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 M4nuOmN6fG:2b4jpZ{BCe3OjeR?= NHvoNYk4OiCq NFqySIhFVVOR MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKEV3NEXLJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMECxOVgh|ryP MYmyOFkxODJ4Nh?=
DU145 NVH5W2diS3m2b4TvfIlkKEG|c3H5 NFz6flE4OiCq Mny3SG1UVw>? NVTQPJNXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN MYGyOFkxODJ4Nh?=
A2780 NYKxU3FKS3m2b4TvfIlkKEG|c3H5 MlXnO|IhcA>? MXfEUXNQ MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N|Uh|ryP NV3lPGpUOjR7MECyOlY>
U87MG Ml35R5l1d3SxeHnjJGF{e2G7 M3zSdVczKGh? NWD1bIVTTE2VTx?= MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh|ryP NVXKTWpEOjR7MECyOlY>
A2780 MYPGeY5kfGmxbjDBd5NigQ>? NEi5W3kyKGh? M2LMdWROW09? M1e2UGlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6wOVUh|ryP MUmyOFkxODJ4Nh?=
DU145 NHnoepVHfW6ldHnvckBCe3OjeR?= NGf5fW0yKGh? M1HoZ2ROW09? MmfwTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? Mo\ZNlQ6ODB{Nk[=
A2780 MUDGeY5kfGmxbjDBd5NigQ>? MlvqNUBp MoHhSG1UVw>? M1vqNWlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP NV7LUZhYOjR7MECyOlY>
MCF7 MmPvSpVv[3Srb36gRZN{[Xl? NXLoWJlxOSCq NF22U4JFVVOR NWDNepFPUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh|ryP Ml;2NlQ6ODB{Nk[=
U87MG M1nOZ2Z2dmO2aX;uJGF{e2G7 NHzJPIcyKGh? NISwWJhFVVOR M13tWWlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1? MUCyOFkxODJ4Nh?=
A2780 M{e1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLzO|IhcA>? M3HUUmROW09? NEPONI9GSzVyPUCuOVIh|ryP MXGyOFkxODJ4Nh?=
SKMES-1 M4PQfGN6fG:2b4jpZ{BCe3OjeR?= MlP5NUDPxE1? MoTnO|IhcA>? NHPWTlFKdmS3Y3XzJINmdGxiZHXheIg> NFW3Z48zPjBzM{OxPC=>
H596 NV\YSlYxTnWwY4Tpc44hSXO|YYm= NXzXbohJOSEQvF2= NFzsUo5KdXCjaYLzJINmdGxibXnndoF1cW:w NF3wWlEzPjBzM{OxPC=>
HCC2450 M17jPGZ2dmO2aX;uJGF{e2G7 MX6xJO69VQ>? MWLJcZBicXK|IHPlcIwhcW64YYPpc44> NX;WeGNSOjZyMUOzNVg>
A549 NEP0Ro5HfW6ldHnvckBCe3OjeR?= NUHpc2JlPTByIH7N MUW0PEBp M1u1ZmROW09? NX3JUHNGUW6qaXLpeJMhSWu2IHHjeIl3[XSrb36= MV[yOVk{PzJ7OR?=
A549 NYTIVnhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorDNUDPxE1? M325dlczKGh? NGDISGtFVVOR M1;UdGlvcGmkaYTzJINmdGxiZ4Lve5Rp NVrsWYtvOjV7M{eyPVk>
H522 NYDnOVhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULpVo5ROSEQvF2= MX[3NkBp MUXEUXNQ M2XqNmlvcGmkaYTzJINmdGxiZ4Lve5Rp MofhNlU6Ozd{OUm=
LNCaP NWTENnczTnWwY4Tpc44hSXO|YYm= NWP6cVBROSEQvF2= M2fYUXN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| MkD2NlU{PjB5OUm=
LNCaP95 NF7Db|JHfW6ldHnvckBCe3OjeR?= M1nxfVEh|ryP MXLTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? NFz4fFYzPTN4MEe5PS=>
HCT-15 NVzrTVdoSXCxdH;zbZMhSXO|YYm= NGHEUngyOCEQvF2= MnPROFghcA>? M2f1XWROW09? NUnhfY54UW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVE2KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= M3nPSlI2OTV{MkS1
HCT-116 NY\1R29JSXCxdH;zbZMhSXO|YYm= NWDoT2VoOTBizszN NXHlZVdGPDhiaB?= NXHKU|hHTE2VTx?= M{f1emlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NVvneGMyOjVzNUKyOFU>
NCI-H460 MUPBdI91d3OrczDBd5NigQ>? M{nNUlExKM7:TR?= MkmzOFghcA>? NHv4XolFVVOR M{DDZ2lv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NELvNJozPTF3MkK0OS=>
SKOV-3 MlizRZBwfG:|aYOgRZN{[Xl? NW\LeXhxOTBizszN M4\WVFQ5KGh? NUDrXVFRTE2VTx?= MlzITY5lfWOnczDhdI9xfG:|aYOgbY4hW0uRVj2zJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MmfiNlUyPTJ{NEW=
BSY-1 MoP2RZBwfG:|aYOgRZN{[Xl? NEjl[5kyOCEQvF2= M{T0UFQ5KGh? M4jiN2ROW09? MlLQTY5lfWOnczDhdI9xfG:|aYOgbY4hSlO\LUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NFXG[5MzPTF3MkK0OS=>
MKN-1 MYXBdI91d3OrczDBd5NigQ>? MkXmNVAh|ryP MUS0PEBp M{PzVmROW09? Mn75TY5lfWOnczDhdI9xfG:|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? M2\JfFI2OTV{MkS1
NCI-H522 NFO1SY5CeG:2b4Ppd{BCe3OjeR?= MXuxNEDPxE1? NF3RWog1QCCq MVrEUXNQ MXvJcoR2[2W|IHHwc5B1d3Orcx?= NVf3fGhGOjVzNUKyOFU>
OVCAR-3 NES1NHZCeG:2b4Ppd{BCe3OjeR?= MX6xNEDPxE1? MWq0PEBp MkTZSG1UVw>? M4fMVGlv\HWlZYOgZZBweHSxc3nz NITiSpMzPTF3MkK0OS=>
HBC-5 NX7X[|FSSXCxdH;zbZMhSXO|YYm= MXuxNEDPxE1? MYC0PEBp MljLSG1UVw>? MmPiTY5lfWOnczDhdI9xfG:|aYO= NGDJbJgzPTF3MkK0OS=>
RXF-631L Mne5RZBwfG:|aYOgRZN{[Xl? NUjIPIlHOTBizszN NGTLTmU1QCCq MkDqSG1UVw>? M2LkO2lv\HWlZYOgZZBweHSxc3nz NHHiRYkzPTF3MkK0OS=>
MKN-45 NV;YcJE{SXCxdH;zbZMhSXO|YYm= NW\OXnlkOTBizszN NE\qXmk1QCCq MkH1SG1UVw>? NXXSPIp3UW6mdXPld{BieG:ydH;zbZM> M1K1T|I2OTV{MkS1
BON-1 NELQPWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFqyRnI2ODBibl2= MXyxNEBl M3;vU2ROW09? NV7PblY6UW6qaXLpeJMh[2WubDDndo94fGh? MViyOVAzPjJ7Mh?=
BON-1 MnTESpVv[3Srb36gRZN{[Xl? NW\0RnBZPTByIH7N Mny5OEBp NXnLTWp2TE2VTx?= MYrJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| NIKwSHQzPTB{NkK5Ni=>
QGP-1 MkK0SpVv[3Srb36gRZN{[Xl? NITueGs2ODBibl2= M2f6XlQhcA>? NX7Lem5[TE2VTx?= NHezdJdKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez NG\URmQzPTB{NkK5Ni=>
Huh7 MmDCSpVv[3Srb36gRZN{[Xl? MUmxJO69VQ>? NUHqOVZtOSCq MUPEUXNQ MVHJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGPldlQ4PA>? NHP3XWIzPTByNESwNy=>
BNL MlPESpVv[3Srb36gRZN{[Xl? M3zoT|Eh|ryP MYGxJIg> NE[5UmZFVVOR NHLjR|hKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZ? MkGxNlUxODR2MEO=
MDA-MB-175 NHKw[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\RXWN7OSEQvF2= MV21JIQ> NVvmToQyTE2VTx?= M3;GRmlEPTB:MTFOwG0> MlrrNlQ5Pzl5OU[=
MDA-MB-134 NIrtOopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfnNUDPxE1? NVXE[VJGPSCm NYrVXIpnTE2VTx?= MUfJR|UxRDFizszN MnToNlQ5Pzl5OU[=
HCC1500 NH7BTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;6S3gyKM7:TR?= NYntVIxZPSCm NWXQSXV[TE2VTx?= M4W5V2lEPTB:MTFOwG0> NF2ybW0zPDh5OUe5Oi=>
EFM-19 NGP2N2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:xNUDPxE1? MV61JIQ> NEfzWYhFVVOR NF7GUVNKSzVyPEGg{txO MlnONlQ5Pzl5OU[=
ZR-75-30 NGjFXlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHUdYcyKM7:TR?= M3fwR|Uh\A>? NIW3TGtFVVOR MnHVTWM2ODxzIN88US=> MWmyOFg4QTd7Nh?=
MDA-MB-361 M3\tS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vLW|Eh|ryP MoHDOUBl MWrEUXNQ M4WxSGlEPTB:MTFOwG0> NYDw[FdbOjR6N{m3PVY>
T-47D NXK2cIdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\FcZN4OSEQvF2= MWq1JIQ> NX\LfZZDTE2VTx?= MVjJR|UxRDFizszN NV;vN3ZMOjR6N{m3PVY>
SK-BR-3 M2G1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r0b|Eh|ryP M4TDSVUh\A>? Mkj2SG1UVw>? NH7YOXBKSzVyPEGg{txO MXiyOFg4QTd7Nh?=
UACC-732 NYHZOHNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xib|Eh|ryP MnX4OUBl MlOwSG1UVw>? NV7sTXJIUUN3MEyxJO69VQ>? NVXiXlFJOjR6N{m3PVY>
BT-474 M1fUNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\xT|Eh|ryP M3vlT|Uh\A>? NXPtNZdxTE2VTx?= NX70foJqUUN3MEyxJO69VQ>? MkTvNlQ5Pzl5OU[=
HCC202 MmnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T2WlEh|ryP MmHkOUBl MUfEUXNQ M{L0R2lEPTB:MTFOwG0> NUPKUnZNOjR6N{m3PVY>
MCF7 NULzTmRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIG5NXcyKM7:TR?= MWq1JIQ> MoHuSG1UVw>? Mk\6TWM2ODxzIN88US=> NFLiPGwzPDh5OUe5Oi=>
MDA-MB-415 MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITU[2YyKM7:TR?= MoTqOUBl MnjZSG1UVw>? NUDWVItlUUN3MEyxJO69VQ>? MUKyOFg4QTd7Nh?=
MDA-MB-453 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCxJO69VQ>? NYO3e|IzPSCm MlviSG1UVw>? Ml7pTWM2ODxzIN88US=> NXLGWpZNOjR6N{m3PVY>
ZR-75-1 NYnuNlNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfBXGlxOSEQvF2= Ml3XOUBl NUnKbHZITE2VTx?= NXX3OotrUUN3MEyxJO69VQ>? M4PETlI1QDd7N{m2
HCC38 M1GwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxJO69VQ>? NFXLN|Y2KGR? NFHwcYFFVVOR MV;JR|UxRDFizszN MmXhNlQ5Pzl5OU[=
HCC1419 M{C2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITXVI4yKM7:TR?= M2rOcFUh\A>? MlvxSG1UVw>? NVP3R5c3UUN3MEyxJO69VQ>? NHfUXIMzPDh5OUe5Oi=>
UACC-812 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LFOlEh|ryP NWXlT5RiPSCm NVfUV5RlTE2VTx?= NFHsOVJKSzVyPEGg{txO MlzUNlQ5Pzl5OU[=
HCC1187 MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInZb5EyKM7:TR?= MoDuOUBl NFO3d45FVVOR MVPJR|UxRDFizszN MUWyOFg4QTd7Nh?=
KPL-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxJO69VQ>? NW\hZ|J3PSCm M1G2ZmROW09? MWXJR|UxRDFizszN MX:yOFg4QTd7Nh?=
SUM-225 NWDmO3FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIKweJoyKM7:TR?= NIHNblU2KGR? MXzEUXNQ NUfKbpRsUUN3MEyxJO69VQ>? NFHRTVUzPDh5OUe5Oi=>
EFM-192A M1npOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fQSFEh|ryP NGG2c242KGR? NF32dFJFVVOR NX;QPYZuUUN3MEyxJO69VQ>? MkDXNlQ5Pzl5OU[=
JIMT-1 NH3wS4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nTU|Eh|ryP Mli3OUBl NULrTXY{TE2VTx?= MlOwTWM2ODxzIN88US=> M3WxbVI1QDd7N{m2
HCC1143 NGHDOFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmzfY8yKM7:TR?= MVi1JIQ> NVH6ZndLTE2VTx?= MWrJR|UxRDFizszN NFvIUJUzPDh5OUe5Oi=>
HCC2218 NXvMfVIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWixJO69VQ>? MWC1JIQ> NICwUoNFVVOR Mn;zTWM2ODxzIN88US=> MV:yOFg4QTd7Nh?=
MDA-MB-468 NYjXcVJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof6NUDPxE1? NX[5TXk{PSCm NXzEcoJxTE2VTx?= NFLP[4lKSzVyPEGg{txO NVfZNIR4OjR6N{m3PVY>
BT-20 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[xJO69VQ>? NV;4Vo1LPSCm NYL6PJhkTE2VTx?= MmTXTWM2ODxzIN88US=> NG\J[2wzPDh5OUe5Oi=>
MDA-MB-435 NXexNY5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSxJO69VQ>? M4PSSlUh\A>? M3nVfGROW09? MWPJR|UxRDFizszN MXuyOFg4QTd7Nh?=
BT-549 NG\4V21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXSNUDPxE1? NYTpSm1ZPSCm NUK2VVFGTE2VTx?= MoPTTWM2ODxzIN88US=> MViyOFg4QTd7Nh?=
HCC1806 NVnBc3lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXyXGFKOSEQvF2= MXu1JIQ> MYrEUXNQ M3H3OGlEPTB:MTFOwG0> M37hT|I1QDd7N{m2
HCC1937 NEW0fopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL3NUDPxE1? MnO1OUBl MWXEUXNQ M2K4fWlEPTB:MTFOwG0> M1zhVVI1QDd7N{m2
Hs578T M4G1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2GzVVEh|ryP M{PSXFUh\A>? MWHEUXNQ NGPYSWFKSzVyPEGg{txO NFrl[ZUzPDh5OUe5Oi=>
LN18 MnftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXVfpZ3OjBizszN MmHIO|IhcA>? M{izOWROW09? MWjJR|UxRDVizszN M1f5UlI1PzRzMEe0
LN229 M3fnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:yNEDPxE1? NWjT[HFoPzJiaB?= Moj2SG1UVw>? NXPnemtlUUN3MEy1JO69VQ>? MknJNlQ4PDFyN{S=
LNZ308 NEG2[JhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e5UFIxKM7:TR?= NGnJb2s4OiCq M1\aRWROW09? NEPQOoZKSzVyPEWg{txO MY[yOFc1OTB5NB?=
T98G MkXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV2yNEDPxE1? MoeyO|IhcA>? NX3kfFZQTE2VTx?= MlPETWM2ODx3IN88US=> M1X6XlI1PzRzMEe0
U87 NHP6XmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\FU24zOCEQvF2= NYXLfFdzPzJiaB?= Mn7qSG1UVw>? MWjJR|UxRDVizszN MXKyOFc1OTB5NB?=
LN18 MYLGeY5kfGmxbjDBd5NigQ>? MWi1JO69VQ>? NFnne5YzPCCq NGrLNG5FVVOR M1viU2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? M4[xbVI1PzRzMEe0
LNZ308 NX24TYVDTnWwY4Tpc44hSXO|YYm= Mmr4OUDPxE1? MX[yOEBp MkfNSG1UVw>? NFnBWFJKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuW M3TWVlI1PzRzMEe0
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MG-63 M4jrb2Z2dmO2aX;uJGF{e2G7 Mk\5OVAh|ryP MlryOFghcA>? NGHZOGZKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v MYCyOFczPzZ4MB?=
SJSA-1 MXvGeY5kfGmxbjDBd5NigQ>? NUi0cIc2PTBizszN NXPoVVlkPDhiaB?= MnTyTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> NEnRTHkzPDd{N{[2NC=>
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HCT116 M3vMOmZ2dmO2aX;uJGF{e2G7 NHvDUmw2KM7:TR?= MlX6NlQhcA>? MnPwSG1UVw>? NXzNNWZRWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MUOyOFY{OTF2Nx?=
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GBM NXPB[lhpSXCxcITvd4l{KEG|c3H5 NHiyOYoz|ryP MUe0PIg> M1SydWROW09? MVfpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5 MmHKNlQ2ODB2OUK=
BON NESxZmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnO0NU02|ryP MW[3Nog> NUflSJVi\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? M4D2eVI1PDR|NUKz
BON MYfBdI9xfG:|aYOgRZN{[Xl? M4f1[|EuPc7:TR?= NGm0SVkzPGh? Ml:wbY5kemWjc3XzJIFxd3C2b4Ppdy=> MV6yOFQ1OzV{Mx?=
H1975 M4fWZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrweGQxNjNvOT62{txO MYS3Nog> M1LLU2ROW09? NHPuN25KSzVyPUGuN|g2|ryP NVztWlh5OjR|M{e4OFY>
H1975 MVHBdI9xfG:|aYOgRZN{[Xl? M3S4U|LPxE1? NVXOcmpJOjSq NVvpNmJMTE2VTx?= NFXtd2pqdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>? NEjSRogzPDN|N{i0Oi=>
T-ALL M1rwNGFxd3C2b4Ppd{BCe3OjeR?= M2Hq[4JmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= NULCfoszOjRib4KgOFhp MoT2SG1UVw>? NXi1dWxm[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM> NIjl[VUzPDNzMEezOi=>
BCR-ABL NE\CS2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnrXmIxNjJ3LUGw{txO NH\jSIU1\A>? M1naRZNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? NIPaV5gzPDJ2NE[xNi=>
LC-1/SQSF NHnFN3VHfW6ldHnvckBCe3OjeR?= M1vzOVPPxE1? MWiyOIg> MUHEUXNQ MV3k[YNz\WG|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy= NVfy[2ZROjN7OECwPVM>
Primary CLL cells NX35WnZCSXCxcITvd4l{KEG|c3H5 MWqxMVEx|ryP NH7pOpo1QGh? NG\DZpdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ MXWyN|g2ODhyNx?=
Primary CLL cells MofkT4lv[XOnIFHzd4F6 NHzGXHMz|ryP NFyxd3Y{OG2rbh?= Mkm5[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? M17lXFI{QDVyOEC3
Primary CLL cells Ml7GR5l1d3SxeHnjJGF{e2G7 NHfpe5Uz|ryP NGHUNmozPGh? MUPpcoR2[2W|IHPlcIwh[3m2b4TvfIlkcXS7 NGrtSlUzOzh3MEiwOy=>
human NSCLC cell lines NEXqXnZCeG:ydH;zbZMhSXO|YYm= M{LNclAvOTJ3LUVOwG0> M1jscVI1cA>? NIn4N4ZFVVOR MoOxTWM2OHNicnHu[4V{KG[{b32gNE41NTMQvF2= NXX6XmUxOjN3NkK0O|I>
human HCC cell lines MnTiR4VtdCC4aXHibYxqfHliYYPzZZk> NGfUVJAxNjByNT2x{txO NV\mdnZQPDiq Ml7TTWM2OD1zzszN MYKyN|Q5QTl7OR?=
Huh7 MVzLbY5ie2ViQYPzZZk> NELOWWYy|ryP MmTDOFhp NHz1OI9{cWewaf-shYNidnSueTDy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NVH3N3p3OjN2OEm5PVk>
SK-HEP1 Ml3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\PdFEuOjEQvF2= NYj4bo1[PzKq M3q5UmROW09? NYq1ZlhyUUN3MP-8oFHPxE1? NWq0RWk3OjN2N{mxN|Y>
786-0 NV;wXVNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:5TGIyNTJyzszN NIPUPJA4Omh? MVLEUXNQ MnvjTWM2OO,:nEJOwG0> M{fqflI{PDd7MUO2
JVM2 MYnDfZRwfG:6aXPpeJkh[XO|YYm= M4XZclAvOi1{MN88US=> NYPoPW9vPzKq MXjEUXNQ NF7SN|NKSzVyPUCuPe69VQ>? NUf3VWRLOjN{M{i2N|k>
EHEB MnPRR5l1d3SxeHnjbZR6KGG|c3H5 NXfWcY9FOC5{LUKw{txO NIr4WHI4Omh? NXrEUVB{TE2VTx?= M4r2WmlEPTB;MD63{txO NUPwRmJPOjN{M{i2N|k>
MEC2 MVHDfZRwfG:6aXPpeJkh[XO|YYm= M1HBW|AvOi1{MN88US=> NEfYepE4Omh? MknXSG1UVw>? Mlv0TWM2OD1yLkhOwG0> MYGyN|I{QDZ|OR?=
primary B-CLL lymphocytes NF3iS25CeG:ydH;zbZMhSXO|YYm= MlrOTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? M2\IfVI1cA>? MW\EUXNQ NXmz[IdIUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>? M2rRbVI{OjN6NkO5
primary B-CLL lymphocytes M2XrWWtqdmG|ZTDBd5NigQ>? M2H1NGlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? NXLWc5M3OjSq NWC2XZJRcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> M{PjdFI{OjN6NkO5
human NSCLC M2fhZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXCPJgxNjVvMt88US=> NV;IRoU5PzKq MWDJR|UxRTIQvF2= NIL4TZIzOjd6MUO5Ny=>
human NSCLC M3\MPWtqdmG|ZTDBd5NigQ>? MmH1Ne69VQ>? NWWxTZJ4OjSq M4XXWYlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= MoP0NlI4QDF|OUO=
Y1 cell line MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3kNE4y|ryPL{JOwG0> MUWyOIg> M{fpRWROW09? NF\XdJhqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?= MkT2NlI3QTJ7MES=
PIK3CA-mutant MCF7 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTkWWRIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= NYDDd5pVPzKq NH3XOlZIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= M4O2TFIzPjV|OU[3
PIK3CA-mutant MCF7 M2f2OmtqdmG|ZTDBd5NigQ>? MV\JR|UxRTFzNNMxN45O NHHZfpc4Omh? M2nueWlEPTB;MUG0xtE{dk1iaX6gdoVlfWOrbnegRYt1KHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= MYOyNlY2Ozl4Nx?=
MCF7-myr-Akt MoLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUmyXlZZT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= MmLjO|Jp MVTHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? MknqNlI3PTN7Nke=
colon cancer cell lines MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzZfVQxNTFyzszN NF7TWm04Omh? Mmf3SG1UVw>? M4fIVGlEPTB;Md88US=> NFr0XFAzOjV2M{i1Oy=>
gastric cancer cell lines NYjuXpB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnpZo0xNTFyzszN NYXXU41SPzKq NWGyXHNSTE2VTx?= NGC4XplKSzVyPUKtOe69VQ>? MX6yNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45 MkW4RZBweHSxc3nzJGF{e2G7 MnnpNu69VQ>? M1\zRVQ5cA>? NFHaT2V{cGmodDDpckBIOiCyaHHz[S=> MnXQNlI2PDN6NUe=
HT-29 and HCT-116 MlfXR4F{eGG|ZTDhd5NigQ>? M4DLcVXPxE1? NUPCV3M3OjSq MWLpcoR2[2W|IHPhd5Bie2ViYXP0bZZqfHl? M4HVN|IzPTR|OEW3
MM cell lines NHz6SGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHz2[5oyOM7:TR?= MWeyOIg> MUfEUXNQ M2D5OmlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? MX2yNlIxPzR6NR?=
ARP-1 Mn7qRZBweHSxc3nzJGF{e2G7 NEXjW48yOM7:TR?= Mn3LNlRp M{DweWROW09? MXzpcoR2[2W|IF3NJINmdGxiYYDvdJRwe2m|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w MoDxNlIzODd2OEW=
SNU-601 NGTlN|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\oT|czcA>? NILBfW1FVVOR M13uNWlEPTB;MD64NVbDuTBwME[z{txO NUWzUJBLOjJzNUm4NVQ>
SNU-1 NX75NINjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2n2bFczcA>? M1XBcmROW09? NGfreXBKSzVyPUGuNFgzyrFyLkCyPO69VQ>? MYGyNlE2QThzNB?=
SNU-668 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nyZ|czcA>? M2T4RmROW09? NHWzU5ZKSzVyPUGuOVc6yrFyLkC3OO69VQ>? NWLscZZPOjJzNUm4NVQ>
AGS MnnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1mwWlczcA>? NEj2V2FFVVOR MmLoTWM2OD1zLkexOOKyOC5zMUhOwG0> NG\Uc4QzOjF3OUixOC=>
SNU-216 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33pUFczcA>? NGO0[llFVVOR NVq2PI45UUN3ME2yMlY6OsLzMD6wPFLPxE1? MVuyNlE2QThzNB?=
SNU-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrNO|Jp NEf3[nBFVVOR MlnVTWM2OD1zLkO1NeKyOC5yOUJOwG0> MXyyNlE2QThzNB?=
SNU-638 M3f5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fpZVczcA>? M4DrU2ROW09? NIDnd5pKSzVyPUKuNlgzyrFyLkC1N:69VQ>? NV7iPIVKOjJzNUm4NVQ>
SNU-16 NVfXdpZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfmVpE4Omh? M1HjSGROW09? MYHJR|UxRTFwNUezxtExNjByMd88US=> MoflNlIyPTl6MUS=
SNU-484 NFXGWI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rtbFczcA>? MkXvSG1UVw>? NVTLTnE1UUN3ME2xMlczQMLzMD6wOFXPxE1? MlLhNlIyPTl6MUS=
SNU-620 MlLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLVXVQ4Omh? MWrEUXNQ NELqfYFKSzVyPUKuPVM6yrFyLkCwNe69VQ>? Mnr6NlIyPTl6MUS=
SNU-719 Mm\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jKTFczcA>? M1fMbmROW09? NUOzb|dNUUN3ME2zMlA{P8LzMD6wN|LPxE1? MlfNNlIyPTl6MUS=
glioma cell lines M172eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUG0OZpTPzKq NGrKTWhKSzVyPUGtNu69VQ>? NIHQbpIzOjB4NUC4NC=>
U87 MmLrRZBweHSxc3nzJGF{e2G7 Ml;RNu69VQ>? MWO3Nog> M13L[4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiYX7kJINt\WG4ZXSgVGFTWCCjbnSgZ4F{eGG|ZT2z MV2yNlA3PTB6MB?=

... 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 slightly soluble or insoluble
In vivo Add solvents individually and in order:
0.5% CMC Na
6 mg/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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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