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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USD 320 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 MULDfZRwfG:6aXOgRZN{[Xl? MXm3NkBp M1PUbWROW09? Ml22R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?= NUTwRldROjR7MECyOlY>
DU145 MWLDfZRwfG:6aXOgRZN{[Xl? MoSwO|IhcA>? NX3JW2Z2TE2VTx?= MlP4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCOS1KxJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMEC0N|Uh|ryP MVSyOFkxODJ4Nh?=
A2780 NUPlXYJOS3m2b4TvfIlkKEG|c3H5 M1nidVczKGh? NInNR3lFVVOR M{XaSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2= NUnofnZTOjR7MECyOlY>
U87MG NH;DcnFEgXSxdH;4bYMhSXO|YYm= MoexO|IhcA>? MXXEUXNQ NXn4OXJrS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjl6IN88US=> NFHxcGczPDlyMEK2Oi=>
A2780 NGizeWNHfW6ldHnvckBCe3OjeR?= MV6xJIg> NX7tTZVpTE2VTx?= NETJPHlKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNFU2KM7:TR?= NXvTNWJQOjR7MECyOlY>
DU145 MULGeY5kfGmxbjDBd5NigQ>? NX7RZo5LOSCq M3LPU2ROW09? Ml3jTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? M2jMblI1QTByMk[2
A2780 M3PRVWZ2dmO2aX;uJGF{e2G7 MlTzNUBp NUjo[5NoTE2VTx?= MVvJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>? NV3ZR3NZOjR7MECyOlY>
MCF7 Ml\NSpVv[3Srb36gRZN{[Xl? NVXyb4JrOSCq MUHEUXNQ Ml3nTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO MWKyOFkxODJ4Nh?=
U87MG NEXHXlNHfW6ldHnvckBCe3OjeR?= MnvENUBp Moi0SG1UVw>? NG[wTWdKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR|UxKG:oIECuNVMh|ryP NVywNVdvOjR7MECyOlY>
A2780 NX:0TYdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3G3c|czKGh? NFSy[I1FVVOR NInmSI5GSzVyPUCuOVIh|ryP NVzldVBwOjR7MECyOlY>
SKMES-1 MYrDfZRwfG:6aXOgRZN{[Xl? MlTjNUDPxE1? MonqO|IhcA>? Mlf1TY5lfWOnczDj[YxtKGSnYYTo M1Tud|I3ODF|M{G4
H596 M1u1c2Z2dmO2aX;uJGF{e2G7 MnrSNUDPxE1? NHLOSllKdXCjaYLzJINmdGxibXnndoF1cW:w Mkf2NlYxOTN|MUi=
HCC2450 NEfDTWRHfW6ldHnvckBCe3OjeR?= M2Sxd|Eh|ryP MkX2TY1x[Wm{czDj[YxtKGmwdnHzbY9v NHPtbIIzPjBzM{OxPC=>
A549 NFvWZlNHfW6ldHnvckBCe3OjeR?= MWK1NFAhdk1? MmnaOFghcA>? NV3DdXp6TE2VTx?= MX3Jcohq[mm2czDBb5Qh[WO2aY\heIlwdg>? Mn60NlU6Ozd{OUm=
A549 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4CxclEh|ryP NF;DR5A4OiCq M1rUSGROW09? NEXQe5pKdmirYnn0d{Bk\WyuIHfyc5d1cA>? MYGyOVk{PzJ7OR?=
H522 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7jNUDPxE1? NILwR2s4OiCq M1OyXGROW09? MX;Jcohq[mm2czDj[YxtKGe{b4f0bC=> MUCyOVk{PzJ7OR?=
LNCaP MmTZSpVv[3Srb36gRZN{[Xl? M2XEcVEh|ryP M{LRPXN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| NW\GZ5pSOjV|NkC3PVk>
LNCaP95 MljmSpVv[3Srb36gRZN{[Xl? NHTBbHMyKM7:TR?= M{n2OXN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| NEPGUWwzPTN4MEe5PS=>
HCT-15 MonMRZBwfG:|aYOgRZN{[Xl? M4rYSVExKM7:TR?= MmO4OFghcA>? NXHNUpNpTE2VTx?= NITXNnlKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVUh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= M1zPVFI2OTV{MkS1
HCT-116 MX;BdI91d3OrczDBd5NigQ>? NE\pTmcyOCEQvF2= M37lR|Q5KGh? MYnEUXNQ M13LbWlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NVnJPFBkOjVzNUKyOFU>
NCI-H460 NUX3UZhzSXCxdH;zbZMhSXO|YYm= M{nmdlExKM7:TR?= M3z0NFQ5KGh? MVfEUXNQ NEjpNIlKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCQQ1mtTFQ3OCClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u Ml3uNlUyPTJ{NEW=
SKOV-3 NUi4N4xHSXCxdH;zbZMhSXO|YYm= MYKxNEDPxE1? MkL3OFghcA>? MVTEUXNQ MYrJcoR2[2W|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MXGyOVE2OjJ2NR?=
BSY-1 M3SxfGFxd3Sxc3nzJGF{e2G7 NH7IOXUyOCEQvF2= M3;CS|Q5KGh? MXfEUXNQ MYPJcoR2[2W|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v M3T3SVI2OTV{MkS1
MKN-1 NIfibVBCeG:2b4Ppd{BCe3OjeR?= NX36Z3U2OTBizszN MUi0PEBp NEDMdJVFVVOR NGrXPI1KdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MW[yOVE2OjJ2NR?=
NCI-H522 MVnBdI91d3OrczDBd5NigQ>? NVXIc2xtOTBizszN Ml61OFghcA>? NGXJR5JFVVOR NVjWZ45FUW6mdXPld{BieG:ydH;zbZM> NXnLTW9vOjVzNUKyOFU>
OVCAR-3 MXrBdI91d3OrczDBd5NigQ>? NWfGNpFGOTBizszN Mn[4OFghcA>? NXL2TpFwTE2VTx?= MU\JcoR2[2W|IHHwc5B1d3Orcx?= NYD1XIgyOjVzNUKyOFU>
HBC-5 M{HqUmFxd3Sxc3nzJGF{e2G7 MUGxNEDPxE1? NUTxRnlyPDhiaB?= Ml;SSG1UVw>? MUTJcoR2[2W|IHHwc5B1d3Orcx?= MWCyOVE2OjJ2NR?=
RXF-631L NEPqZXVCeG:2b4Ppd{BCe3OjeR?= NXHxZZpkOTBizszN NX7FNoRwPDhiaB?= NWTFNZQ5TE2VTx?= MlThTY5lfWOnczDhdI9xfG:|aYO= M1j3VFI2OTV{MkS1
MKN-45 M4rqVWFxd3Sxc3nzJGF{e2G7 MVWxNEDPxE1? MVm0PEBp MXrEUXNQ MXzJcoR2[2W|IHHwc5B1d3Orcx?= M4S2Z|I2OTV{MkS1
BON-1 NHy2OIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr3bopOPTByIH7N MXuxNEBl NIK1[5RFVVOR NXjZ[|hVUW6qaXLpeJMh[2WubDDndo94fGh? Mn\PNlUxOjZ{OUK=
BON-1 MmfXSpVv[3Srb36gRZN{[Xl? M{D6elUxOCCwTR?= M4q1[VQhcA>? NGmyPFJFVVOR MV;Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| NIHTZ|AzPTB{NkK5Ni=>
QGP-1 Mn;rSpVv[3Srb36gRZN{[Xl? MYK1NFAhdk1? NUfBcmJZPCCq Mof1SG1UVw>? M33rWWlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= M4PBRVI2ODJ4Mkmy
Huh7 Mm\ISpVv[3Srb36gRZN{[Xl? NX7HZ5BGOSEQvF2= NUPke|JUOSCq NUnnUI41TE2VTx?= M{Ty[GlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgV4VzPDd2 NWCzPFlyOjVyMES0NFM>
BNL NFvRe3ZHfW6ldHnvckBCe3OjeR?= MYGxJO69VQ>? M1PDblEhcA>? M2DxNGROW09? MYjJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Y> M3f6NlI2ODB2NECz
MDA-MB-175 NVLC[lRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\JcoQyKM7:TR?= MY[1JIQ> NVTn[mN4TE2VTx?= MonaTWM2ODxzIN88US=> MoLxNlQ5Pzl5OU[=
MDA-MB-134 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnl[osyKM7:TR?= NEfieYU2KGR? M3zsPGROW09? NFvFVHZKSzVyPEGg{txO MXmyOFg4QTd7Nh?=
HCC1500 M{K4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT4WYduOSEQvF2= M3\ZNFUh\A>? MV7EUXNQ MnTNTWM2ODxzIN88US=> MmXCNlQ5Pzl5OU[=
EFM-19 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfENI8yKM7:TR?= NWPENmdiPSCm MnPLSG1UVw>? M{iz[WlEPTB:MTFOwG0> NWDqUVlQOjR6N{m3PVY>
ZR-75-30 Mn7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XW[|Eh|ryP M1fESFUh\A>? Ml;wSG1UVw>? MWHJR|UxRDFizszN NFj5N5MzPDh5OUe5Oi=>
MDA-MB-361 NHrDb4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\kcVEh|ryP MUW1JIQ> MnWwSG1UVw>? NFXaV2RKSzVyPEGg{txO NVTxNFRFOjR6N{m3PVY>
T-47D NEPD[XlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2xJO69VQ>? M1rscFUh\A>? MnLSSG1UVw>? MWrJR|UxRDFizszN M2jHdlI1QDd7N{m2
SK-BR-3 NVniNGI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzIN5UyKM7:TR?= NG\GZpc2KGR? NUDheGlTTE2VTx?= MWTJR|UxRDFizszN NX;XcI5rOjR6N{m3PVY>
UACC-732 NEXHNGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOxJO69VQ>? MU[1JIQ> NXPMflE4TE2VTx?= M{jsUWlEPTB:MTFOwG0> MnriNlQ5Pzl5OU[=
BT-474 NF3ZN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjGNUDPxE1? M1:4V|Uh\A>? Mne4SG1UVw>? M2nwO2lEPTB:MTFOwG0> Mnu4NlQ5Pzl5OU[=
HCC202 Mmq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTZOXQyKM7:TR?= NXrEVI5mPSCm Mn3USG1UVw>? NInkZ3BKSzVyPEGg{txO Ml3FNlQ5Pzl5OU[=
MCF7 NX3qO49ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLpOFYyKM7:TR?= MXi1JIQ> MoT5SG1UVw>? NGO4XJRKSzVyPEGg{txO M3rPN|I1QDd7N{m2
MDA-MB-415 M37PSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHRemJUOSEQvF2= MoG3OUBl M1z2dWROW09? M2fEUGlEPTB:MTFOwG0> M33Z[lI1QDd7N{m2
MDA-MB-453 MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGCzV4wyKM7:TR?= M4XrW|Uh\A>? NUP2cnJZTE2VTx?= MUHJR|UxRDFizszN MV[yOFg4QTd7Nh?=
ZR-75-1 MlfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rYeVEh|ryP MoX1OUBl MV3EUXNQ M1\0TGlEPTB:MTFOwG0> NFnDVG8zPDh5OUe5Oi=>
HCC38 NFPQZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPxXnYyKM7:TR?= M1PaW|Uh\A>? MlO5SG1UVw>? M2LMcmlEPTB:MTFOwG0> NHSyb5QzPDh5OUe5Oi=>
HCC1419 M3\QOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWOw[IxHOSEQvF2= MUC1JIQ> MWXEUXNQ NFq4cphKSzVyPEGg{txO MYeyOFg4QTd7Nh?=
UACC-812 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLzOFcxOSEQvF2= MU[1JIQ> NW\K[I5QTE2VTx?= MnLITWM2ODxzIN88US=> M1TSe|I1QDd7N{m2
HCC1187 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxJO69VQ>? M12ybVUh\A>? NV\uTnVuTE2VTx?= MWrJR|UxRDFizszN MmPYNlQ5Pzl5OU[=
KPL-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[xJO69VQ>? NH\qb402KGR? MmexSG1UVw>? MWDJR|UxRDFizszN MknoNlQ5Pzl5OU[=
SUM-225 MlnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHDRmhsOSEQvF2= NWHj[XJTPSCm MUPEUXNQ NEfx[VBKSzVyPEGg{txO NIfHW3YzPDh5OUe5Oi=>
EFM-192A NIDyUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlyxNUDPxE1? M1r5RVUh\A>? NEnIZ2lFVVOR MXPJR|UxRDFizszN MkDZNlQ5Pzl5OU[=
JIMT-1 NWrORmpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2KxcVEh|ryP NYjPVJl7PSCm NGXFcW5FVVOR MX3JR|UxRDFizszN MWKyOFg4QTd7Nh?=
HCC1143 NIPocY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWixJO69VQ>? NYXyNmpWPSCm MlnQSG1UVw>? NF:wWIlKSzVyPEGg{txO Ml7XNlQ5Pzl5OU[=
HCC2218 M{nWd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnS5NUDPxE1? MV[1JIQ> M3HGcmROW09? MYnJR|UxRDFizszN NGS0SWUzPDh5OUe5Oi=>
MDA-MB-468 NGq5[plIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSxJO69VQ>? MXm1JIQ> MUTEUXNQ NHvybGVKSzVyPEGg{txO NHvsNZgzPDh5OUe5Oi=>
BT-20 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TuTFEh|ryP NXLvXlRFPSCm NXjuPWl4TE2VTx?= MlTxTWM2ODxzIN88US=> MVeyOFg4QTd7Nh?=
MDA-MB-435 M3;3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTuOWYyKM7:TR?= NWnQXmhDPSCm NFjCdJNFVVOR M3TOcmlEPTB:MTFOwG0> NH7TcZEzPDh5OUe5Oi=>
BT-549 NET2ZZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWxJO69VQ>? MYO1JIQ> Mn7ySG1UVw>? NXfSTG5oUUN3MEyxJO69VQ>? NHjwd20zPDh5OUe5Oi=>
HCC1806 M2DRR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInqWIYyKM7:TR?= NE\wd2E2KGR? NG\T[VVFVVOR MoLxTWM2ODxzIN88US=> M33vc|I1QDd7N{m2
HCC1937 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHoNUDPxE1? M4[4T|Uh\A>? Mo\MSG1UVw>? MWLJR|UxRDFizszN NHLqcFczPDh5OUe5Oi=>
Hs578T NYj2NIluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6xJO69VQ>? NVn0flJSPSCm M2juNWROW09? MUnJR|UxRDFizszN NULNOVBiOjR6N{m3PVY>
LN18 NYXZb|FwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXyyNEDPxE1? NHPZdms4OiCq NHr2T2ZFVVOR MlvKTWM2ODx3IN88US=> MljiNlQ4PDFyN{S=
LN229 NV3IXmNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXmWo5SOjBizszN MXm3NkBp MVXEUXNQ NF7r[2FKSzVyPEWg{txO NHr0UVEzPDd2MUC3OC=>
LNZ308 NHHDeoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[2Zmw{OjBizszN Moj0O|IhcA>? NYPXZnl1TE2VTx?= MVLJR|UxRDVizszN Mne5NlQ4PDFyN{S=
T98G Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKyNEDPxE1? NUPGfHVwPzJiaB?= NFe2V2NFVVOR MoLqTWM2ODx3IN88US=> MVeyOFc1OTB5NB?=
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LN18 M{S3O2Z2dmO2aX;uJGF{e2G7 MnvrOUDPxE1? M3nZZVI1KGh? MYfEUXNQ MmC0TY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? Ml;aNlQ4PDFyN{S=
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MG-63 NXPJSnVlTnWwY4Tpc44hSXO|YYm= NF;Zb5I2OCEQvF2= NITWWpA1QCCq NHHmRZBKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v MVSyOFczPzZ4MB?=
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MG-63 NGrETmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWS1NEDPxE1? MVq0PEBp MWDJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? MmDDNlQ4Ojd4NkC=
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FaDu NF36T2pHfW6ldHnvckBCe3OjeR?= MUS1JO69VQ>? NVjOO2FROjRiaB?= MlvuSG1UVw>? NWDRTnVnWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NYfaSmhNOjR4M{GxOFc>
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HCT116 M1SzNmZ2dmO2aX;uJGF{e2G7 MXe1JO69VQ>? NWXxflFwOjRiaB?= NGfmSXVFVVOR Ml;RVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= MV6yOFY{OTF2Nx?=
U87 NHu5dI5HfW6ldHnvckBCe3OjeR?= MXS1JO69VQ>? NE[xPZQzPCCq M2rTc2ROW09? NWLV[lVNWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NX\IcYtmOjR4M{GxOFc>
GBM MnyxRZBweHSxc3nzJGF{e2G7 MlnXNu69VQ>? NXW1fJJtPDiq M2noc2ROW09? MYLpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5 MWKyOFUxODR7Mh?=
BON MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M164R|EuPc7:TR?= NVLvU3g6PzKq M{PRUIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MVqyOFQ1OzV{Mx?=
BON NGT2WlNCeG:ydH;zbZMhSXO|YYm= NGnB[VYyNTYQvF2= NFS4UXgzPGh? NVK0fnZTcW6lcnXhd4V{KGGyb4D0c5Nqew>? NFHDb5MzPDR2M{WyNy=>
H1975 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XIWVAvOy17LkdOwG0> MmXrO|Jp MYHEUXNQ MYTJR|UxRTFwM{i1{txO M{LZ[VI1OzN5OES2
H1975 NX3BdGUxSXCxcITvd4l{KEG|c3H5 Ml7rNu69VQ>? NX7LSphnOjSq M{C3NWROW09? NXG5dpB2cW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl? NYXPZ|VbOjR|M{e4OFY>
T-ALL M{m4TmFxd3C2b4Ppd{BCe3OjeR?= M{SzeYJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= NXLWdG1NOjRib4KgOFhp NYC2NW1sTE2VTx?= MWfh[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= M4DJWlI1OzFyN{O2
BCR-ABL NHrHSWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\oUVAvOjVvMUFOwG0> M4SwZlRl M{PLZpNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? MnPmNlQzPDR4MUK=
LC-1/SQSF M3LGW2Z2dmO2aX;uJGF{e2G7 NFWw[5I{|ryP M2j6TFI1cA>? MnvCSG1UVw>? NEHwU5dl\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw> MnLaNlM6QDByOUO=
Primary CLL cells Ml\zRZBweHSxc3nzJGF{e2G7 MWmxMVEx|ryP MkW2OFhp MV7pcoR2[2W|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz NFK1bXEzOzh3MEiwOy=>
Primary CLL cells MXrLbY5ie2ViQYPzZZk> NI[5XJUz|ryP Mo\KN|BucW5? NYnzeVJn\GWlcnXhd4VlKFCLM1ugZYN1cX[rdIm= NVewPYh3OjN6NUC4NFc>
Primary CLL cells MVfDfZRwfG:6aXOgRZN{[Xl? NF7ve5Uz|ryP MV[yOIg> M3nFT4lv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= NEfvOFczOzh3MEiwOy=>
human NSCLC cell lines Ml;KRZBweHSxc3nzJGF{e2G7 MnPINE4yOjVvNN88US=> MkTLNlRp Mn;BSG1UVw>? NYCwN2xyUUN3MIOgdoFv\2W|IH\yc40hOC52LUNOwG0> MYKyN|U3OjR5Mh?=
human HCC cell lines MVTD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NEHVSYMxNjByNT2x{txO NEHjenQ1QGh? M1rE[GlEPTB;Md88US=> NWXOOmhuOjN2OEm5PVk>
Huh7 MV;LbY5ie2ViQYPzZZk> M1PocFHPxE1? MmH1OFhp NXrKe2lQe2mpbnpvsKFk[W62bImgdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MWqyN|Q5QTl7OR?=
SK-HEP1 MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzMSXBEOS1{MN88US=> MYW3Nog> Mn3zSG1UVw>? MlLOTWM2OO,:nEJOwG0> MUCyN|Q4QTF|Nh?=
786-0 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4G2dFEuOjEQvF2= NVe0TmhMPzKq MV7EUXNQ NHP5dHFKSzVy78{cNe69VQ>? NILCdWgzOzR5OUGzOi=>
JVM2 MWfDfZRwfG:6aXPpeJkh[XO|YYm= NEH2U5UxNjJvMkFOwG0> Ml;yO|Jp MVPEUXNQ NXzIPW9KUUN3ME2wMlnPxE1? MkfqNlMzOzh4M{m=
EHEB M3fO[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NHz4cWIxNjJvMkFOwG0> NIr1UFQ4Omh? MY\EUXNQ NUXlSJFWUUN3ME2wMlfPxE1? M1WzelI{OjN6NkO5
MEC2 NWj6SJlmS3m2b4TvfIlkcXS7IHHzd4F6 MljaNE4zNTJyzszN NXS5fHJwPzKq M{DBR2ROW09? NVvjbZJiUUN3ME2wMlfPxE1? NIOyXm8zOzJ|OE[zPS=>
primary B-CLL lymphocytes MYLBdI9xfG:|aYOgRZN{[Xl? NV3vZnJXUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= NHzjNlAzPGh? MVfEUXNQ M2DEVmlEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM> NETicFgzOzJ|OE[zPS=>
primary B-CLL lymphocytes MX3LbY5ie2ViQYPzZZk> Mm\CTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MnvYNlRp M17qU4lvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u M4LpTFI{OjN6NkO5
human NSCLC M{XqNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmwMlUuOs7:TR?= MXe3Nog> MWXJR|UxRTIQvF2= M3;BN|IzPzhzM{mz
human NSCLC NH\0ToVMcW6jc3WgRZN{[Xl? M3raOFHPxE1? MlXMNlRp MUnpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 NWjn[I9JOjJ5OEGzPVM>
Y1 cell line NFL6eJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjPNE4y|ryPL{JOwG0> M3[4SlI1cA>? MYfEUXNQ NXTHVIg{cW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= MWqyNlY6OjlyNB?=
PIK3CA-mutant MCF7 MnjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvwc5VIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= MY[3Nog> Mn3tS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? M4jOWlIzPjV|OU[3
PIK3CA-mutant MCF7 M1XQT2tqdmG|ZTDBd5NigQ>? MmjLTWM2OD1zMUVCtVNvVQ>? MnvYO|Jp MonUTWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= NEnRW|kzOjZ3M{m2Oy=>
MCF7-myr-Akt NIfzXVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvsfIpIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= Ml[yO|Jp NXq3[|I2T0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= M3vFVFIzPjV|OU[3
colon cancer cell lines M1Ptd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOwMVEx|ryP MoHZO|Jp MVHEUXNQ NYP6UXNYUUN3ME2x{txO M2LTUFIzPTR|OEW3
gastric cancer cell lines NH6wSYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnub3cxOC1zMN88US=> MmfXO|Jp NHr2cHpFVVOR NUf2SpZvUUN3ME2yMVXPxE1? Mn;RNlI2PDN6NUe=
HCT-116/HT-29/MKN-45 NWHlXVRESXCxcITvd4l{KEG|c3H5 MWOy{txO MXS0PIg> NHu5Tod{cGmodDDpckBIOiCyaHHz[S=> NWGySlZxOjJ3NEO4OVc>
HT-29 and HCT-116 MXvDZZNx[XOnIHHzd4F6 NF\hSYk2|ryP NFfmPHkzPGh? NH64[XpqdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm= NUO4dYt6OjJ3NEO4OVc>
MM cell lines MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfW[JhKOTEQvF2= MYKyOIg> M2XBbWROW09? M4LOc2lEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? NYTzV3NDOjJ{MEe0PFU>
ARP-1 NV7uT5htSXCxcITvd4l{KEG|c3H5 NUnPVmViOTEQvF2= MkXvNlRp NVHnXHR3TE2VTx?= M2X5d4lv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= MkTvNlIzODd2OEW=
SNU-601 NHLkbFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTtO|Jp M2nVXmROW09? NVvucXlbUUN3ME2wMlgyPsLzMD6wOlPPxE1? M4HsUlIzOTV7OEG0
SNU-1 NH;veFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:3Nog> M{XO[mROW09? M3P5SmlEPTB;MT6wPFLDuTBwMEK4{txO M1vlT|IzOTV7OEG0
SNU-668 M4XHOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWG3Nog> NF;Mc4FFVVOR NXrDdlhXUUN3ME2xMlU4QcLzMD6wO|TPxE1? NXvpOW1qOjJzNUm4NVQ>
AGS MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnhOJc4Omh? NUL1OFRGTE2VTx?= M4\RT2lEPTB;MT63NVTDuTBwMUG3{txO M1HkfVIzOTV7OEG0
SNU-216 NH72ZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVm3Nog> NWjudZc1TE2VTx?= MYXJR|UxRTJwNkmyxtExNjB6Mt88US=> MWOyNlE2QThzNB?=
SNU-5 M1v3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXD[YtNPzKq NXjyeohbTE2VTx?= M{Lrc2lEPTB;MT6zOVHDuTBwMEmx{txO NEPBcW4zOjF3OUixOC=>
SNU-638 NHj6e4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnmS2R{PzKq NF3B[YtFVVOR NHnEUZNKSzVyPUKuNlgzyrFyLkC1N:69VQ>? MnrTNlIyPTl6MUS=
SNU-16 MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLMO|Jp M{DrNGROW09? NXe4UlNKUUN3ME2xMlU4O8LzMD6wNFHPxE1? M4f4VFIzOTV7OEG0
SNU-484 Mo[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHjR4M4Omh? MXTEUXNQ NV\HTJBKUUN3ME2xMlczQMLzMD6wOFXPxE1? MmPZNlIyPTl6MUS=
SNU-620 NF7aS4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPWTGY4Omh? MlzQSG1UVw>? NV\RSWNUUUN3ME2yMlk{QcLzMD6wNFHPxE1? NUL6eWpuOjJzNUm4NVQ>
SNU-719 NI\nOHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fLXlczcA>? NGj2OFJFVVOR MnLZTWM2OD1|LkCzO:KyOC5yM{NOwG0> MYmyNlE2QThzNB?=
glioma cell lines M2LnUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLOSHZbPzKq MnK3TWM2OD1zLUNOwG0> NFK3RoUzOjB4NUC4NC=>
U87 NVnVSZB6SXCxcITvd4l{KEG|c3H5 NGHmR|gz|ryP NHr1NFE4Omh? M1W1fIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiYX7kJINt\WG4ZXSgVGFTWCCjbnSgZ4F{eGG|ZT2z NX7HXXNmOjJyNkWwPFA>

... 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 <1 mg/mL
In vivo 0.5% CMC Na 6 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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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