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	MWfDfZRwfG:6aXOgRZN{[Xl?		MUe3NkBp	NGXPdGtFVVOR	MljNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?=	MWKyOFkxODJ4Nh?=
DU145	MXvDfZRwfG:6aXOgRZN{[Xl?		M1j4dlczKGh?	NY\udpltTE2VTx?=	MmTTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCOS1KxJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMEC0N\|Uh\|ryP	MWiyOFkxODJ4Nh?=
A2780	NYqzU4NwS3m2b4TvfIlkKEG\|c3H5		MYe3NkBp	MlK1SG1UVw>?	MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N\|Uh\|ryP	NF64OGYzPDlyMEK2Oi=>
U87MG	NGXudJZEgXSxdH;4bYMhSXO\|YYm=		MV63NkBp	MULEUXNQ	MnnCR5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlk5KM7:TR?=	MlS0NlQ6ODB{Nk[=
A2780	NX;yOIxZTnWwY4Tpc44hSXO\|YYm=		MmPqNUBp	NYTsUm86TE2VTx?=	NVjTfpRRUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlA2PSEQvF2=	M{fsflI1QTByMk[2
DU145	NWTqeZVXTnWwY4Tpc44hSXO\|YYm=		NITiWJEyKGh?	M3fyO2ROW09?	M37WdmlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBFXTF2NTDj[YxteyCqYYLic5JqdmdiTFvCNUBufXSjdHnvckB4cXSqIFXDOVAhd2ZiMD6wO\|Mh\|ryP	MoTuNlQ6ODB{Nk[=
A2780	NYHTUpF5TnWwY4Tpc44hSXO\|YYm=		M2rReFEhcA>?	MV3EUXNQ	M{HCPWlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO\|Qh\|ryP	NEn3NnMzPDlyMEK2Oi=>
MCF7	NWD5RYJiTnWwY4Tpc44hSXO\|YYm=		MlvSNUBp	Mn7PSG1UVw>?	NHTDZohKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR\|UxKG:oIECuNUDPxE1?	M4\HeFI1QTByMk[2
U87MG	NFjxOpVHfW6ldHnvckBCe3OjeR?=		MkTMNUBp	NXP6cZpQTE2VTx?=	M2HqO2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1?	NWPQWZhVOjR7MECyOlY>
A2780	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MVK3NkBp	NUP1c5lLTE2VTx?=	MoPUSWM2OD1yLkWyJO69VQ>?	Mk[1NlQ6ODB{Nk[=
SKMES-1	NG[0dZNEgXSxdH;4bYMhSXO\|YYm=	NV21OZJ6OSEQvF2=	NEHkS3U4OiCq		M1PBXmlv\HWlZYOgZ4VtdCCmZXH0bC=>	NIjH[XgzPjBzM{OxPC=>
H596	M{TlWWZ2dmO2aX;uJGF{e2G7	MX:xJO69VQ>?			NVXWU4FZUW2yYXnyd{Bk\WyuIH3p[5JifGmxbh?=	NUTpZWx5OjZyMUOzNVg>
HCC2450	NWS1TnI5TnWwY4Tpc44hSXO\|YYm=	M3j0SFEh\|ryP			M4nIb2lueGGrcoOgZ4VtdCCrbo\hd4lwdg>?	NVrMVGlzOjZyMUOzNVg>
A549	NFv4fHFHfW6ldHnvckBCe3OjeR?=	MY[1NFAhdk1?	NUTLc\|dnPDhiaB?=	NHzQZnlFVVOR	MU\Jcohq[mm2czDBb5Qh[WO2aY\heIlwdg>?	M2DZWFI2QTN5Mkm5
A549	M3zQeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXv1WYpIOSEQvF2=	NVHacXV3PzJiaB?=	MmnPSG1UVw>?	NWXy[HM3UW6qaXLpeJMh[2WubDDndo94fGh?	M3zjelI2QTN5Mkm5
H522	MnTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoDWNUDPxE1?	MmDXO\|IhcA>?	MoXSSG1UVw>?	MWDJcohq[mm2czDj[YxtKGe{b4f0bC=>	M1\a[lI2QTN5Mkm5
LNCaP	NHv5eVVHfW6ldHnvckBCe3OjeR?=	M2n3SlEh\|ryP			NXzIWIp1W3WycILld5NmeyCyLVHLWEBt\X[nbIO=	MWmyOVM3ODd7OR?=
LNCaP95	NUDwOJpRTnWwY4Tpc44hSXO\|YYm=	M3y0SVEh\|ryP			MoDCV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN?	MmntNlU{PjB5OUm=
HCT-15	M4PufmFxd3Sxc3nzJGF{e2G7	NG\wbpIyOCEQvF2=	NECwTFM1QCCq	Mn3uSG1UVw>?	MlHqTY5lfWOnczDhdI9xfG:\|aYOgbY4hUEOWLUG1JINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	MWCyOVE2OjJ2NR?=
HCT-116	M{nqcWFxd3Sxc3nzJGF{e2G7	NH34N2IyOCEQvF2=	Mn;DOFghcA>?	MYnEUXNQ	MW\JcoR2[2W\|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	M1jnTVI2OTV{MkS1
NCI-H460	NILST4dCeG:2b4Ppd{BCe3OjeR?=	M3zDN\|ExKM7:TR?=	M{D5RlQ5KGh?	NHOySmxFVVOR	NV3PeXRFUW6mdXPld{BieG:ydH;zbZMhcW5iTlPJMWg1PjBiY3XscJMhcGG{Yn;1dolv\yCSSVuzR2EhcG:2c4DveEBufXSjdHnvci=>	NEH0ZlczPTF3MkK0OS=>
SKOV-3	NUDSdnhwSXCxdH;zbZMhSXO\|YYm=	MXKxNEDPxE1?	NI\DRWc1QCCq	NHHXSodFVVOR	M2fRcWlv\HWlZYOgZZBweHSxc3nzJIlvKFONT2[tN{Bk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	NFfScHozPTF3MkK0OS=>
BSY-1	MmrnRZBwfG:\|aYOgRZN{[Xl?	NXzPbWNoOTBizszN	NYL3clJ5PDhiaB?=	MVHEUXNQ	MVrJcoR2[2W\|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT\|NESSCqb4TzdI91KG23dHH0bY9v	M4nJSVI2OTV{MkS1
MKN-1	NETmeIpCeG:2b4Ppd{BCe3OjeR?=	Ml24NVAh\|ryP	MkG3OFghcA>?	M1nsS2ROW09?	NILmeolKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	NFf5Ro0zPTF3MkK0OS=>
NCI-H522	NEWxeHVCeG:2b4Ppd{BCe3OjeR?=	MnrpNVAh\|ryP	M1f0Z\|Q5KGh?	MVPEUXNQ	Mo\MTY5lfWOnczDhdI9xfG:\|aYO=	NH6yTY8zPTF3MkK0OS=>
OVCAR-3	M4PKbWFxd3Sxc3nzJGF{e2G7	MU[xNEDPxE1?	MUK0PEBp	MorvSG1UVw>?	MYXJcoR2[2W\|IHHwc5B1d3Orcx?=	NF7HfG8zPTF3MkK0OS=>
HBC-5	MVHBdI91d3OrczDBd5NigQ>?	MVWxNEDPxE1?	NGr3[ZQ1QCCq	NYPtd4ZoTE2VTx?=	MX3JcoR2[2W\|IHHwc5B1d3Orcx?=	NXvIPWJzOjVzNUKyOFU>
RXF-631L	Mn60RZBwfG:\|aYOgRZN{[Xl?	NV7FUpdTOTBizszN	MWC0PEBp	MXvEUXNQ	NIr6T2lKdmS3Y3XzJIFxd3C2b4Ppdy=>	MmHTNlUyPTJ{NEW=
MKN-45	NFvHdYRCeG:2b4Ppd{BCe3OjeR?=	MmWxNVAh\|ryP	Mo\mOFghcA>?	M1TBWmROW09?	MYTJcoR2[2W\|IHHwc5B1d3Orcx?=	NUPYUodzOjVzNUKyOFU>
BON-1	NYnhUYdRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWDOUI1pPTByIH7N	NGn5cZoyOCCm	MUTEUXNQ	NYTLPIppUW6qaXLpeJMh[2WubDDndo94fGh?	MnPxNlUxOjZ{OUK=
BON-1	M4jlPWZ2dmO2aX;uJGF{e2G7	NHvCc2g2ODBibl2=	MlnROEBp	MmTxSG1UVw>?	MmXqTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?=	MV6yOVAzPjJ7Mh?=
QGP-1	M4C4NGZ2dmO2aX;uJGF{e2G7	NFG0O\|A2ODBibl2=	MWC0JIg>	M2XEO2ROW09?	NIS4WIVKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez	NWXwe5lOOjVyMk[yPVI>
Huh7	NYLibmhDTnWwY4Tpc44hSXO\|YYm=	M4DD[VEh\|ryP	NGXyZ3AyKGh?	MoLDSG1UVw>?	NUXmUnpPUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S=	M1P0dVI2ODB2NECz
BNL	MVTGeY5kfGmxbjDBd5NigQ>?	MmPUNUDPxE1?	MoLONUBp	Mn;qSG1UVw>?	NFW5elJKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhWzZ?	Mk[zNlUxODR2MEO=
MDA-MB-175	MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1f2VlEh\|ryP	MoDEOUBl	M1LBSmROW09?	NFn1TFZKSzVyPEGg{txO	NXTBO4ZHOjR6N{m3PVY>
MDA-MB-134	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGHRZ3EyKM7:TR?=	MX[1JIQ>	MX;EUXNQ	MXnJR\|UxRDFizszN	NXvXPXllOjR6N{m3PVY>
HCC1500	MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWHaXlQ1OSEQvF2=	M3T3blUh\A>?	M4PyNGROW09?	MU\JR\|UxRDFizszN	NF;EbJAzPDh5OUe5Oi=>
EFM-19	NGPMUYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnPYNUDPxE1?	MUO1JIQ>	MV\EUXNQ	NGDFc4NKSzVyPEGg{txO	MmfrNlQ5Pzl5OU[=
ZR-75-30	NIH6VHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV3KW415OSEQvF2=	M{jLdlUh\A>?	NV;EdHEyTE2VTx?=	NEjiVXRKSzVyPEGg{txO	NEWyWZEzPDh5OUe5Oi=>
MDA-MB-361	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4[wPVEh\|ryP	M165blUh\A>?	M4jP[GROW09?	M1rMV2lEPTB:MTFOwG0>	MmPCNlQ5Pzl5OU[=
T-47D	MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkHiNUDPxE1?	NYj1O3NJPSCm	MWLEUXNQ	M3LJW2lEPTB:MTFOwG0>	M{\rN\|I1QDd7N{m2
SK-BR-3	M2TnZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Ml7SNUDPxE1?	MVS1JIQ>	Mof5SG1UVw>?	MXnJR\|UxRDFizszN	MVmyOFg4QTd7Nh?=
UACC-732	MlzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NH25fm8yKM7:TR?=	M3u4VFUh\A>?	NXXTblMxTE2VTx?=	MnPNTWM2ODxzIN88US=>	MVuyOFg4QTd7Nh?=
BT-474	M3TGcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkTvNUDPxE1?	NYiwO3JPPSCm	NFPWfGVFVVOR	Ml\TTWM2ODxzIN88US=>	M1TmSFI1QDd7N{m2
HCC202	M13Yb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NITLOHQyKM7:TR?=	MXG1JIQ>	NXLQU3FxTE2VTx?=	M4DFZmlEPTB:MTFOwG0>	NEfpN3ozPDh5OUe5Oi=>
MCF7	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFGw[lYyKM7:TR?=	NXvZeYdFPSCm	MWXEUXNQ	NFHFTWhKSzVyPEGg{txO	MmDFNlQ5Pzl5OU[=
MDA-MB-415	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mn\lNUDPxE1?	MUK1JIQ>	MoDqSG1UVw>?	M2ixfmlEPTB:MTFOwG0>	MX6yOFg4QTd7Nh?=
MDA-MB-453	MlP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmnHNUDPxE1?	MkfxOUBl	MkjnSG1UVw>?	MU\JR\|UxRDFizszN	NX7GW3BjOjR6N{m3PVY>
ZR-75-1	MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUWxJO69VQ>?	NEX2RmE2KGR?	Mkn4SG1UVw>?	M2L4TmlEPTB:MTFOwG0>	Mn7pNlQ5Pzl5OU[=
HCC38	NUCw[HdRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYWxJO69VQ>?	M1zMV\|Uh\A>?	MWfEUXNQ	NFnMdG1KSzVyPEGg{txO	MlHCNlQ5Pzl5OU[=
HCC1419	MoT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVS5S29SOSEQvF2=	NFTCZ242KGR?	Mk[5SG1UVw>?	M4niZWlEPTB:MTFOwG0>	M1jFWFI1QDd7N{m2
UACC-812	NV3CXVRuT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1\zWlEh\|ryP	M4nWdVUh\A>?	NYGxfHliTE2VTx?=	M12yO2lEPTB:MTFOwG0>	NGLRO3YzPDh5OUe5Oi=>
HCC1187	MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHezO3oyKM7:TR?=	Mn3POUBl	MWLEUXNQ	NGrQOHVKSzVyPEGg{txO	MknuNlQ5Pzl5OU[=
KPL-1	NFrWboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoP0NUDPxE1?	NVrkZYY2PSCm	MYfEUXNQ	MoLrTWM2ODxzIN88US=>	MnnJNlQ5Pzl5OU[=
SUM-225	NUnzU\|RlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGTYTWUyKM7:TR?=	MlLkOUBl	MlzqSG1UVw>?	M323WWlEPTB:MTFOwG0>	NX7te3Z2OjR6N{m3PVY>
EFM-192A	MmXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlvDNUDPxE1?	MXq1JIQ>	NHHnZ3JFVVOR	MWXJR\|UxRDFizszN	Mnf1NlQ5Pzl5OU[=
JIMT-1	NV7aRY5YT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVPPTZdYOSEQvF2=	MWC1JIQ>	MXHEUXNQ	NUHr[IJuUUN3MEyxJO69VQ>?	M2XwUlI1QDd7N{m2
HCC1143	Mof5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXHtXGMxOSEQvF2=	M{\qelUh\A>?	NHnUPXdFVVOR	MlfQTWM2ODxzIN88US=>	NX7ld5RNOjR6N{m3PVY>
HCC2218	M4nIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NW\RTW9[OSEQvF2=	MWi1JIQ>	NFvxTWRFVVOR	NXHVeotOUUN3MEyxJO69VQ>?	NHPsWnMzPDh5OUe5Oi=>
MDA-MB-468	MoHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MV[xJO69VQ>?	MWG1JIQ>	Mn;KSG1UVw>?	MnO3TWM2ODxzIN88US=>	M{PUSlI1QDd7N{m2
BT-20	NHjDOGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYCxJO69VQ>?	MWG1JIQ>	M4PsOmROW09?	M{DRbmlEPTB:MTFOwG0>	MoHsNlQ5Pzl5OU[=
MDA-MB-435	NXjje4xVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXvEUplCOSEQvF2=	MWq1JIQ>	M4LtR2ROW09?	NF3Eb\|NKSzVyPEGg{txO	NXzWNJVoOjR6N{m3PVY>
BT-549	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Ml[zNUDPxE1?	MWG1JIQ>	Ml;pSG1UVw>?	MVTJR\|UxRDFizszN	NHPHWGgzPDh5OUe5Oi=>
HCC1806	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUmxJO69VQ>?	NYDKS5dsPSCm	MX3EUXNQ	MVvJR\|UxRDFizszN	M3XiSVI1QDd7N{m2
HCC1937	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVH6T3doOSEQvF2=	NHe0RYY2KGR?	MXrEUXNQ	MoX1TWM2ODxzIN88US=>	NGG0PZQzPDh5OUe5Oi=>
Hs578T	NVLyfm02T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVKxJO69VQ>?	MlKzOUBl	NHn2[GNFVVOR	M4i5eGlEPTB:MTFOwG0>	NH\CcI0zPDh5OUe5Oi=>
LN18	M4L5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV3ZZ41KOjBizszN	M1rlSVczKGh?	NV7MSJdrTE2VTx?=	MV;JR\|UxRDVizszN	MVSyOFc1OTB5NB?=
LN229	MkLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXL0VIl4OjBizszN	MnLXO\|IhcA>?	MVjEUXNQ	NH;wOJFKSzVyPEWg{txO	NGLYUmszPDd2MUC3OC=>
LNZ308	NUHJenNHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYjWU2hwOjBizszN	NIToUlE4OiCq	MXLEUXNQ	MnjlTWM2ODx3IN88US=>	NWj5fVJtOjR5NEGwO\|Q>
T98G	NGf3UXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXjCdWdZOjBizszN	MmjOO\|IhcA>?	MnHtSG1UVw>?	M2Px[WlEPTB:NTFOwG0>	NELQfW4zPDd2MUC3OC=>
U87	NWfZZVY4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NELk[HgzOCEQvF2=	M1LxRVczKGh?	NVfTZ3hvTE2VTx?=	MYHJR\|UxRDVizszN	MlHxNlQ4PDFyN{S=
LN18	NIPKRoZHfW6ldHnvckBCe3OjeR?=	MmjCOUDPxE1?	NYHQ[WZEOjRiaB?=	M4TpeGROW09?	Mm\DTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>?	MnvxNlQ4PDFyN{S=
LNZ308	NF;sc5NHfW6ldHnvckBCe3OjeR?=	NHnibWI2KM7:TR?=	NXHSO\|dsOjRiaB?=	NX7jOGRNTE2VTx?=	NGXiTYhKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuW	M4LqV\|I1PzRzMEe0
Saos-2	NXrZZ4FmTnWwY4Tpc44hSXO\|YYm=	NGXDSWE2OCEQvF2=	NX[1bGVnPDhiaB?=		MX;Jcohq[mm2czDj[YxtKGmwdnHzbY9v	M3uyfFI1PzJ5Nk[w
MG-63	MmjRSpVv[3Srb36gRZN{[Xl?	NYPhT4dJPTBizszN	NHPkSIk1QCCq		Ml3VTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	NXSzNIN6OjR5Mke2OlA>
SJSA-1	MkfDSpVv[3Srb36gRZN{[Xl?	Ml2xOVAh\|ryP	MUi0PEBp		NUXCZW03UW6qaXLpeJMh[2WubDDpcpZie2mxbh?=	NHHFbHMzPDd{N{[2NC=>
Saos-2	NX\nc5UzTnWwY4Tpc44hSXO\|YYm=	MYi1NEDPxE1?	M3PWTFQ5KGh?		NELXc5FKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v	MlTFNlQ4Ojd4NkC=
MG-63	NHqzR3BHfW6ldHnvckBCe3OjeR?=	NWHDeHU6PTBizszN	M1vK[\|Q5KGh?		NGDiNGpKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v	M3myN\|I1PzJ5Nk[w
SJSA-1	MkTKSpVv[3Srb36gRZN{[Xl?	MUS1NEDPxE1?	MnXxOFghcA>?		MVvJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	NFG3blUzPDd{N{[2NC=>
Saos-2	MnTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVy1NEDPxE1?	NHLwbXM1QCCq		NIHDUlhKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?=	M3fXd\|I1PzJ5Nk[w
MG-63	M1vZTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkXxOVAh\|ryP	Mm\HOFghcA>?		NFTZO4xKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?=	M3v2eVI1PzJ5Nk[w
SJSA-1	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1\iPVUxKM7:TR?=	MknFOFghcA>?		NXPDSWZmUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	NWK3VXV3OjR5Mke2OlA>
FaDu	NWLjZopLTnWwY4Tpc44hSXO\|YYm=	MkDqOUDPxE1?	MXyyOEBp	MYDEUXNQ	NWizXoRMWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	Mkn0NlQ3OzFzNEe=
EMT6	MorGSpVv[3Srb36gRZN{[Xl?	M2H2SFUh\|ryP	MmrPNlQhcA>?	MmLMSG1UVw>?	MVHS[YR2[2W\|IH;4fYdmdiClb37zeY1xfGmxbh?=	NEfWSHkzPDZ\|MUG0Oy=>
HCT116	MmLZSpVv[3Srb36gRZN{[Xl?	NGHsdZE2KM7:TR?=	MUOyOEBp	NUGwPVFZTE2VTx?=	M3HlWnJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	M1zGblI1PjNzMUS3
U87	MomySpVv[3Srb36gRZN{[Xl?	MYG1JO69VQ>?	NVf4SlI5OjRiaB?=	M3;tWWROW09?	NHHFVXRT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=>	M4HyW\|I1PjNzMUS3
GBM	MnS5RZBweHSxc3nzJGF{e2G7	NHzObFcz\|ryP	NVjMeWdiPDiq	NET0No1FVVOR	NIDMVG1qdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6	MXuyOFUxODR7Mh?=
BON	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFvEZ4EyNTYQvF2=	NITQU3M4Omh?		M4LmfYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44>	NILFdmczPDR2M{WyNy=>
BON	MVHBdI9xfG:\|aYOgRZN{[Xl?	NXnoNmdbOS13zszN	NVn5XlVPOjSq		MkLvbY5kemWjc3XzJIFxd3C2b4Ppdy=>	MVKyOFQ1OzV{Mx?=
H1975	NYfLTlZvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVLiVZN6OC5\|LUmuOu69VQ>?	M{HEXlczcA>?	MUTEUXNQ	Mm[xTWM2OD1zLkO4Oe69VQ>?	MYKyOFM{Pzh2Nh?=
H1975	M37vNmFxd3C2b4Ppd{BCe3OjeR?=	MVyy{txO	NVXSfnc{OjSq	MVnEUXNQ	NW[yeHdocW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl?	M2LCNVI1OzN5OES2
T-ALL	MYDBdI9xfG:\|aYOgRZN{[Xl?	MYDi[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV?	MkC0NlQhd3JiNEjo	NVnuS2NyTE2VTx?=	Ml\zZYZn\WO2czD0bIUhWEl\|SzDwZZRpf2G7IHnuJHQuSUyOIHPlcIwhdGmwZYO=	M4TGdVI1OzFyN{O2
BCR-ABL	M2r6Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoHXNE4zPS1zMN88US=>	NX\OPHFyPGR?		MVzzbYdvcW[rY3HueIx6KGmwaHnibZQh[2WubDDwdo9tcW[ncnH0bY9v	NILVR\|YzPDJ2NE[xNi=>
LC-1/SQSF	MnPuSpVv[3Srb36gRZN{[Xl?	NUnsSHBsO87:TR?=	MV6yOIg>	MWjEUXNQ	NHLVdHhl\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw>	MXeyN\|k5ODB7Mx?=
Primary CLL cells	MV7BdI9xfG:\|aYOgRZN{[Xl?	M1;WT\|EuOTEQvF2=	NUXlbWZWPDiq		NEH6U2FqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{	MnLQNlM5PTB6MEe=
Primary CLL cells	M{HiXmtqdmG\|ZTDBd5NigQ>?	NH\6NZQz\|ryP	MlLhN\|BucW5?		Mn70[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl?	MlfKNlM5PTB6MEe=
Primary CLL cells	M1TmOWN6fG:2b4jpZ{BCe3OjeR?=	MoHBNu69VQ>?	NX7RVGw{OjSq		NXvYe2tHcW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=>	M3rTW\|I{QDVyOEC3
human NSCLC cell lines	NHLBbHlCeG:ydH;zbZMhSXO\|YYm=	M3PnXFAvOTJ3LUVOwG0>	NXi0V3FtOjSq	M4O3NWROW09?	NI\JVGJKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=>	MkOzNlM2PjJ2N{K=
human HCC cell lines	NHjQ[GJE\WyuII\pZYJqdGm2eTDhd5NigQ>?	NVjGVoFLOC5yMEWtNe69VQ>?	NGHUOYU1QGh?		Mnn2TWM2OD1zzszN	NGPhOJgzOzR6OUm5PS=>
Huh7	NF3DSlJMcW6jc3WgRZN{[Xl?	Ml7NNe69VQ>?	Ml3uOFhp		NXHsVpp2e2mpbnpvsKFk[W62bImgdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gRYt1	MYKyN\|Q5QTl7OR?=
SK-HEP1	MkDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEPlOmkyNTJyzszN	MlLpO\|Jp	NVLzbmpMTE2VTx?=	MnzqTWM2OO,:nEJOwG0>	NUXL[GlbOjN2N{mxN\|Y>
786-0	NVK5OYFrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3OwU\|EuOjEQvF2=	MlHxO\|Jp	M2m1fWROW09?	M2\5RmlEPTExvKyx{txO	NGjVZWwzOzR5OUGzOi=>
JVM2	Mm\HR5l1d3SxeHnjbZR6KGG\|c3H5	Moi5NE4zNTJyzszN	NF[1cJk4Omh?	NXXEVIF3TE2VTx?=	MoSxTWM2OD1yLkpOwG0>	MWqyN\|I{QDZ\|OR?=
EHEB	NXLNbXE{S3m2b4TvfIlkcXS7IHHzd4F6	MWewMlIuOjEQvF2=	MXK3Nog>	M4LWZWROW09?	MXPJR\|UxRTBwN988US=>	MkXONlMzOzh4M{m=
MEC2	M371e2N6fG:2b4jpZ4l1gSCjc4PhfS=>	NWfVU3dCOC5{LUKw{txO	NIfGPJQ4Omh?	MXfEUXNQ	M{DJOGlEPTB;MD63{txO	M{TTOlI{OjN6NkO5
primary B-CLL lymphocytes	NES4e4xCeG:ydH;zbZMhSXO\|YYm=	MXXJR\|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m	NYnlcVJCOjSq	MoPVSG1UVw>?	M{DQ[2lEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM>	NXHtcWY6OjN{M{i2N\|k>
primary B-CLL lymphocytes	MUfLbY5ie2ViQYPzZZk>	MmH0TWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>?	Ml7iNlRp		NH7WflNqdmirYnn0d{BxPzCVNlugKkA1TS2EUEGg[ZhxemW\|c3nvci=>	MUWyN\|I{QDZ\|OR?=
human NSCLC	MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF;jWpQxNjVvMt88US=>	MoD1O\|Jp		MkTJTWM2OD1zzszN	NIrqd48zOjd6MUO5Ny=>
human NSCLC	Ml30T4lv[XOnIFHzd4F6	M4S3[\|HPxE1?	MVyyOIg>		NV;kdGk6cW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=>	NWm4UZNTOjJ5OEGzPVM>
Y1 cell line	NGXreIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlzLNE4y\|ryPL{JOwG0>	M4X1U\|I1cA>?	NXzkV5NFTE2VTx?=	M3n6TIlvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy\|	MV[yNlY6OjlyNB?=
PIK3CA-mutant MCF7	NUexRVBHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MljWS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	NWrhWpQ1PzKq		MXjHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO\|NvVQ>?	MVKyNlY2Ozl4Nx?=
PIK3CA-mutant MCF7	M1rn[WtqdmG\|ZTDBd5NigQ>?	MoD6TWM2OD1zMUVCtVNvVQ>?	MXO3Nog>		MUfJR\|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:\|cHjvdplt[XSrb36gcIV3\Wy\|	MYmyNlY2Ozl4Nx?=
MCF7-myr-Akt	M3\GVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3zkVGdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P	M4HhPFczcA>?		NXnCWGwyT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2=	MoH4NlI3PTN7Nke=
colon cancer cell lines	NGfwSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUXBW2ZHOC1zMN88US=>	M{fpNFczcA>?	NILlRnlFVVOR	MnnqTWM2OD1zzszN	MmHINlI2PDN6NUe=
gastric cancer cell lines	NGPlTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1;D[\|AuOTEQvF2=	NIr0eYI4Omh?	NHTlSZZFVVOR	MWXJR\|UxRTJvNd88US=>	MnHINlI2PDN6NUe=
HCT-116/HT-29/MKN-45	NXTqNo1USXCxcITvd4l{KEG\|c3H5	NUnR[FFVOs7:TR?=	MYG0PIg>		NF7XSHd{cGmodDDpckBIOiCyaHHz[S=>	M{KyN\|IzPTR\|OEW3
HT-29 and HCT-116	M1;UO2Nie3Cjc3WgZZN{[Xl?	NIi1Umw2\|ryP	NFjTXYQzPGh?		MXXpcoR2[2W\|IHPhd5Bie2ViYXP0bZZqfHl?	MV[yNlU1Ozh3Nx?=
MM cell lines	M{PpSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2LJe\|Ex\|ryP	NHjHUG4zPGh?	NEftcFJFVVOR	MWnJR\|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U>	MWeyNlIxPzR6NR?=
ARP-1	MX\BdI9xfG:\|aYOgRZN{[Xl?	MVuxNO69VQ>?	Moq3NlRp	MUXEUXNQ	M3uyNYlv\HWlZYOgUW0h[2WubDDhdI9xfG:\|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36=	M2f6WlIzOjB5NEi1
SNU-601	Mk\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYfPVlhFPzKq	MWfEUXNQ	M2TjNmlEPTB;MD64NVbDuTBwME[z{txO	NEK5T40zOjF3OUixOC=>
SNU-1	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NH;nUpM4Omh?	MmDkSG1UVw>?	MVLJR\|UxRTFwMEiyxtExNjB{ON88US=>	NHPSdHUzOjF3OUixOC=>
SNU-668	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXryZ\|h7PzKq	M4jD[WROW09?	MVnJR\|UxRTFwNUe5xtExNjB5NN88US=>	MXKyNlE2QThzNB?=
AGS	NUHOdHJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NUHDNZRiPzKq	MmnuSG1UVw>?	NIPINJRKSzVyPUGuO\|E1yrFyLkGxO:69VQ>?	NXH6RoprOjJzNUm4NVQ>
SNU-216	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NUS1ZXV3PzKq	MoLISG1UVw>?	M3T0NWlEPTB;Mj62PVLDuTBwMEiy{txO	NEm0VFkzOjF3OUixOC=>
SNU-5	M{\BZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MVO3Nog>	NHro[I1FVVOR	M3fVNGlEPTB;MT6zOVHDuTBwMEmx{txO	NHLIb5czOjF3OUixOC=>
SNU-638	NHPEXXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NGTFNHQ4Omh?	M1q2NGROW09?	M3\rTWlEPTB;Mj6yPFLDuTBwMEWz{txO	MmToNlIyPTl6MUS=
SNU-16	NWXLV4t2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NYjTO5dDPzKq	MYHEUXNQ	M3HmbGlEPTB;MT61O\|PDuTBwMECx{txO	NHrqOG0zOjF3OUixOC=>
SNU-484	NUDVS255T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NXnYR5NJPzKq	MofJSG1UVw>?	NITzVIdKSzVyPUGuO\|I5yrFyLkC0Oe69VQ>?	M3Xs[lIzOTV7OEG0
SNU-620	M1u1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MnjEO\|Jp	M4ThWWROW09?	NH;MSmZKSzVyPUKuPVM6yrFyLkCwNe69VQ>?	NEHMe2IzOjF3OUixOC=>
SNU-719	NGHzcJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M{fq[FczcA>?	MlzrSG1UVw>?	Mmr2TWM2OD1\|LkCzO:KyOC5yM{NOwG0>	NEfJ[HozOjF3OUixOC=>
glioma cell lines	MnflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NE[0T4Q4Omh?		MmLLTWM2OD1zLUNOwG0>	MnrqNlIxPjVyOEC=
U87	Ml;URZBweHSxc3nzJGF{e2G7	MV2y{txO	NXf6d3ZNPzKq		MmLXbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO=	NUGwPVN2OjJyNkWwPFA>

... 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.
Selective PI3K Inhibitors

TGX-221 : p110β-specific, IC50=5 nM.
Most Potent PI3K Inhibitor

BEZ235 (NVP-BEZ235, Dactolisib) : p110α/γ/δ/β, IC50=4 nM/5 nM/7 nM/75 nM.
FDA-approved PI3K Inhibitor

CAL-101 (Idelalisib, GS-1101) : Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.
Newest PI3K Inhibitor

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

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Taselisib (GDC 0032) ^New

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)