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	MnG4R5l1d3SxeHnjJGF{e2G7		NUL6W2Z2PzJiaB?=	M2TrTmROW09?	NEfSbZBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN	MX6yOFkxODJ4Nh?=
DU145	MnnUR5l1d3SxeHnjJGF{e2G7		Mn7BO\|IhcA>?	NF7V[VZFVVOR	MnHSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCOS1KxJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMEC0N\|Uh\|ryP	MUGyOFkxODJ4Nh?=
A2780	M4HI[mN6fG:2b4jpZ{BCe3OjeR?=		NIHGcFY4OiCq	MlPUSG1UVw>?	NXXTXlZ5S3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjN3IN88US=>	MXKyOFkxODJ4Nh?=
U87MG	NWXNbpZNS3m2b4TvfIlkKEG\|c3H5		NELyVYg4OiCq	MmXTSG1UVw>?	MlGzR5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlk5KM7:TR?=	NVn4OJFJOjR7MECyOlY>
A2780	NGPv[GlHfW6ldHnvckBCe3OjeR?=		MlroNUBp	MnjJSG1UVw>?	MVvJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:\|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>?	NUHYOVdPOjR7MECyOlY>
DU145	MX\GeY5kfGmxbjDBd5NigQ>?		M3q0TFEhcA>?	NIfnTZBFVVOR	MkDTTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1?	MVmyOFkxODJ4Nh?=
A2780	M1vCWWZ2dmO2aX;uJGF{e2G7		MX6xJIg>	M1\JWmROW09?	M1;kb2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO\|Qh\|ryP	M1\mO\|I1QTByMk[2
MCF7	Mk\LSpVv[3Srb36gRZN{[Xl?		NInsNIcyKGh?	M1H6T2ROW09?	M17OZ2lvcGmkaYTpc44hd2ZiUFmzT4FteGijIFW1OFVMKG23dHHueE1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6xJO69VQ>?	NWC3e\|AzOjR7MECyOlY>
U87MG	M3fCVmZ2dmO2aX;uJGF{e2G7		MoDuNUBp	NVT6VlRrTE2VTx?=	M37BWmlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1?	NF\1cVMzPDlyMEK2Oi=>
A2780	NHfScohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NH\ZZVg4OiCq	Mo\3SG1UVw>?	MVnFR\|UxRTBwNUKg{txO	Mor4NlQ6ODB{Nk[=
SKMES-1	NWGyd3V{S3m2b4TvfIlkKEG\|c3H5	NWLqTG1DOSEQvF2=	NGjxS4E4OiCq		NV\H[VF[UW6mdXPld{Bk\WyuIHTlZZRp	NEfpUIUzPjBzM{OxPC=>
H596	MnK1SpVv[3Srb36gRZN{[Xl?	M2\x[\|Eh\|ryP			MXPJcZBicXK\|IHPlcIwhdWmpcnH0bY9v	NVXoSoV2OjZyMUOzNVg>
HCC2450	MWTGeY5kfGmxbjDBd5NigQ>?	MYSxJO69VQ>?			MkK2TY1x[Wm{czDj[YxtKGmwdnHzbY9v	MX6yOlAyOzNzOB?=
A549	NVfnfo5DTnWwY4Tpc44hSXO\|YYm=	MorSOVAxKG6P	MUe0PEBp	NXnRXlNMTE2VTx?=	MXrJcohq[mm2czDBb5Qh[WO2aY\heIlwdg>?	NYTVd49nOjV7M{eyPVk>
A549	MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYCxJO69VQ>?	NGrGOW84OiCq	MUDEUXNQ	MmLNTY5pcWKrdIOgZ4VtdCCpcn;3eIg>	M3;TWVI2QTN5Mkm5
H522	MnPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NU\WWVJMOSEQvF2=	NVvuT4JSPzJiaB?=	NGPiWmFFVVOR	MULJcohq[mm2czDj[YxtKGe{b4f0bC=>	NYHPdVRUOjV7M{eyPVk>
LNCaP	M17zXWZ2dmO2aX;uJGF{e2G7	MWOxJO69VQ>?			M4fySXN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy\|	MkHBNlU{PjB5OUm=
LNCaP95	MX3GeY5kfGmxbjDBd5NigQ>?	MYmxJO69VQ>?			M4nld3N2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy\|	NXjFWVZPOjV\|NkC3PVk>
HCT-15	NUXpc5FWSXCxdH;zbZMhSXO\|YYm=	MYCxNEDPxE1?	MYO0PEBp	MWLEUXNQ	MlPrTY5lfWOnczDhdI9xfG:\|aYOgbY4hUEOWLUG1JINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	MWGyOVE2OjJ2NR?=
HCT-116	M4TsfmFxd3Sxc3nzJGF{e2G7	MnO1NVAh\|ryP	MlPwOFghcA>?	MlnmSG1UVw>?	M3jUS2lv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	NEXhZmszPTF3MkK0OS=>
NCI-H460	M3Pid2Fxd3Sxc3nzJGF{e2G7	M4\mZVExKM7:TR?=	NGPKV2k1QCCq	NV7JV4dPTE2VTx?=	M3TuSWlv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36=	NWTWdYlyOjVzNUKyOFU>
SKOV-3	MlGxRZBwfG:\|aYOgRZN{[Xl?	NV6zXJg{OTBizszN	NWXtSHo6PDhiaB?=	NGD0cWhFVVOR	NFG0V3BKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCVS1;WMVMh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	MYqyOVE2OjJ2NR?=
BSY-1	NUTyUGpWSXCxdH;zbZMhSXO\|YYm=	NWG0ZpZ4OTBizszN	M4P1Z\|Q5KGh?	NEm3bJlFVVOR	NVWzepRGUW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	M4T2T\|I2OTV{MkS1
MKN-1	NFKwO5ZCeG:2b4Ppd{BCe3OjeR?=	NWTwW5htOTBizszN	M3vwNFQ5KGh?	Ml:zSG1UVw>?	NXT5eVlmUW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt\|Q1GgbI91e3CxdDDteZRifGmxbh?=	MmnzNlUyPTJ{NEW=
NCI-H522	Ml3KRZBwfG:\|aYOgRZN{[Xl?	MlHFNVAh\|ryP	MlPOOFghcA>?	MmDDSG1UVw>?	NXribm1qUW6mdXPld{BieG:ydH;zbZM>	NF32WZozPTF3MkK0OS=>
OVCAR-3	MmPmRZBwfG:\|aYOgRZN{[Xl?	MnzyNVAh\|ryP	NXH6VFc1PDhiaB?=	NUPOOotoTE2VTx?=	MmryTY5lfWOnczDhdI9xfG:\|aYO=	NEjWXIszPTF3MkK0OS=>
HBC-5	MUnBdI91d3OrczDBd5NigQ>?	MoP5NVAh\|ryP	MnjHOFghcA>?	Mn75SG1UVw>?	MWLJcoR2[2W\|IHHwc5B1d3Orcx?=	MXGyOVE2OjJ2NR?=
RXF-631L	M{CyNGFxd3Sxc3nzJGF{e2G7	NHPhRWIyOCEQvF2=	NFnMToc1QCCq	MVLEUXNQ	MXTJcoR2[2W\|IHHwc5B1d3Orcx?=	NHuwTGgzPTF3MkK0OS=>
MKN-45	M{fJZWFxd3Sxc3nzJGF{e2G7	NWnXTmNyOTBizszN	Ml3KOFghcA>?	NIeyRldFVVOR	NYq2Nm9pUW6mdXPld{BieG:ydH;zbZM>	M1;uWlI2OTV{MkS1
BON-1	NGK0U5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGjHV4g2ODBibl2=	Mnv0NVAh\A>?	NIrYWG9FVVOR	M4j0c2lvcGmkaYTzJINmdGxiZ4Lve5Rp	M33WRlI2ODJ4Mkmy
BON-1	NIHzeXlHfW6ldHnvckBCe3OjeR?=	NXfSUHlsPTByIH7N	NXG1SXlQPCCq	NGOx[HVFVVOR	NWnRNlVlUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ\|MEigZY5lKFOnckS3Ny=>	M{TSdlI2ODJ4Mkmy
QGP-1	NE\EVIJHfW6ldHnvckBCe3OjeR?=	NXm5TWR[PTByIH7N	Mn:xOEBp	NYXXV5JxTE2VTx?=	NInzNmpKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez	MmrDNlUxOjZ{OUK=
Huh7	MmLoSpVv[3Srb36gRZN{[Xl?	MorLNUDPxE1?	NXH2XngzOSCq	MUfEUXNQ	NG\NTVlKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhSUuWIHH0JHNmejR5NB?=	NVTtfpR7OjVyMES0NFM>
BNL	NVGybYFrTnWwY4Tpc44hSXO\|YYm=	M370RVEh\|ryP	Ml\TNUBp	MULEUXNQ	M4Tt[GlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>?	NFXmSXgzPTByNESwNy=>
MDA-MB-175	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGr0T5UyKM7:TR?=	MYm1JIQ>	M1ToVWROW09?	Mni1TWM2ODxzIN88US=>	NXnx[ZZtOjR6N{m3PVY>
MDA-MB-134	NGGz[VlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVSzd3VuOSEQvF2=	NVjoZWVLPSCm	NUfhPIZqTE2VTx?=	NF3ZSXFKSzVyPEGg{txO	NIXBVW4zPDh5OUe5Oi=>
HCC1500	NY[zclVUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnvQNUDPxE1?	NUDLfoZDPSCm	M2Dnb2ROW09?	MkjTTWM2ODxzIN88US=>	MV6yOFg4QTd7Nh?=
EFM-19	M4rU[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWDrSnJtOSEQvF2=	M1jZelUh\A>?	NGr2cINFVVOR	Mn3UTWM2ODxzIN88US=>	MlHENlQ5Pzl5OU[=
ZR-75-30	M2jVNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NITLS5UyKM7:TR?=	NGW1OGk2KGR?	MmnVSG1UVw>?	MnnvTWM2ODxzIN88US=>	M3H6PFI1QDd7N{m2
MDA-MB-361	NIrDVZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3TBVVEh\|ryP	MUW1JIQ>	M37JZWROW09?	NIPqR2dKSzVyPEGg{txO	MVGyOFg4QTd7Nh?=
T-47D	NFfFbXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFfae3cyKM7:TR?=	M1y5c\|Uh\A>?	MonkSG1UVw>?	MofwTWM2ODxzIN88US=>	M3TkeVI1QDd7N{m2
SK-BR-3	MoXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoThNUDPxE1?	MVS1JIQ>	MnjKSG1UVw>?	MXrJR\|UxRDFizszN	NEj0e3kzPDh5OUe5Oi=>
UACC-732	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlK2NUDPxE1?	NW[2SoZ2PSCm	Ml3VSG1UVw>?	M1PQeWlEPTB:MTFOwG0>	MljoNlQ5Pzl5OU[=
BT-474	NE\WflFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV:xJO69VQ>?	Mom4OUBl	Mm\RSG1UVw>?	NIXRNlRKSzVyPEGg{txO	MX6yOFg4QTd7Nh?=
HCC202	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4P4PVEh\|ryP	MnHsOUBl	M{X6fGROW09?	MoPlTWM2ODxzIN88US=>	NWHGOoR1OjR6N{m3PVY>
MCF7	Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXGxJO69VQ>?	NHHSfpU2KGR?	MUXEUXNQ	M1ri[WlEPTB:MTFOwG0>	NWfNWlgzOjR6N{m3PVY>
MDA-MB-415	MoHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWixJO69VQ>?	Mnf2OUBl	NETERllFVVOR	MXvJR\|UxRDFizszN	MYiyOFg4QTd7Nh?=
MDA-MB-453	Mn;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVuxJO69VQ>?	M2i3TFUh\A>?	MY\EUXNQ	MX3JR\|UxRDFizszN	M{nlZ\|I1QDd7N{m2
ZR-75-1	NYj1bIVCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV\WVndLOSEQvF2=	NVrNdYJmPSCm	MX3EUXNQ	NEHJWFZKSzVyPEGg{txO	M37a[VI1QDd7N{m2
HCC38	M{LQdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWrsNndCOSEQvF2=	NHXsN4U2KGR?	M2HjXWROW09?	MV\JR\|UxRDFizszN	M{X3OFI1QDd7N{m2
HCC1419	M17pWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWOyb2U5OSEQvF2=	NYXHbotjPSCm	M{jEUmROW09?	MYjJR\|UxRDFizszN	NH71PJczPDh5OUe5Oi=>
UACC-812	M{LjR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWGxJO69VQ>?	MoDVOUBl	M4jhUWROW09?	NHT0cmRKSzVyPEGg{txO	Mly1NlQ5Pzl5OU[=
HCC1187	NFLJ[\|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2naTVEh\|ryP	NVLBbI5GPSCm	NFO5ZmVFVVOR	Ml\UTWM2ODxzIN88US=>	NWnPPXBNOjR6N{m3PVY>
KPL-1	NGXG[3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnX0NUDPxE1?	NX3KU3hNPSCm	NXLEdZRmTE2VTx?=	NHTrcHBKSzVyPEGg{txO	NWDjcoZoOjR6N{m3PVY>
SUM-225	M1H2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYX1RnNmOSEQvF2=	NWfsNpM2PSCm	Mm[0SG1UVw>?	NXvwR2xlUUN3MEyxJO69VQ>?	NWP5SYhwOjR6N{m3PVY>
EFM-192A	M3jKSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NULUS4dpOSEQvF2=	M1jZR\|Uh\A>?	MXrEUXNQ	M3ewTmlEPTB:MTFOwG0>	Mn7QNlQ5Pzl5OU[=
JIMT-1	NHXtXHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVmxJO69VQ>?	NWTNSWJmPSCm	MWHEUXNQ	MX7JR\|UxRDFizszN	M2jkNFI1QDd7N{m2
HCC1143	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFH5NYYyKM7:TR?=	M2nY[VUh\A>?	M36xUmROW09?	Mmf5TWM2ODxzIN88US=>	M17nUFI1QDd7N{m2
HCC2218	M4KzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3fwRVEh\|ryP	MXi1JIQ>	M37GRWROW09?	Mk\wTWM2ODxzIN88US=>	M1rVVVI1QDd7N{m2
MDA-MB-468	M1\rTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1nvelEh\|ryP	NG\3dIg2KGR?	NGXabFJFVVOR	MmG2TWM2ODxzIN88US=>	MYqyOFg4QTd7Nh?=
BT-20	NUDWNJNvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnPINUDPxE1?	NV7RNZVrPSCm	M1K2UmROW09?	MkHnTWM2ODxzIN88US=>	NFjRTpAzPDh5OUe5Oi=>
MDA-MB-435	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXPIS2c4OSEQvF2=	NFHoW4k2KGR?	M1zxT2ROW09?	M4PBfGlEPTB:MTFOwG0>	M3PqOFI1QDd7N{m2
BT-549	NEXT[YZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXmxJO69VQ>?	M{LN[lUh\A>?	NF\Te2ZFVVOR	M4fGRmlEPTB:MTFOwG0>	NGfuXnozPDh5OUe5Oi=>
HCC1806	M3jPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWixJO69VQ>?	NEHROYI2KGR?	NGPKcXFFVVOR	MX;JR\|UxRDFizszN	M4nIR\|I1QDd7N{m2
HCC1937	NYXOSWM2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4T6NVEh\|ryP	NH:zelk2KGR?	M3L0dWROW09?	M2L4UmlEPTB:MTFOwG0>	NHXXT2YzPDh5OUe5Oi=>
Hs578T	Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF\zVlAyKM7:TR?=	M17UZlUh\A>?	NEDNRWVFVVOR	NXrHWmtqUUN3MEyxJO69VQ>?	NYjtN4tkOjR6N{m3PVY>
LN18	NYHPfIllT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnHWNlAh\|ryP	NX;4U5NkPzJiaB?=	M3vseWROW09?	MkfJTWM2ODx3IN88US=>	MWqyOFc1OTB5NB?=
LN229	NVvyO4tUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFWxVZYzOCEQvF2=	MWi3NkBp	NVvNTYxPTE2VTx?=	NGjmSGlKSzVyPEWg{txO	NX31T29QOjR5NEGwO\|Q>
LNZ308	NIDaS\|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGnDZpIzOCEQvF2=	M2n5W\|czKGh?	NULuPVdjTE2VTx?=	NHXXbHVKSzVyPEWg{txO	NWPsWIdKOjR5NEGwO\|Q>
T98G	NHzyUYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUeyNEDPxE1?	NYPad4l2PzJiaB?=	MmXnSG1UVw>?	NIfrcVVKSzVyPEWg{txO	M3rpXlI1PzRzMEe0
U87	NUPuTWhUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVeyNEDPxE1?	NX\lUJNKPzJiaB?=	M2jLT2ROW09?	M17uPGlEPTB:NTFOwG0>	Mn;SNlQ4PDFyN{S=
LN18	NHXOW5JHfW6ldHnvckBCe3OjeR?=	MlH1OUDPxE1?	MmT1NlQhcA>?	Ml\tSG1UVw>?	MmL1TY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>?	NGLxN3MzPDd2MUC3OC=>
LNZ308	MYXGeY5kfGmxbjDBd5NigQ>?	MW[1JO69VQ>?	NGOxWnEzPCCq	NEnYOpBFVVOR	MnvJTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>?	MnvnNlQ4PDFyN{S=
Saos-2	M3eyVmZ2dmO2aX;uJGF{e2G7	Mmn5OVAh\|ryP	MWS0PEBp		MlzBTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	MkPSNlQ4Ojd4NkC=
MG-63	MVLGeY5kfGmxbjDBd5NigQ>?	MXG1NEDPxE1?	MYG0PEBp		MUXJcohq[mm2czDj[YxtKGmwdnHzbY9v	MViyOFczPzZ4MB?=
SJSA-1	M4PJZ2Z2dmO2aX;uJGF{e2G7	MX21NEDPxE1?	M1vTN\|Q5KGh?		M{LKeGlvcGmkaYTzJINmdGxiaX72ZZNqd25?	MnTrNlQ4Ojd4NkC=
Saos-2	Mnu1SpVv[3Srb36gRZN{[Xl?	Mk\tOVAh\|ryP	NUjrem14PDhiaB?=		MX7Jcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	M4fkXFI1PzJ5Nk[w
MG-63	M4jFWWZ2dmO2aX;uJGF{e2G7	MoPhOVAh\|ryP	MoTOOFghcA>?		NHHWeJhKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v	M3HjWVI1PzJ5Nk[w
SJSA-1	M{exPGZ2dmO2aX;uJGF{e2G7	M2r0clUxKM7:TR?=	MYK0PEBp		NX3DNmJTUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>?	MmHENlQ4Ojd4NkC=
Saos-2	MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{PTN\|UxKM7:TR?=	NHm3Xoo1QCCq		NUDCPIRjUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	M2nxfFI1PzJ5Nk[w
MG-63	NX[1cmZnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEj2U2s2OCEQvF2=	NGe3d2U1QCCq		NFHWOGZKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?=	MoThNlQ4Ojd4NkC=
SJSA-1	NEfiT2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWfjXYJ[PTBizszN	M1ntVFQ5KGh?		NVLDTVhEUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	M{n0VVI1PzJ5Nk[w
FaDu	MmX4SpVv[3Srb36gRZN{[Xl?	NGXFRok2KM7:TR?=	Mn3oNlQhcA>?	NYfE[mxETE2VTx?=	NVLiW2IyWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44>	NGDXWG8zPDZ\|MUG0Oy=>
EMT6	Moj1SpVv[3Srb36gRZN{[Xl?	M2TGZlUh\|ryP	MUeyOEBp	NYWwZZpkTE2VTx?=	M1;icXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	NXjJNXdSOjR4M{GxOFc>
HCT116	NFGyPYNHfW6ldHnvckBCe3OjeR?=	NVvSPGszPSEQvF2=	NUP1VpBjOjRiaB?=	MWTEUXNQ	MXjS[YR2[2W\|IH;4fYdmdiClb37zeY1xfGmxbh?=	M1jjRlI1PjNzMUS3
U87	Mn[2SpVv[3Srb36gRZN{[Xl?	MojiOUDPxE1?	MnvqNlQhcA>?	NEDwXpZFVVOR	MnTlVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36=	MoWzNlQ3OzFzNEe=
GBM	NHSzZ3hCeG:ydH;zbZMhSXO\|YYm=	Mn7PNu69VQ>?	M3e5VlQ5cA>?	NIraN5lFVVOR	MXLpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m\|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5	MU[yOFUxODR7Mh?=
BON	NVG1[\|Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIDPflYyNTYQvF2=	MX63Nog>		M17k[IRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44>	MmqwNlQ1PDN3MkO=
BON	M3PQ[2Fxd3C2b4Ppd{BCe3OjeR?=	NXLZO3MzOS13zszN	MkfVNlRp		MWrpcoNz\WG\|ZYOgZZBweHSxc3nz	MlroNlQ1PDN3MkO=
H1975	MnrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlLrNE4{NTlwNt88US=>	NEXtNpg4Omh?	MYXEUXNQ	NUjOVm13UUN3ME2xMlM5Pc7:TR?=	MmDWNlQ{Ozd6NE[=
H1975	M2\PdGFxd3C2b4Ppd{BCe3OjeR?=	M3\BUlLPxE1?	M{\BNVI1cA>?	M2jPUWROW09?	M3TtU4lv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6	Mmj6NlQ{Ozd6NE[=
T-ALL	MVPBdI9xfG:\|aYOgRZN{[Xl?	NUG3fHlj[mW2d3XlckAyNjRiYX7kJFUvOyCvTTDheEAzPGhiYX7kJFAvQSCjbnSgOU42KG2PIHH0JFQ5cCCrbjDkbYZn\XKnboSgZ4VtdCCuaX7l	NFG2[JQzPCCxcjC0PIg>	NXL5dIx1TE2VTx?=	MVjh[oZm[3S\|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?=	NGPuWIIzPDNzMEezOi=>
BCR-ABL	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmTaNE4zPS1zMN88US=>	NHOzOFI1\A>?		NWPVV5Jbe2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?=	MkiyNlQzPDR4MUK=
LC-1/SQSF	MUjGeY5kfGmxbjDBd5NigQ>?	NVvkVWwzO87:TR?=	MnyxNlRp	MnS2SG1UVw>?	NYi3[\|ZU\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt	NFj5ZWszOzl6MEC5Ny=>
Primary CLL cells	M3z2O2Fxd3C2b4Ppd{BCe3OjeR?=	Mn\yNU0yOM7:TR?=	M3fHXFQ5cA>?		NInucItqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{	NVnKV3o1OjN6NUC4NFc>
Primary CLL cells	MYfLbY5ie2ViQYPzZZk>	MWKy{txO	NIDkRYI{OG2rbh?=		Mlvi[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl?	MXiyN\|g2ODhyNx?=
Primary CLL cells	MX\DfZRwfG:6aXOgRZN{[Xl?	M4nET\|LPxE1?	MX:yOIg>		MYnpcoR2[2W\|IHPlcIwh[3m2b4TvfIlkcXS7	NGDyXYgzOzh3MEiwOy=>
human NSCLC cell lines	MVPBdI9xfG:\|aYOgRZN{[Xl?	MWmwMlEzPS12zszN	MnvxNlRp	NHr6c3pFVVOR	M3SzOWlEPTC\|IILhcodmeyCocn;tJFAvPC1{zszN	M3\CO\|I{PTZ{NEey
human HCC cell lines	NGjxfZpE\WyuII\pZYJqdGm2eTDhd5NigQ>?	NYHiWGdZOC5yMEWtNe69VQ>?	NGPyR3g1QGh?		MknMTWM2OD1zzszN	NYfl[lRyOjN2OEm5PVk>
Huh7	NIPab2JMcW6jc3WgRZN{[Xl?	NUf4bYhkOc7:TR?=	MmLLOFhp		NVu4UoFOe2mpbnpvsKFk[W62bImgdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gRYt1	NUjKTmlxOjN2OEm5PVk>
SK-HEP1	MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF[zZVMyNTJyzszN	MYW3Nog>	MWfEUXNQ	NVe2UVZsUUN3MP-8oFHPxE1?	MUeyN\|Q4QTF\|Nh?=
786-0	NF7qOmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYXkO3EzOS1{MN88US=>	NFfTTFk4Omh?	MYfEUXNQ	NXizXoRkUUN3MP-8oFHPxE1?	M4ftVlI{PDd7MUO2
JVM2	NVj2TodLS3m2b4TvfIlkcXS7IHHzd4F6	NXP1WXVtOC5{LUKw{txO	M2jiRlczcA>?	MXvEUXNQ	NInGUWFKSzVyPUCuPe69VQ>?	M1TubVI{OjN6NkO5
EHEB	MlXyR5l1d3SxeHnjbZR6KGG\|c3H5	MU[wMlIuOjEQvF2=	NX7OcmF2PzKq	NXnjXmRnTE2VTx?=	NFfNZoNKSzVyPUCuO:69VQ>?	NXjFRoJ5OjN{M{i2N\|k>
MEC2	M2HOdWN6fG:2b4jpZ4l1gSCjc4PhfS=>	NEPzdpYxNjJvMkFOwG0>	MmDCO\|Jp	M1zORmROW09?	M1HP[2lEPTB;MD63{txO	M4nmSVI{OjN6NkO5
primary B-CLL lymphocytes	M1fydGFxd3C2b4Ppd{BCe3OjeR?=	NHPwOopKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n	MUSyOIg>	MmizSG1UVw>?	MVXJR\|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz	NEC2TWkzOzJ\|OE[zPS=>
primary B-CLL lymphocytes	NFnIfm1McW6jc3WgRZN{[Xl?	NXLYdI9nUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?=	MVSyOIg>		MkTPbY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36=	NGnaSmgzOzJ\|OE[zPS=>
human NSCLC	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFfFOpMxNjVvMt88US=>	NETo[Yw4Omh?		MmHkTWM2OD1zzszN	NIjQUZYzOjd6MUO5Ny=>
human NSCLC	M2r2SmtqdmG\|ZTDBd5NigQ>?	NF7oO48y\|ryP	MUiyOIg>		MU\pcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62	NXmzZmlCOjJ5OEGzPVM>
Y1 cell line	MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXiwMlHPxE1xMd88US=>	M2rJTVI1cA>?	NWf0VGl2TE2VTx?=	NVz5W\|F5cW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO=	NX:0W\|NpOjJ4OUK5NFQ>
PIK3CA-mutant MCF7	M4PZNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXzKT206T0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd\|bl2=	NFnobIc4Omh?		MorVS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	MUSyNlY2Ozl4Nx?=
PIK3CA-mutant MCF7	NHnCSpZMcW6jc3WgRZN{[Xl?	MlrLTWM2OD1zMUVCtVNvVQ>?	NFfDOVk4Omh?		MVLJR\|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:\|cHjvdplt[XSrb36gcIV3\Wy\|	M{nrZVIzPjV\|OU[3
MCF7-myr-Akt	NEi0NmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MULHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>?	Moj4O\|Jp		MVvHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>?	M2DNSVIzPjV\|OU[3
colon cancer cell lines	M3O4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUGwMVEx\|ryP	NITjT244Omh?	NX3UWpRZTE2VTx?=	M3LSd2lEPTB;Md88US=>	MlvWNlI2PDN6NUe=
gastric cancer cell lines	NE\wPYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NF3DSYoxNTFyzszN	MVq3Nog>	MWPEUXNQ	MlezTWM2OD1{LUZOwG0>	MXeyNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45	MWPBdI9xfG:\|aYOgRZN{[Xl?	M4ryNlLPxE1?	M2PmdFQ5cA>?		NXLXXnIze2irZoSgbY4hTzJicHjhd4U>	NETm[GozOjV2M{i1Oy=>
HT-29 and HCT-116	NX[yN\|Y2S2G\|cHHz[UBie3OjeR?=	MonrOe69VQ>?	M1Lo[\|I1cA>?		NXSwOWlEcW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5	MYCyNlU1Ozh3Nx?=
MM cell lines	M37HZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn3wNVDPxE1?	NUPreFd7OjSq	MmXySG1UVw>?	NVexOIY6UUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn	NG\2bXUzOjJyN{S4OS=>
ARP-1	MnLpRZBweHSxc3nzJGF{e2G7	NITVeoUyOM7:TR?=	NGHmeoMzPGh?	MWDEUXNQ	NFe5cIRqdmS3Y3XzJG1OKGOnbHygZZBweHSxc3nzJJRpem:3Z3igZ4F{eGG\|ZTDhZ5RqfmG2aX;u	NXvQclRzOjJ{MEe0PFU>
SNU-601	NYnJTlNTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		Mlj1O\|Jp	M2nHd2ROW09?	MkexTWM2OD1yLkixOuKyOC5yNkROwG0>	NF7JSXczOjF3OUixOC=>
SNU-1	NUDEUoViT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NYrrNm4yPzKq	NULUZo02TE2VTx?=	M4m5TWlEPTB;MT6wPFLDuTBwMEK4{txO	MWqyNlE2QThzNB?=
SNU-668	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MWS3Nog>	NWPnSmJrTE2VTx?=	Mnq2TWM2OD1zLkW3PeKyOC5yN{VOwG0>	NUX1VYtHOjJzNUm4NVQ>
AGS	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NY\4fGQxPzKq	NYnRNpRnTE2VTx?=	Mly0TWM2OD1zLkexOOKyOC5zMUhOwG0>	NV7odFhYOjJzNUm4NVQ>
SNU-216	NYD4eWdrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2H5O\|czcA>?	MmDUSG1UVw>?	NI\lXpNKSzVyPUKuOlkzyrFyLkC4Nu69VQ>?	M{SxWlIzOTV7OEG0
SNU-5	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NF\6V444Omh?	M3fJNGROW09?	MlLXTWM2OD1zLkO1NeKyOC5yOUJOwG0>	MmLCNlIyPTl6MUS=
SNU-638	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NGjZRVU4Omh?	M2faNWROW09?	NInRXFdKSzVyPUKuNlgzyrFyLkC1N:69VQ>?	NWXjO2dROjJzNUm4NVQ>
SNU-16	MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MmTaO\|Jp	MoG2SG1UVw>?	M2DaOWlEPTB;MT61O\|PDuTBwMECx{txO	NIDhR5ozOjF3OUixOC=>
SNU-484	M{nsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1XN[\|czcA>?	MVTEUXNQ	Mk[3TWM2OD1zLkeyPOKyOC5yNEZOwG0>	MnnZNlIyPTl6MUS=
SNU-620	M1Hmdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NILyR\|Q4Omh?	NUnyfXhtTE2VTx?=	M2j6[GlEPTB;Mj65N\|nDuTBwMECx{txO	MWmyNlE2QThzNB?=
SNU-719	M{HKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MYS3Nog>	NVuwWHViTE2VTx?=	MW\JR\|UxRTNwMEO3xtExNjB\|Mt88US=>	NGDHRYwzOjF3OUixOC=>
glioma cell lines	MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MmW4O\|Jp		MUTJR\|UxRTFvMt88US=>	M4fyelIzODZ3MEiw
U87	NFi0PWhCeG:ydH;zbZMhSXO\|YYm=	MoLKNu69VQ>?	NIrQTYM4Omh?		MWnpcoR2[2W\|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?=	M33ENlIzODZ3MEiw

... 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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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)