Buparlisib (BKM120, NVP-BKM120)

Catalog No.S2247

Buparlisib (BKM120, NVP-BKM120) Chemical Structure

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.

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In DMSO USD 272 In stock
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Cited by 38 Publications

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 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.
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)
52 nM 116 nM 166 nM 262 nM 2.4 μM
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 NHHFdINEgXSxdH;4bYMhSXO|YYm= NEXkeHQ4OiCq NXn6U3dETE2VTx?= NYDRcGRyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=> NIm5bG4zPDlyMEK2Oi=>
DU145 MWXDfZRwfG:6aXOgRZN{[Xl? NGDTZ5U4OiCq MV;EUXNQ M{TuTmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiTFvCNUBufXSjboSge4l1cCCJSUWwJI9nKDBwMECwOFM2KM7:TR?= MXmyOFkxODJ4Nh?=
A2780 NIHKS2FEgXSxdH;4bYMhSXO|YYm= MlrlO|IhcA>? M3P3bWROW09? MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N|Uh|ryP MXiyOFkxODJ4Nh?=
U87MG MYHDfZRwfG:6aXOgRZN{[Xl? NX;Pd|FoPzJiaB?= M3zqfmROW09? MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh|ryP NIO1eFMzPDlyMEK2Oi=>
A2780 MXjGeY5kfGmxbjDBd5NigQ>? NFrFc3YyKGh? MY\EUXNQ NIf6OVBKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNFU2KM7:TR?= NHfBT5EzPDlyMEK2Oi=>
DU145 NYe5[4htTnWwY4Tpc44hSXO|YYm= M3njNFEhcA>? M4HGdmROW09? MlnBTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? NUHUPJREOjR7MECyOlY>
A2780 MnnKSpVv[3Srb36gRZN{[Xl? M2XKPFEhcA>? NXvNdnA5TE2VTx?= MVTJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>? M3\4eVI1QTByMk[2
MCF7 NFPyZmtHfW6ldHnvckBCe3OjeR?= MnG0NUBp M2LhSWROW09? MnfyTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO MVmyOFkxODJ4Nh?=
U87MG NXfUUo43TnWwY4Tpc44hSXO|YYm= M3robFEhcA>? NXXN[VNGTE2VTx?= NFLTVXlKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR|UxKG:oIECuNVMh|ryP M3zWelI1QTByMk[2
A2780 NF3WfWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf0O|IhcA>? M3Xs[WROW09? Mnf3SWM2OD1yLkWyJO69VQ>? NGXY[4kzPDlyMEK2Oi=>
SKMES-1 M1rOTGN6fG:2b4jpZ{BCe3OjeR?= MlH2NUDPxE1? M3[2blczKGh? M{PvOmlv\HWlZYOgZ4VtdCCmZXH0bC=> NYTkc3lvOjZyMUOzNVg>
H596 M3PKUmZ2dmO2aX;uJGF{e2G7 NES1[4UyKM7:TR?= Moj1TY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>? MWKyOlAyOzNzOB?=
HCC2450 MkXoSpVv[3Srb36gRZN{[Xl? NXvTWpFwOSEQvF2= M4DQVWlueGGrcoOgZ4VtdCCrbo\hd4lwdg>? MlvJNlYxOTN|MUi=
A549 MVjGeY5kfGmxbjDBd5NigQ>? MYm1NFAhdk1? MkLtOFghcA>? Ml3TSG1UVw>? NFXOTpNKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= NWPLbpRJOjV7M{eyPVk>
A549 M1fvd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLPNUDPxE1? MkPxO|IhcA>? NWWxWlltTE2VTx?= MWLJcohq[mm2czDj[YxtKGe{b4f0bC=> NHTtWlEzPTl|N{K5PS=>
H522 M4PRV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIqxOJAyKM7:TR?= NG\GVWY4OiCq NIDGTllFVVOR MYHJcohq[mm2czDj[YxtKGe{b4f0bC=> M3rtNVI2QTN5Mkm5
LNCaP MYHGeY5kfGmxbjDBd5NigQ>? MXexJO69VQ>? NEHPNHFUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?= MVmyOVM3ODd7OR?=
LNCaP95 NEfQUGVHfW6ldHnvckBCe3OjeR?= M4fYcFEh|ryP MljCV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? MUiyOVM3ODd7OR?=
HCT-15 NEj0PI9CeG:2b4Ppd{BCe3OjeR?= NEnZcVUyOCEQvF2= NYPkc4xpPDhiaB?= MUPEUXNQ Mo[2TY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUG1JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MYCyOVE2OjJ2NR?=
HCT-116 MXPBdI91d3OrczDBd5NigQ>? NG\K[poyOCEQvF2= MnfYOFghcA>? NH;INpVFVVOR NH;qb4pKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVE3KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NH\qcZYzPTF3MkK0OS=>
NCI-H460 M1nueWFxd3Sxc3nzJGF{e2G7 NXvVeZptOTBizszN NGrrXnY1QCCq M2PTZmROW09? M4rI[Glv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= M2LSR|I2OTV{MkS1
SKOV-3 M{nTZmFxd3Sxc3nzJGF{e2G7 Mk\mNVAh|ryP NInkR3g1QCCq Mk\1SG1UVw>? NEjxUXJKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCVS1;WMVMh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NGLLVHYzPTF3MkK0OS=>
BSY-1 NYjzNIJoSXCxdH;zbZMhSXO|YYm= MmrINVAh|ryP MWq0PEBp MlfQSG1UVw>? M3PWTWlv\HWlZYOgZZBweHSxc3nzJIlvKEKVWT2xJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? M{LubVI2OTV{MkS1
MKN-1 MXzBdI91d3OrczDBd5NigQ>? M1v4ZlExKM7:TR?= MlfkOFghcA>? NFfydZhFVVOR MY\JcoR2[2W|IHHwc5B1d3OrczDpckBOU05vMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NXjZbHRqOjVzNUKyOFU>
NCI-H522 NXHUe5ZGSXCxdH;zbZMhSXO|YYm= NVPWZ4RGOTBizszN NHXvW2Q1QCCq M1:1WGROW09? NHHIeWtKdmS3Y3XzJIFxd3C2b4Ppdy=> NWrQOFZOOjVzNUKyOFU>
OVCAR-3 NYXQdZpXSXCxdH;zbZMhSXO|YYm= M1L1N|ExKM7:TR?= NUTKN3lEPDhiaB?= NVnzNYwxTE2VTx?= NIr4emNKdmS3Y3XzJIFxd3C2b4Ppdy=> MWWyOVE2OjJ2NR?=
HBC-5 MXvBdI91d3OrczDBd5NigQ>? NXLjVHlmOTBizszN M4fidVQ5KGh? NFHlfYJFVVOR NHH3dHhKdmS3Y3XzJIFxd3C2b4Ppdy=> Mo\TNlUyPTJ{NEW=
RXF-631L MnXyRZBwfG:|aYOgRZN{[Xl? NEDpSJIyOCEQvF2= MUC0PEBp MXfEUXNQ MmLOTY5lfWOnczDhdI9xfG:|aYO= NIX0fmEzPTF3MkK0OS=>
MKN-45 MWDBdI91d3OrczDBd5NigQ>? M1jPXVExKM7:TR?= MnfJOFghcA>? NFXlTolFVVOR MonYTY5lfWOnczDhdI9xfG:|aYO= M1y5eVI2OTV{MkS1
BON-1 NFvjZY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlj2OVAxKG6P MYKxNEBl NYHPNoQ{TE2VTx?= M2TXTWlvcGmkaYTzJINmdGxiZ4Lve5Rp NGrVbIIzPTB{NkK5Ni=>
BON-1 M{XDTWZ2dmO2aX;uJGF{e2G7 NY\sXYhRPTByIH7N NFnidIk1KGh? MU\EUXNQ M4\yeGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= NXLsSWlLOjVyMk[yPVI>
QGP-1 M36zdmZ2dmO2aX;uJGF{e2G7 M2DRPVUxOCCwTR?= Ml7lOEBp NXTPe2M6TE2VTx?= M4\YdWlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= MViyOVAzPjJ7Mh?=
Huh7 NVm2XVJCTnWwY4Tpc44hSXO|YYm= MV2xJO69VQ>? MlLvNUBp Mm\3SG1UVw>? MX\Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGPldlQ4PA>? MkfaNlUxODR2MEO=
BNL M4jrWmZ2dmO2aX;uJGF{e2G7 NEXhbWwyKM7:TR?= MVGxJIg> NX7NSnE5TE2VTx?= MU\Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Y> NXH1U2k5OjVyMES0NFM>
MDA-MB-175 NVH0PWN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nKcVEh|ryP NITufpk2KGR? NVq4Z5JxTE2VTx?= MnriTWM2ODxzIN88US=> MoTzNlQ5Pzl5OU[=
MDA-MB-134 NF64dIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvOZYpJOSEQvF2= NWDEfGs{PSCm NUf5SYx6TE2VTx?= NWjTc3BSUUN3MEyxJO69VQ>? NGmxcnkzPDh5OUe5Oi=>
HCC1500 M{e3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKxJO69VQ>? NHi1VJc2KGR? NY\EN5FOTE2VTx?= NEDHcVFKSzVyPEGg{txO M4TNPVI1QDd7N{m2
EFM-19 NUnaUVVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\oNUDPxE1? NFi5eI02KGR? NYLBSWVLTE2VTx?= MmTPTWM2ODxzIN88US=> NXfCdoFYOjR6N{m3PVY>
ZR-75-30 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjaclUyKM7:TR?= M33pS|Uh\A>? MUHEUXNQ MUfJR|UxRDFizszN MkTxNlQ5Pzl5OU[=
MDA-MB-361 NH\pSnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHxfY5bOSEQvF2= MWW1JIQ> MlHCSG1UVw>? MWjJR|UxRDFizszN NIfnXWkzPDh5OUe5Oi=>
T-47D NFfCc5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3ONUDPxE1? MVe1JIQ> M4PEV2ROW09? M{TRNmlEPTB:MTFOwG0> Ml;FNlQ5Pzl5OU[=
SK-BR-3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[xJO69VQ>? NV\z[2dZPSCm M4nGc2ROW09? NYLkR5lmUUN3MEyxJO69VQ>? MVSyOFg4QTd7Nh?=
UACC-732 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fMXVEh|ryP M3e4eFUh\A>? Mn3uSG1UVw>? NWTlcHdNUUN3MEyxJO69VQ>? MWGyOFg4QTd7Nh?=
BT-474 M2Ds[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHmWlcyKM7:TR?= NF\5Uno2KGR? M4rCNmROW09? Mn\uTWM2ODxzIN88US=> M122TVI1QDd7N{m2
HCC202 NHS4PFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXJTmgyKM7:TR?= M33KcFUh\A>? NH3tSXZFVVOR M{nWZmlEPTB:MTFOwG0> MkXSNlQ5Pzl5OU[=
MCF7 NHvIcoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUKxJO69VQ>? M4\jcFUh\A>? NUTQboRUTE2VTx?= NEXaSnNKSzVyPEGg{txO NFfqcWszPDh5OUe5Oi=>
MDA-MB-415 NYr4dpB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnqe5NmOSEQvF2= MkDaOUBl M3n6OWROW09? MUTJR|UxRDFizszN NXe2U45oOjR6N{m3PVY>
MDA-MB-453 Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fGVlEh|ryP NVr6bnBJPSCm MUTEUXNQ NXvXeZRqUUN3MEyxJO69VQ>? NIfJWFUzPDh5OUe5Oi=>
ZR-75-1 MnrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;q[JAyKM7:TR?= MkD1OUBl MVjEUXNQ NInJe|hKSzVyPEGg{txO NVT4bo9GOjR6N{m3PVY>
HCC38 NXK3OpBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jnTlEh|ryP NWnMPWNEPSCm M4TGSWROW09? NX6yfZJvUUN3MEyxJO69VQ>? MXKyOFg4QTd7Nh?=
HCC1419 M1r0Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOxJO69VQ>? NX3EWXVDPSCm M2WyT2ROW09? MVLJR|UxRDFizszN MX6yOFg4QTd7Nh?=
UACC-812 M1PXXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTwNUDPxE1? MlToOUBl MU\EUXNQ NVzUOpUzUUN3MEyxJO69VQ>? M3zJV|I1QDd7N{m2
HCC1187 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKxJO69VQ>? NFjV[pQ2KGR? MkDvSG1UVw>? NI[x[GlKSzVyPEGg{txO NXizZ5pjOjR6N{m3PVY>
KPL-1 Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPjVnlUOSEQvF2= NHfUXYQ2KGR? M2LiO2ROW09? NYLyW4Q{UUN3MEyxJO69VQ>? MYGyOFg4QTd7Nh?=
SUM-225 NGX1RYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXewZ3FZOSEQvF2= MUC1JIQ> NHfkXndFVVOR MWDJR|UxRDFizszN MkXsNlQ5Pzl5OU[=
EFM-192A MmPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PPV|Eh|ryP Ml;yOUBl M320SWROW09? NH:5U|RKSzVyPEGg{txO MVSyOFg4QTd7Nh?=
JIMT-1 Mn7uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPnd20yKM7:TR?= MVS1JIQ> NEj6O5RFVVOR NEPsZ4NKSzVyPEGg{txO M1jiRlI1QDd7N{m2
HCC1143 NVjEZ3FqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT6cnAyKM7:TR?= NFWyWlM2KGR? NGjMUVhFVVOR NWPOO3R[UUN3MEyxJO69VQ>? M{\hTVI1QDd7N{m2
HCC2218 M12xcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCxJO69VQ>? NWHwPWs2PSCm M17JfGROW09? Mne1TWM2ODxzIN88US=> NWLsclNLOjR6N{m3PVY>
MDA-MB-468 Mn7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj2[5hoOSEQvF2= NUHxZWNxPSCm MV7EUXNQ MkDWTWM2ODxzIN88US=> MnnjNlQ5Pzl5OU[=
BT-20 MoHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjmNUDPxE1? NEXCPHM2KGR? M2nYdGROW09? NHvyUI9KSzVyPEGg{txO NXH6THQ{OjR6N{m3PVY>
MDA-MB-435 MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInOXoMyKM7:TR?= M4nycFUh\A>? NV[1cZprTE2VTx?= NEO2[GZKSzVyPEGg{txO NXzHfG9lOjR6N{m3PVY>
BT-549 MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rNWVEh|ryP NWDmR2xqPSCm MkfhSG1UVw>? NF6wc3dKSzVyPEGg{txO NHzQ[HEzPDh5OUe5Oi=>
HCC1806 MnHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXyxJO69VQ>? NHTFfog2KGR? MlLISG1UVw>? NInDcohKSzVyPEGg{txO MlK4NlQ5Pzl5OU[=
HCC1937 NWXJSoZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmxJO69VQ>? MUO1JIQ> MX3EUXNQ MmfyTWM2ODxzIN88US=> M1\FSVI1QDd7N{m2
Hs578T MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDrT3kyKM7:TR?= MXy1JIQ> M4Xrd2ROW09? NWjZS|JYUUN3MEyxJO69VQ>? M2j6[FI1QDd7N{m2
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H1975 NFT4cYhCeG:ydH;zbZMhSXO|YYm= NH;OUpgz|ryP MlrKNlRp M3jVfGROW09? MYrpcoNz\WG|ZYOgZZBweHSxc3nzJJJifGVic3nncolncWOjboTsfS=> NYnGeVNzOjR|M{e4OFY>
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Primary CLL cells NVnnNYJSU2mwYYPlJGF{e2G7 MX2y{txO M2LhOlMxdWmw NGHwO2Jl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= MXyyN|g2ODhyNx?=
Primary CLL cells NHflSW5EgXSxdH;4bYMhSXO|YYm= MWGy{txO NXu5WpZpOjSq NG\IdVlqdmS3Y3XzJINmdGxiY4n0c5RwgGmlaYT5 MV[yN|g2ODhyNx?=
human NSCLC cell lines NXfRWYFKSXCxcITvd4l{KEG|c3H5 NGD6XZIxNjF{NT20{txO MonHNlRp MkfRSG1UVw>? NFPueodKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> NGjQ[JAzOzV4MkS3Ni=>
human HCC cell lines M2XR[WNmdGxidnnhZoltcXS7IHHzd4F6 MknxNE4xODVvMd88US=> MkfpOFhp NX\XNIo5UUN3ME2x{txO MV2yN|Q5QTl7OR?=
Huh7 NWrCdWtbU2mwYYPlJGF{e2G7 NEHofYoy|ryP NV63OZZnPDiq Mknwd4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NHraeZEzOzR6OUm5PS=>
SK-HEP1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG0NU0zOM7:TR?= MYS3Nog> MWXEUXNQ MnPVTWM2OO,:nEJOwG0> M3f4[FI{PDd7MUO2
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JVM2 M1PzT2N6fG:2b4jpZ4l1gSCjc4PhfS=> MW[wMlIuOjEQvF2= MlrjO|Jp NX7yblVETE2VTx?= NGLOOZhKSzVyPUCuPe69VQ>? NHe0WGozOzJ|OE[zPS=>
EHEB NHraSIdEgXSxdH;4bYNqfHliYYPzZZk> MVOwMlIuOjEQvF2= MVW3Nog> NHzuSGtFVVOR MVfJR|UxRTBwN988US=> M1G5bFI{OjN6NkO5
MEC2 MYnDfZRwfG:6aXPpeJkh[XO|YYm= MYCwMlIuOjEQvF2= M2P6bVczcA>? MX\EUXNQ MUnJR|UxRTBwN988US=> MkLiNlMzOzh4M{m=
primary B-CLL lymphocytes NHvERXlCeG:ydH;zbZMhSXO|YYm= MUfJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m M2n0N|I1cA>? M1jvbmROW09? Mmr4TWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> NWPpNnEyOjN{M{i2N|k>
primary B-CLL lymphocytes NUi3OGJzU2mwYYPlJGF{e2G7 MXXJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m NFXoUmIzPGh? NYPNT2pbcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> NVv6clJ1OjN{M{i2N|k>
human NSCLC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HQdFAvPS1{zszN MYC3Nog> MXXJR|UxRTIQvF2= NXzPdW9iOjJ5OEGzPVM>
human NSCLC MlLpT4lv[XOnIFHzd4F6 M{nUTVHPxE1? NUnqPZRyOjSq NGD1eIRqdmirYnn0d{B1cGViQXv0M41VV1Jic3nncoFtcW6pIIDheIh4[XliYYSgN4gh[W[2ZYKgeJJm[XSvZX70 MknzNlI4QDF|OUO=
Y1 cell line NUKyeZoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMlHPxE1xMd88US=> M4rGSFI1cA>? NUixOpBkTE2VTx?= M3SwUIlvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy| NYexXXp[OjJ4OUK5NFQ>
PIK3CA-mutant MCF7 NIXSfItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3FeVZIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= NFnrTlc4Omh? MnfXS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? M4X6SFIzPjV|OU[3
PIK3CA-mutant MCF7 MYjLbY5ie2ViQYPzZZk> MYfJR|UxRTFzNNMxN45O NH2yU4I4Omh? M2PWUWlEPTB;MUG0xtE{dk1iaX6gdoVlfWOrbnegRYt1KHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= NFL5SXozOjZ3M{m2Oy=>
MCF7-myr-Akt M3GwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljPS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? NX23UmkzPzKq NX:4[Xh{T0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= MX6yNlY2Ozl4Nx?=
colon cancer cell lines NYjGcFdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjOSmk3OC1zMN88US=> M2GxTVczcA>? NGe5VXFFVVOR NYDKO4lLUUN3ME2x{txO NVi4e5NNOjJ3NEO4OVc>
gastric cancer cell lines NYDLfJBIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYOwMVEx|ryP M4[1SFczcA>? NIjOcolFVVOR NGDCZWpKSzVyPUKtOe69VQ>? MUGyNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45 M1z0emFxd3C2b4Ppd{BCe3OjeR?= M4SydVLPxE1? M2\FXVQ5cA>? MX\zbIlnfCCrbjDHNkBxcGG|ZR?= NGq3b4kzOjV2M{i1Oy=>
HT-29 and HCT-116 M17KcGNie3Cjc3WgZZN{[Xl? M1vkRlXPxE1? MV6yOIg> M{Wxbolv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= MUCyNlU1Ozh3Nx?=
MM cell lines MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4n2fFEx|ryP M{jwc|I1cA>? MVfEUXNQ NYXVSpZCUUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn MUCyNlIxPzR6NR?=
ARP-1 NWXtfFZDSXCxcITvd4l{KEG|c3H5 M3fT[FEx|ryP NH;ufJYzPGh? NU\s[plzTE2VTx?= NW\WelFDcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> NIfDNY4zOjJyN{S4OS=>
SNU-601 NVr4[41tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvZdI84Omh? M4fvO2ROW09? NIjqTnBKSzVyPUCuPFE3yrFyLkC2N:69VQ>? MYSyNlE2QThzNB?=
SNU-1 MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXroO2x3PzKq NFnyWFlFVVOR NGDOWVRKSzVyPUGuNFgzyrFyLkCyPO69VQ>? MnHGNlIyPTl6MUS=
SNU-668 M1PzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PQW|czcA>? M4LocGROW09? M37BbWlEPTB;MT61O|nDuTBwMEe0{txO NWLqcppkOjJzNUm4NVQ>
AGS NHTPWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\hO|Jp NVTWOXY{TE2VTx?= M1nJSWlEPTB;MT63NVTDuTBwMUG3{txO M3y0ZlIzOTV7OEG0
SNU-216 M4D0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvTN2JHPzKq NWXtcXI4TE2VTx?= MmWxTWM2OD1{Lk[5NuKyOC5yOENOwG0> NI\2bYQzOjF3OUixOC=>
SNU-5 M1PLOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ixS|czcA>? MXvEUXNQ MXjJR|UxRTFwM{WxxtExNjB7Md88US=> Mn:0NlIyPTl6MUS=
SNU-638 NH3GW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWD5dGVwPzKq NYjJSIdHTE2VTx?= MV\JR|UxRTJwMkiyxtExNjB3M988US=> MX6yNlE2QThzNB?=
SNU-16 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkflO|Jp MV3EUXNQ NH7hNWZKSzVyPUGuOVc{yrFyLkCwNe69VQ>? NGjvWmQzOjF3OUixOC=>
SNU-484 NWrIOmxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mne5O|Jp MUPEUXNQ NYnNWZhGUUN3ME2xMlczQMLzMD6wOFXPxE1? MojtNlIyPTl6MUS=
SNU-620 NH\ETpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\4N|czcA>? NXHSW4VoTE2VTx?= NYL3bIRoUUN3ME2yMlk{QcLzMD6wNFHPxE1? M4i0fFIzOTV7OEG0
SNU-719 M3;HZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmm0O|Jp M1jrVWROW09? NYPtS5IyUUN3ME2zMlA{P8LzMD6wN|LPxE1? MUGyNlE2QThzNB?=
glioma cell lines NE\wfo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjmfpVJPzKq NUS5dpdiUUN3ME2xMVLPxE1? Mo\6NlIxPjVyOEC=
U87 MYTBdI9xfG:|aYOgRZN{[Xl? NXXGU2d2Os7:TR?= M4W2SlczcA>? M3HnOIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiYX7kJINt\WG4ZXSgVGFTWCCjbnSgZ4F{eGG|ZT2z NFqyTIIzOjB4NUC4NC=>

... 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)

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

Molecular Weight 410.39
Formula

C18H21F3N6O2

CAS No. 944396-07-0
Storage powder
in solvent
Synonyms N/A

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Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01870726 Terminated c-MET Inhibitor; PI3K Inhibitor PTEN Mutations Homozygous Del. of PTEN or PTEN Neg. by IHC c-Met Ampli. by FISH INC280 BKM120 Buparlisib; Recurrent GBM Novartis Pharmaceuticals|Novartis January 9 2014 Phase 1|Phase 2
NCT01820325 Terminated Non-Small Cell Lunch Cancer Novartis Pharmaceuticals|Novartis September 9 2013 Phase 1
NCT01512251 Completed BRAF Mutant Metastatic Melanoma University of California San Francisco|Novartis June 9 2012 Phase 1|Phase 2
NCT01610284 Active not recruiting Breast Cancer Novartis Pharmaceuticals|Novartis August 7 2012 Phase 3
NCT02340780 Active not recruiting Chronic Lymphocytic Leukemia Canadian Cancer Trials Group|Novartis January 30 2015 Phase 2
NCT01473901 Completed Glioblastoma Novartis Pharmaceuticals|Novartis December 30 2011 Phase 1

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID