NFrsfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MlPPO\|Jp	NVPmdmcxTE2VTx?=	M2CzSWlEPTB;MT61O\|PDuTBwMECx{txO	M{fNZVIzOTV7OEG0
SNU-484	NUDXc5hMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2fJVFczcA>?	MmHLSG1UVw>?	MYjJR\|UxRTFwN{K4xtExNjB2Nd88US=>	NHm3WIozOjF3OUixOC=>
SNU-620	NF;GcJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M1P1OlczcA>?	NWfHPJF4TE2VTx?=	NGXmWW1KSzVyPUKuPVM6yrFyLkCwNe69VQ>?	NXS0TIY{OjJzNUm4NVQ>
SNU-719	NHjkV\|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mlu1O\|Jp	MYDEUXNQ	MYjJR\|UxRTNwMEO3xtExNjB\|Mt88US=>	MX2yNlE2QThzNB?=
glioma cell lines	MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYfPZnJIPzKq		NEXjZZZKSzVyPUGtNu69VQ>?	MViyNlA3PTB6MB?=
U87	NXrUd2dLSXCxcITvd4l{KEG\|c3H5	NUDWTG14Os7:TR?=	MU[3Nog>		MXnpcoR2[2W\|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?=	M1SxW\|IzODZ3MEiw

... Click to View More Cell Line Experimental Data

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

Tech Support

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

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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

6 Customer Reviews

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

Choose Your Country or Region

By Signaling Pathways

By product type

Buparlisib (BKM120, NVP-BKM120)

Cited by 41 Publications

6 Customer Reviews

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)