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 37 Publications

5 Customer Reviews

  • 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.. 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 NHLU[FlEgXSxdH;4bYMhSXO|YYm= Mn7HO|IhcA>? NVrwOHJyTE2VTx?= MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKEV3NEXLJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMECxOVgh|ryP NU[3XlRuOjR7MECyOlY>
DU145 NFu1eo5EgXSxdH;4bYMhSXO|YYm= M1K1UFczKGh? NFTEZmpFVVOR NV3jOpdrS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN MkPUNlQ6ODB{Nk[=
A2780 MUfDfZRwfG:6aXOgRZN{[Xl? M4rGTVczKGh? NXTQVm83TE2VTx?= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N|Uh|ryP MWCyOFkxODJ4Nh?=
U87MG NWPtVHdIS3m2b4TvfIlkKEG|c3H5 NHPr[oY4OiCq NV7nc5BQTE2VTx?= NHLiOoREgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN MorNNlQ6ODB{Nk[=
A2780 MXLGeY5kfGmxbjDBd5NigQ>? NFnUe4EyKGh? NFi5UW1FVVOR NGDBeVNKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNFU2KM7:TR?= NGL4XIgzPDlyMEK2Oi=>
DU145 M{e0OWZ2dmO2aX;uJGF{e2G7 NWfFS4twOSCq MnTpSG1UVw>? MUTJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>? NHvISmUzPDlyMEK2Oi=>
A2780 MkPZSpVv[3Srb36gRZN{[Xl? MVuxJIg> NVv2bo9ITE2VTx?= NGr5WpdKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDFR|UxKG:oIECuNFc1KM7:TR?= MViyOFkxODJ4Nh?=
MCF7 NFHsZVFHfW6ldHnvckBCe3OjeR?= M4j0SFEhcA>? NXjJTGZRTE2VTx?= MWrJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCHNUS1T{BufXSjboStcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMTFOwG0> MViyOFkxODJ4Nh?=
U87MG MontSpVv[3Srb36gRZN{[Xl? M2nveFEhcA>? NEjSc4tFVVOR M4PvO2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1? M{n1e|I1QTByMk[2
A2780 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEO5e2E4OiCq MkO5SG1UVw>? NULRUot[TUN3ME2wMlUzKM7:TR?= M13I[FI1QTByMk[2
SKMES-1 NILBN4ZEgXSxdH;4bYMhSXO|YYm= M2\6N|Eh|ryP M1z3UFczKGh? M3vNUGlv\HWlZYOgZ4VtdCCmZXH0bC=> MWqyOlAyOzNzOB?=
H596 MmD1SpVv[3Srb36gRZN{[Xl? Ml3sNUDPxE1? M4[wcWlueGGrcoOgZ4VtdCCvaXfyZZRqd25? MVWyOlAyOzNzOB?=
HCC2450 MYXGeY5kfGmxbjDBd5NigQ>? MknWNUDPxE1? NXvjVHpxUW2yYXnyd{Bk\WyuIHnueoF{cW:w M2W3dlI3ODF|M{G4
A549 M{jOU2Z2dmO2aX;uJGF{e2G7 MlfEOVAxKG6P MYC0PEBp NFL1UINFVVOR M{XGXWlvcGmkaYTzJGFsfCCjY4TpeoF1cW:w MnLBNlU6Ozd{OUm=
A549 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:xJO69VQ>? MljOO|IhcA>? M1LmNmROW09? MWPJcohq[mm2czDj[YxtKGe{b4f0bC=> MXmyOVk{PzJ7OR?=
H522 NWrQVJN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixJO69VQ>? MWe3NkBp NF\BbY5FVVOR NYPiO5BQUW6qaXLpeJMh[2WubDDndo94fGh? M3jub|I2QTN5Mkm5
LNCaP NVXUTItvTnWwY4Tpc44hSXO|YYm= NX;aN5J4OSEQvF2= MkDlV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? M3PqOlI2OzZyN{m5
LNCaP95 NYnXXXJ4TnWwY4Tpc44hSXO|YYm= NWPvUVZbOSEQvF2= NE\oPVRUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?= MWeyOVM3ODd7OR?=
HCT-15 MWPBdI91d3OrczDBd5NigQ>? MnXHNVAh|ryP NUPHfVVzPDhiaB?= NWXicpdXTE2VTx?= NUfq[3hsUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVE2KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NWfhbmd4OjVzNUKyOFU>
HCT-116 MkPMRZBwfG:|aYOgRZN{[Xl? NIjGSGkyOCEQvF2= MX20PEBp MnzsSG1UVw>? NGLlcIdKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVE3KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= MWCyOVE2OjJ2NR?=
NCI-H460 M4n0bmFxd3Sxc3nzJGF{e2G7 NUTaTYhyOTBizszN M1HDelQ5KGh? MXnEUXNQ M2n1cGlv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= Ml7KNlUyPTJ{NEW=
SKOV-3 NHLjR5lCeG:2b4Ppd{BCe3OjeR?= NVPB[pVnOTBizszN M1vQ[lQ5KGh? MVnEUXNQ NFnyU3BKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCVS1;WMVMh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= M2LvbFI2OTV{MkS1
BSY-1 NGHGcJVCeG:2b4Ppd{BCe3OjeR?= NHntNWIyOCEQvF2= MknLOFghcA>? MlHQSG1UVw>? NILU[29KdmS3Y3XzJIFxd3C2b4Ppd{BqdiCEU2mtNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MWSyOVE2OjJ2NR?=
MKN-1 MWHBdI91d3OrczDBd5NigQ>? Mon5NVAh|ryP MXe0PEBp M4i1W2ROW09? NUXEZ2t7UW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NGj0bo0zPTF3MkK0OS=>
NCI-H522 NGTJO3VCeG:2b4Ppd{BCe3OjeR?= NXrrNnA{OTBizszN MVu0PEBp MlXxSG1UVw>? MnXzTY5lfWOnczDhdI9xfG:|aYO= NUDoSnNCOjVzNUKyOFU>
OVCAR-3 MULBdI91d3OrczDBd5NigQ>? M2LFPVExKM7:TR?= MmTTOFghcA>? NULlNVhTTE2VTx?= NVm4c3hwUW6mdXPld{BieG:ydH;zbZM> MlrpNlUyPTJ{NEW=
HBC-5 NXrLVXJ5SXCxdH;zbZMhSXO|YYm= M4HNXVExKM7:TR?= M3W3RlQ5KGh? MYLEUXNQ MV3JcoR2[2W|IHHwc5B1d3Orcx?= MXqyOVE2OjJ2NR?=
RXF-631L NYLyU|l5SXCxdH;zbZMhSXO|YYm= NED1VZQyOCEQvF2= MUe0PEBp NU\CNHoyTE2VTx?= NGHGPJRKdmS3Y3XzJIFxd3C2b4Ppdy=> MYCyOVE2OjJ2NR?=
MKN-45 M{fRcGFxd3Sxc3nzJGF{e2G7 MWqxNEDPxE1? NV;oN2dSPDhiaB?= MmXySG1UVw>? NXvrb5lZUW6mdXPld{BieG:ydH;zbZM> MmnNNlUyPTJ{NEW=
BON-1 NX6zd49ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX21NFAhdk1? M3TsXlExKGR? NWD3RpJPTE2VTx?= M3K1emlvcGmkaYTzJINmdGxiZ4Lve5Rp NHzHUFMzPTB{NkK5Ni=>
BON-1 MkjrSpVv[3Srb36gRZN{[Xl? NXS3fJg6PTByIH7N NXTtdZI5PCCq Ml;HSG1UVw>? MYPJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| NFfJcHEzPTB{NkK5Ni=>
QGP-1 MYnGeY5kfGmxbjDBd5NigQ>? NFrob2Q2ODBibl2= MVi0JIg> M33CbmROW09? MWjJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| NUjQToV{OjVyMk[yPVI>
Huh7 MmjMSpVv[3Srb36gRZN{[Xl? NV7lfoZ1OSEQvF2= Ml30NUBp M4L2fmROW09? M2Tjb2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgV4VzPDd2 MlzLNlUxODR2MEO=
BNL NYnycnFTTnWwY4Tpc44hSXO|YYm= M1niclEh|ryP NHjDSJkyKGh? NYjadIpJTE2VTx?= M3;XW2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>? MlnyNlUxODR2MEO=
MDA-MB-175 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDQWG8yKM7:TR?= M{\sOlUh\A>? MYPEUXNQ NETteWVKSzVyPEGg{txO M3i4fFI1QDd7N{m2
MDA-MB-134 Mkn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\PNUDPxE1? MWG1JIQ> M1LXcGROW09? MoTsTWM2ODxzIN88US=> MX[yOFg4QTd7Nh?=
HCC1500 NWXRU2tvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmm4NUDPxE1? NUHhdIVbPSCm MWLEUXNQ M2f3[GlEPTB:MTFOwG0> M4\EXVI1QDd7N{m2
EFM-19 M3\rb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HpdlEh|ryP MWm1JIQ> MXzEUXNQ M2jKWGlEPTB:MTFOwG0> NHq4VXUzPDh5OUe5Oi=>
ZR-75-30 M2H6UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHZS2tYOSEQvF2= M{PkOVUh\A>? MYDEUXNQ M3\GWGlEPTB:MTFOwG0> NUOwcXE1OjR6N{m3PVY>
MDA-MB-361 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHaNUDPxE1? Mkn2OUBl NEnGUHZFVVOR NInuWlJKSzVyPEGg{txO NH;QcpYzPDh5OUe5Oi=>
T-47D NIXpWlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxJO69VQ>? MV61JIQ> M{Pxb2ROW09? MWXJR|UxRDFizszN MmH0NlQ5Pzl5OU[=
SK-BR-3 NV;3Z|RZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxJO69VQ>? MYS1JIQ> M1jrfGROW09? NVHoWnJVUUN3MEyxJO69VQ>? M{HXXVI1QDd7N{m2
UACC-732 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDJNUDPxE1? NVnzU5gzPSCm M174cmROW09? NEX5WpNKSzVyPEGg{txO MVyyOFg4QTd7Nh?=
BT-474 NEPqZphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKxJO69VQ>? MXW1JIQ> NYr5Z3ByTE2VTx?= MlHCTWM2ODxzIN88US=> NWLTcWRwOjR6N{m3PVY>
HCC202 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzzcnk1OSEQvF2= MoXKOUBl M2T6[WROW09? MXzJR|UxRDFizszN MkHzNlQ5Pzl5OU[=
MCF7 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfO[ZNyOSEQvF2= NFrRV4c2KGR? MXLEUXNQ NXTR[Yw2UUN3MEyxJO69VQ>? M4\XbFI1QDd7N{m2
MDA-MB-415 M33M[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DsUVEh|ryP MlGxOUBl NEDyXGJFVVOR M3vQNGlEPTB:MTFOwG0> M{X1RVI1QDd7N{m2
MDA-MB-453 NWW1e5BPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTESWI5OSEQvF2= M2C0SFUh\A>? NXy3eVVKTE2VTx?= MniwTWM2ODxzIN88US=> NHL6O4EzPDh5OUe5Oi=>
ZR-75-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTSWVQxOSEQvF2= NXLFRWx3PSCm NUf0[XNiTE2VTx?= MW\JR|UxRDFizszN MXSyOFg4QTd7Nh?=
HCC38 NFTufXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzDNUDPxE1? MWW1JIQ> M2DBWGROW09? MV;JR|UxRDFizszN MWeyOFg4QTd7Nh?=
HCC1419 NGnsNlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjxb2hIOSEQvF2= MoD3OUBl M2\zO2ROW09? NVLOOI9FUUN3MEyxJO69VQ>? NXXVeFA1OjR6N{m3PVY>
UACC-812 NIT5doRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7FU5IyKM7:TR?= M{LkcVUh\A>? NFrWVI1FVVOR MlvrTWM2ODxzIN88US=> M4nvTlI1QDd7N{m2
HCC1187 NWTKWZJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVyxJO69VQ>? NIjMfYg2KGR? NGHOXmZFVVOR MYTJR|UxRDFizszN MViyOFg4QTd7Nh?=
KPL-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\iNUDPxE1? NFzjdlk2KGR? M37jfGROW09? M4jP[WlEPTB:MTFOwG0> MXOyOFg4QTd7Nh?=
SUM-225 NVP6U4VCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO0cVEyKM7:TR?= MWG1JIQ> NEXqV|BFVVOR Mk\2TWM2ODxzIN88US=> NUXMVWVvOjR6N{m3PVY>
EFM-192A Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jCc|Eh|ryP M3q4RVUh\A>? M1rxdmROW09? Ml70TWM2ODxzIN88US=> M3jXe|I1QDd7N{m2
JIMT-1 M{fEWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVThZYZmOSEQvF2= M4\nUFUh\A>? M1\2NGROW09? M4nUSmlEPTB:MTFOwG0> NU\GRZVtOjR6N{m3PVY>
HCC1143 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDlNUDPxE1? M2Xm[|Uh\A>? M{XSS2ROW09? M4rjS2lEPTB:MTFOwG0> MkniNlQ5Pzl5OU[=
HCC2218 NWTwXGFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3TVZUyKM7:TR?= Mk\KOUBl M{fTeWROW09? M4rMeWlEPTB:MTFOwG0> NX;R[nN4OjR6N{m3PVY>
MDA-MB-468 MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvW[Wd2OSEQvF2= MVu1JIQ> NHPuWmhFVVOR NFnXXoFKSzVyPEGg{txO M2jRcFI1QDd7N{m2
BT-20 NX7CXoJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDvN2lZOSEQvF2= NYK3elZqPSCm NV3lcoUxTE2VTx?= Mn3rTWM2ODxzIN88US=> MYGyOFg4QTd7Nh?=
MDA-MB-435 MlvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;vNUDPxE1? MVG1JIQ> MkjrSG1UVw>? NFHNdHhKSzVyPEGg{txO MnH0NlQ5Pzl5OU[=
BT-549 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTCNUDPxE1? M3fabVUh\A>? MmrGSG1UVw>? NEfuSWFKSzVyPEGg{txO MlXhNlQ5Pzl5OU[=
HCC1806 NFXhRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWxJO69VQ>? NGjlVZE2KGR? MW\EUXNQ NWnxNYdIUUN3MEyxJO69VQ>? NFP3R2IzPDh5OUe5Oi=>
HCC1937 NHjySXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m0bVEh|ryP M{CwO|Uh\A>? NH\YWXJFVVOR NHW2ZVlKSzVyPEGg{txO NW[0W4s5OjR6N{m3PVY>
Hs578T NVGxfo9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvFWndMOSEQvF2= M{CxVFUh\A>? NHfvVnNFVVOR NVHzSHoyUUN3MEyxJO69VQ>? M2izOFI1QDd7N{m2
LN18 M3HkZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj3fFhSOjBizszN M1HRVlczKGh? MVfEUXNQ NE\GeZlKSzVyPEWg{txO M2n4cVI1PzRzMEe0
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LN18 MlPlSpVv[3Srb36gRZN{[Xl? NVixUIRJPSEQvF2= NUHTV5ppOjRiaB?= Mk\1SG1UVw>? NEnwOJJKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuW MnrINlQ4PDFyN{S=
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Saos-2 MYjGeY5kfGmxbjDBd5NigQ>? MXS1NEDPxE1? M1HQTlQ5KGh? NYTT[G9kUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? NEXoTJEzPDd{N{[2NC=>
MG-63 M3npdWZ2dmO2aX;uJGF{e2G7 NUDvUYZGPTBizszN NILnSXE1QCCq M2nad2lvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> NFLsT4EzPDd{N{[2NC=>
SJSA-1 NFvSV3pHfW6ldHnvckBCe3OjeR?= MX61NEDPxE1? Ml72OFghcA>? M2nXcmlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> M4mxRVI1PzJ5Nk[w
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MG-63 NXT5SII{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPyOVAh|ryP Mn\sOFghcA>? NFHab4NKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MoSzNlQ4Ojd4NkC=
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HCT116 MUTGeY5kfGmxbjDBd5NigQ>? NUT0WpdmPSEQvF2= M{LRXlI1KGh? NHfZdZFFVVOR NHvWZldT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> NG\tcVYzPDZ|MUG0Oy=>
U87 NVvz[pl1TnWwY4Tpc44hSXO|YYm= Mo\yOUDPxE1? MXSyOEBp NUnh[JFxTE2VTx?= NXWxbW04WmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NVrCdlMzOjR4M{GxOFc>
GBM MYjBdI9xfG:|aYOgRZN{[Xl? Mn;MNu69VQ>? MXO0PIg> M4ewbmROW09? NWfLV2F2cW6mdXPl[EBpcWeqZYKgcIV3\Wy|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>? M2LQXFI1PTByNEmy
BON NXfYOFMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml74NU02|ryP M2PIbVczcA>? MkDO[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NHrKXIMzPDR2M{WyNy=>
BON MnLjRZBweHSxc3nzJGF{e2G7 MVmxMVXPxE1? Mkj0NlRp MVjpcoNz\WG|ZYOgZZBweHSxc3nz MUeyOFQ1OzV{Mx?=
H1975 NV;uOnQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXRenJsOC5|LUmuOu69VQ>? NGTwVWI4Omh? MorFSG1UVw>? M1KySWlEPTB;MT6zPFXPxE1? Mm\nNlQ{Ozd6NE[=
H1975 MVrBdI9xfG:|aYOgRZN{[Xl? M2DzSlLPxE1? Mmm2NlRp MYfEUXNQ NGXPXFJqdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>? NELXNHMzPDN|N{i0Oi=>
T-ALL NG\GdmxCeG:ydH;zbZMhSXO|YYm= MlvnZoV1f2WnbjCxMlQh[W6mIEWuN{BuVSCjdDCyOIgh[W6mIECuPUBidmRiNT61JI1OKGG2IES4bEBqdiCmaX\m[ZJmdnRiY3XscEBtcW6n M4LZb|I1KG:{IES4bC=> M1;IZmROW09? MnvUZYZn\WO2czD0bIUhWEl|SzDwZZRpf2G7IHnuJHQuSUyOIHPlcIwhdGmwZYO= M2LNU|I1OzFyN{O2
BCR-ABL MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DBN|AvOjVvMUFOwG0> NX\TOVhZPGR? MXrzbYdvcW[rY3HueIx6KGmwaHnibZQh[2WubDDwdo9tcW[ncnH0bY9v MnnGNlQzPDR4MUK=
LC-1/SQSF MkjISpVv[3Srb36gRZN{[Xl? M1HLOlPPxE1? NFH6NlYzPGh? NIC0V41FVVOR MofJ[IVkemWjc3WgUnJHOiCycn;0[YlvKGyndnXs NGG1XlUzOzl6MEC5Ny=>
Primary CLL cells M4LLe2Fxd3C2b4Ppd{BCe3OjeR?= MYGxMVEx|ryP MljtOFhp NETmb45qdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ Ml\FNlM5PTB6MEe=
Primary CLL cells MUHLbY5ie2ViQYPzZZk> NEXuZ4kz|ryP MmjpN|BucW5? MlHI[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? NV7sVFIxOjN6NUC4NFc>
Primary CLL cells Moe3R5l1d3SxeHnjJGF{e2G7 MVey{txO MWiyOIg> MmC0bY5lfWOnczDj[YxtKGO7dH;0c5hq[2m2eR?= MV2yN|g2ODhyNx?=
human NSCLC cell lines MlvERZBweHSxc3nzJGF{e2G7 MorZNE4yOjVvNN88US=> NWr1dZFPOjSq MXnEUXNQ NWHpUWJKUUN3MIOgdoFv\2W|IH\yc40hOC52LUNOwG0> MnfTNlM2PjJ2N{K=
human HCC cell lines M3rIZWNmdGxidnnhZoltcXS7IHHzd4F6 MWSwMlAxPS1zzszN NWPsZWJMPDiq MXzJR|UxRTIQvF2= NWPRU445OjN2OEm5PVk>
Huh7 NWDUeo9DU2mwYYPlJGF{e2G7 NGPsPW0y|ryP MXm0PIg> NIjTeXh{cWewaf-shYNidnSueTDy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NGnEW|EzOzR6OUm5PS=>
SK-HEP1 NVi2cHFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULFVFVEOS1{MN88US=> NUjWeZhFPzKq MkPnSG1UVw>? Mk\nTWM2OO,:nEJOwG0> MWeyN|Q4QTF|Nh?=
786-0 NVXuUFVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv2SotIOS1{MN88US=> NYfhZYJIPzKq M2fBbGROW09? MmizTWM2OO,:nEJOwG0> NVLOPJE6OjN2N{mxN|Y>
JVM2 M{i1NmN6fG:2b4jpZ4l1gSCjc4PhfS=> M1yzOVAvOi1{MN88US=> NF7B[ZE4Omh? M4q3WmROW09? M3flTWlEPTB;MD65{txO MVyyN|I{QDZ|OR?=
EHEB MkD0R5l1d3SxeHnjbZR6KGG|c3H5 MYOwMlIuOjEQvF2= MlrOO|Jp NI\ySIpFVVOR MnHKTWM2OD1yLkhOwG0> MV:yN|I{QDZ|OR?=
MEC2 NFLNfpFEgXSxdH;4bYNqfHliYYPzZZk> NVLzemQxOC5{LUKw{txO MoftO|Jp MljYSG1UVw>? MmfMTWM2OD1yLkhOwG0> MljDNlMzOzh4M{m=
primary B-CLL lymphocytes M{LITWFxd3C2b4Ppd{BCe3OjeR?= MUfJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m NF7PfnQzPGh? NE\3d5BFVVOR MlKyTWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> NYP6RVNOOjN{M{i2N|k>
primary B-CLL lymphocytes MlzST4lv[XOnIFHzd4F6 MVXJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m MkDJNlRp NWXnZZM6cW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> NELXS2szOzJ|OE[zPS=>
human NSCLC NVfjSFh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fPdlAvPS1{zszN NHTMcY44Omh? MYDJR|UxRTIQvF2= NWX2N29MOjJ5OEGzPVM>
human NSCLC MXjLbY5ie2ViQYPzZZk> MUGx{txO MlPYNlRp NH32fZNqdmirYnn0d{B1cGViQXv0M41VV1Jic3nncoFtcW6pIIDheIh4[XliYYSgN4gh[W[2ZYKgeJJm[XSvZX70 MY[yNlc5OTN7Mx?=
Y1 cell line MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWmwMlHPxE1xMd88US=> M4TpVFI1cA>? NHrUU3lFVVOR NVrDdWhvcW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= Mle3NlI3QTJ7MES=
PIK3CA-mutant MCF7 MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? MkTGO|Jp NHfaNppIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= MYWyNlY2Ozl4Nx?=
PIK3CA-mutant MCF7 NFfjTW9McW6jc3WgRZN{[Xl? Mn:5TWM2OD1zMUVCtVNvVQ>? NGTRO2k4Omh? MXLJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| NV;GOpc6OjJ4NUO5Olc>
MCF7-myr-Akt Ml\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\HTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? NEjsWo84Omh? M2LEWWdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P M1jk[lIzPjV|OU[3
colon cancer cell lines MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO1[HN7OC1zMN88US=> M{PucFczcA>? M3\6e2ROW09? NU\je4VPUUN3ME2x{txO M1TMd|IzPTR|OEW3
gastric cancer cell lines MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:4NE0yOM7:TR?= MkfSO|Jp MVfEUXNQ M3fC[2lEPTB;Mj21{txO NWrjTJVxOjJ3NEO4OVc>
HCT-116/HT-29/MKN-45 NVn3VVBpSXCxcITvd4l{KEG|c3H5 M3T3O|LPxE1? M2XjflQ5cA>? MlL3d4hq\nRiaX6gS|IheGijc3W= NHrmUpQzOjV2M{i1Oy=>
HT-29 and HCT-116 NGDES5lE[XOyYYPlJIF{e2G7 NYnTTFI6Pc7:TR?= NW\6dpVSOjSq MYXpcoR2[2W|IHPhd5Bie2ViYXP0bZZqfHl? MV:yNlU1Ozh3Nx?=
MM cell lines M3jvUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fWU|Ex|ryP NWWyVGJTOjSq MlzBSG1UVw>? NGPE[GFKSzVyII\hdolmeyCjbX;u[{BlcW[oZYLlcpQh[2WubDDsbY5meyCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVv[2V? MkT3NlIzODd2OEW=
ARP-1 MWHBdI9xfG:|aYOgRZN{[Xl? NHrLZYQyOM7:TR?= Mo\5NlRp NHu4dYdFVVOR NVfWV5hIcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> NGWwNXgzOjJyN{S4OS=>
SNU-601 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOyVXBrPzKq NEjhdlVFVVOR NX70fo5LUUN3ME2wMlgyPsLzMD6wOlPPxE1? NF\xVZMzOjF3OUixOC=>
SNU-1 NUP1eYlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTDPZI4Omh? MnPwSG1UVw>? MVTJR|UxRTFwMEiyxtExNjB{ON88US=> MmfTNlIyPTl6MUS=
SNU-668 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLhO|Jp M{PKcWROW09? MWPJR|UxRTFwNUe5xtExNjB5NN88US=> NH7iXXczOjF3OUixOC=>
AGS NHnzOnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fTUFczcA>? MULEUXNQ MnzOTWM2OD1zLkexOOKyOC5zMUhOwG0> MYCyNlE2QThzNB?=
SNU-216 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L4bVczcA>? MUTEUXNQ M1XRUmlEPTB;Mj62PVLDuTBwMEiy{txO MXOyNlE2QThzNB?=
SNU-5 NV7uW4J2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrnT2g4Omh? MlftSG1UVw>? NVu3d5ZRUUN3ME2xMlM2OcLzMD6wPVHPxE1? MXWyNlE2QThzNB?=
SNU-638 NWPjTnlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX23Nog> MWfEUXNQ M2DnbGlEPTB;Mj6yPFLDuTBwMEWz{txO M3\mbVIzOTV7OEG0
SNU-16 Mny3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHEOVR4PzKq MVHEUXNQ NULYW21SUUN3ME2xMlU4O8LzMD6wNFHPxE1? M2XIXlIzOTV7OEG0
SNU-484 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzMO|Jp MV3EUXNQ NXjISlVSUUN3ME2xMlczQMLzMD6wOFXPxE1? MlT3NlIyPTl6MUS=
SNU-620 MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLscJI4Omh? NYXxS49rTE2VTx?= NUfqfm96UUN3ME2yMlk{QcLzMD6wNFHPxE1? MUKyNlE2QThzNB?=
SNU-719 NFLG[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDofZcxPzKq MoLPSG1UVw>? NHiwR4FKSzVyPUOuNFM4yrFyLkCzNu69VQ>? NX7xb3ZlOjJzNUm4NVQ>
glioma cell lines MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnz5O|Jp M1vSXmlEPTB;MT2y{txO NEntbFgzOjB4NUC4NC=>
U87 M2iwUmFxd3C2b4Ppd{BCe3OjeR?= M4jrVFLPxE1? NUHBUYZIPzKq Mn2xbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= NHntWJAzOjB4NUC4NC=>

... 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 individually and in order:
5% DMSO+30% PEG 300+ddH2O
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
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01870726 Completed 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
NCT01473901 Active, not recruiting Glioblastoma Novartis Pharmaceuticals|Novartis December 30, 2011 Phase 1
NCT01633060 Active, not recruiting Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis October 3, 2012 Phase 3
NCT02756247 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
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.

Handling Instructions

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID