Buparlisib (BKM120)

For research use only. Not for use in humans.

Catalog No.S2247 Synonyms: NVP-BKM120

137 publications

Buparlisib (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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 272 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Buparlisib (BKM120) has been cited by 137 publications

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 M2D0OmN6fG:2b4jpZ{BCe3OjeR?= M4PxTVczKGh? MVnEUXNQ NXL5b2ZqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=> M4rkVFI1QTByMk[2
DU145 MUTDfZRwfG:6aXOgRZN{[Xl? MoPYO|IhcA>? NILFfI5FVVOR NHjRNphEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2= MXOyOFkxODJ4Nh?=
A2780 NXHv[FFjS3m2b4TvfIlkKEG|c3H5 NYThRYdEPzJiaB?= M2jVR2ROW09? NYfEc4dFS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjN3IN88US=> M{e1d|I1QTByMk[2
U87MG NUjsO|FFS3m2b4TvfIlkKEG|c3H5 M37WWlczKGh? MnfCSG1UVw>? NVS5cVRlS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjl6IN88US=> NH7s[pEzPDlyMEK2Oi=>
A2780 M{XteGZ2dmO2aX;uJGF{e2G7 MXuxJIg> NGfmTItFVVOR MXvJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>? NYXkdpltOjR7MECyOlY>
DU145 Mm\uSpVv[3Srb36gRZN{[Xl? M1zxW|EhcA>? NXvEXm5RTE2VTx?= M4O4cGlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBFXTF2NTDj[YxteyCqYYLic5JqdmdiTFvCNUBufXSjdHnvckB4cXSqIFXDOVAhd2ZiMD6wO|Mh|ryP MU[yOFkxODJ4Nh?=
A2780 NWfib4tPTnWwY4Tpc44hSXO|YYm= MVWxJIg> M{jyPWROW09? NIDMeGxKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDFR|UxKG:oIECuNFc1KM7:TR?= MnzUNlQ6ODB{Nk[=
MCF7 NFLlflZHfW6ldHnvckBCe3OjeR?= MUexJIg> Ml3jSG1UVw>? M2jOWWlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFW1OFVMKG23dHHueE1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6xJO69VQ>? MlTqNlQ6ODB{Nk[=
U87MG MVjGeY5kfGmxbjDBd5NigQ>? MVmxJIg> NW\WPYR6TE2VTx?= M3;Uc2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1? Mnm0NlQ6ODB{Nk[=
A2780 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDE[ZlHPzJiaB?= MkTqSG1UVw>? NYXZc3hVTUN3ME2wMlUzKM7:TR?= M2Hld|I1QTByMk[2
SKMES-1 M1THWGN6fG:2b4jpZ{BCe3OjeR?= NUfWRXl[OSEQvF2= NVv2WpJ6PzJiaB?= M3:yXmlv\HWlZYOgZ4VtdCCmZXH0bC=> M37KWFI3ODF|M{G4
H596 M4DxVGZ2dmO2aX;uJGF{e2G7 Mmq1NUDPxE1? MnzBTY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>? NFfV[4ozPjBzM{OxPC=>
HCC2450 NGe1NXdHfW6ldHnvckBCe3OjeR?= NUHiVnJjOSEQvF2= MofvTY1x[Wm{czDj[YxtKGmwdnHzbY9v NHjLXGszPjBzM{OxPC=>
A549 MX7GeY5kfGmxbjDBd5NigQ>? MVK1NFAhdk1? M17IXVQ5KGh? MlvBSG1UVw>? M3n5S2lvcGmkaYTzJGFsfCCjY4TpeoF1cW:w MV:yOVk{PzJ7OR?=
A549 NHrQSHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:xJO69VQ>? MkCwO|IhcA>? Mo\FSG1UVw>? NF;4SGdKdmirYnn0d{Bk\WyuIHfyc5d1cA>? MWmyOVk{PzJ7OR?=
H522 NH7veHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHvNUDPxE1? NEOydmY4OiCq MWLEUXNQ NYWwUFY6UW6qaXLpeJMh[2WubDDndo94fGh? NEHqdmszPTl|N{K5PS=>
LNCaP MXnGeY5kfGmxbjDBd5NigQ>? NEnCboQyKM7:TR?= M2npUnN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| Mlz1NlU{PjB5OUm=
LNCaP95 NInaWVVHfW6ldHnvckBCe3OjeR?= M2GwWFEh|ryP M1e5NHN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| MmL4NlU{PjB5OUm=
HCT-15 Mk\ZRZBwfG:|aYOgRZN{[Xl? NIHjSmgyOCEQvF2= NFLoboo1QCCq MWfEUXNQ NVLVcFQxUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVE2KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NYjDV5JwOjVzNUKyOFU>
HCT-116 NYDlS2NESXCxdH;zbZMhSXO|YYm= MofZNVAh|ryP MXW0PEBp MXnEUXNQ M{T4Zmlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NHHQN3kzPTF3MkK0OS=>
NCI-H460 NXP5PJkzSXCxdH;zbZMhSXO|YYm= Mn60NVAh|ryP Mmi3OFghcA>? NVHwXoRxTE2VTx?= MUfJcoR2[2W|IHHwc5B1d3OrczDpckBPS0lvSES2NEBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w M3XGUlI2OTV{MkS1
SKOV-3 NGTVSmhCeG:2b4Ppd{BCe3OjeR?= MX:xNEDPxE1? NGXIUIM1QCCq NUf6O5dsTE2VTx?= NIP4cpdKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCVS1;WMVMh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= MkjmNlUyPTJ{NEW=
BSY-1 NV3kWXpjSXCxdH;zbZMhSXO|YYm= NEfnS5UyOCEQvF2= MVe0PEBp M1PyOGROW09? M3izb2lv\HWlZYOgZZBweHSxc3nzJIlvKEKVWT2xJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? NVvwRldMOjVzNUKyOFU>
MKN-1 Ml7SRZBwfG:|aYOgRZN{[Xl? MlS3NVAh|ryP MVO0PEBp MkTMSG1UVw>? MUPJcoR2[2W|IHHwc5B1d3OrczDpckBOU05vMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NVLIeVFROjVzNUKyOFU>
NCI-H522 MoKzRZBwfG:|aYOgRZN{[Xl? NIjQfGMyOCEQvF2= Mn7YOFghcA>? M2nIVGROW09? MX3JcoR2[2W|IHHwc5B1d3Orcx?= NUO4bFM6OjVzNUKyOFU>
OVCAR-3 MX\BdI91d3OrczDBd5NigQ>? M4HqZlExKM7:TR?= MVi0PEBp NFv2SppFVVOR NIrjN2VKdmS3Y3XzJIFxd3C2b4Ppdy=> M{Xw[|I2OTV{MkS1
HBC-5 NXLnNnhWSXCxdH;zbZMhSXO|YYm= MkjFNVAh|ryP NGPmZ2I1QCCq MVrEUXNQ NILHd3JKdmS3Y3XzJIFxd3C2b4Ppdy=> MV2yOVE2OjJ2NR?=
RXF-631L NFj1TWRCeG:2b4Ppd{BCe3OjeR?= MV:xNEDPxE1? NGPhXnQ1QCCq MoX4SG1UVw>? NE\TdGtKdmS3Y3XzJIFxd3C2b4Ppdy=> NWXtWZJIOjVzNUKyOFU>
MKN-45 NWi5bnRQSXCxdH;zbZMhSXO|YYm= M2jMZlExKM7:TR?= M4PlVVQ5KGh? M3LmUWROW09? MmTSTY5lfWOnczDhdI9xfG:|aYO= M3y3UVI2OTV{MkS1
BON-1 NIjNc5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;RflFpPTByIH7N MVKxNEBl MVnEUXNQ M4TkSmlvcGmkaYTzJINmdGxiZ4Lve5Rp MknBNlUxOjZ{OUK=
BON-1 MnPRSpVv[3Srb36gRZN{[Xl? M4fvfVUxOCCwTR?= NW[5N|hmPCCq MknGSG1UVw>? NInWWpBKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez MUeyOVAzPjJ7Mh?=
QGP-1 M{HndmZ2dmO2aX;uJGF{e2G7 NIjTPFA2ODBibl2= M3G1T|QhcA>? NWDTfXJCTE2VTx?= NGXyV|hKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez Ml7yNlUxOjZ{OUK=
Huh7 Ml7SSpVv[3Srb36gRZN{[Xl? M3zZN|Eh|ryP MkPrNUBp NWjzO2dKTE2VTx?= NVLzVYlsUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S= M{X0dlI2ODB2NECz
BNL MnjTSpVv[3Srb36gRZN{[Xl? MX[xJO69VQ>? NXfuUFh3OSCq MlfESG1UVw>? NVvyTVVSUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4 M333TlI2ODB2NECz
MDA-MB-175 NUfIVoVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuxJO69VQ>? NV7I[mJXPSCm MmO1SG1UVw>? NX\2OpRvUUN3MEyxJO69VQ>? MVqyOFg4QTd7Nh?=
MDA-MB-134 M2nFcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrK[4JpOSEQvF2= Mn3JOUBl MXXEUXNQ Ml36TWM2ODxzIN88US=> M1T1SFI1QDd7N{m2
HCC1500 NFLyOYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nXPVEh|ryP NYS5WI5GPSCm MXLEUXNQ MlfQTWM2ODxzIN88US=> NFLWS2ozPDh5OUe5Oi=>
EFM-19 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;JPHdiOSEQvF2= M3\2XlUh\A>? NW[2NHdrTE2VTx?= M{jvTWlEPTB:MTFOwG0> NHfrepgzPDh5OUe5Oi=>
ZR-75-30 NGjqWW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHKe|AyKM7:TR?= MWW1JIQ> NYTDPXdPTE2VTx?= MkXzTWM2ODxzIN88US=> Mk\kNlQ5Pzl5OU[=
MDA-MB-361 NUfqfWtUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O4V|Eh|ryP MY[1JIQ> M1nuT2ROW09? Mof5TWM2ODxzIN88US=> Mnq3NlQ5Pzl5OU[=
T-47D MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nlZ|Eh|ryP Mon5OUBl MWHEUXNQ MnzHTWM2ODxzIN88US=> MoW2NlQ5Pzl5OU[=
SK-BR-3 MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL1NUDPxE1? M2e0RlUh\A>? NGDQSnBFVVOR NInwVmpKSzVyPEGg{txO MoPwNlQ5Pzl5OU[=
UACC-732 Ml70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUexJO69VQ>? MlPmOUBl NXLjcll5TE2VTx?= MV7JR|UxRDFizszN M3zPWVI1QDd7N{m2
BT-474 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLmZ2o6OSEQvF2= MWe1JIQ> MWrEUXNQ MV;JR|UxRDFizszN MmTSNlQ5Pzl5OU[=
HCC202 NUHxVXVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKzNUDPxE1? NFPoOZQ2KGR? M2DoTGROW09? Mk\0TWM2ODxzIN88US=> NHfzVY4zPDh5OUe5Oi=>
MCF7 NF:zSYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfvbo5oOSEQvF2= M4j4RVUh\A>? MYjEUXNQ M4XlfmlEPTB:MTFOwG0> NHniPVQzPDh5OUe5Oi=>
MDA-MB-415 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXtRol{OSEQvF2= NEfVRVQ2KGR? MkXSSG1UVw>? NV23WmFrUUN3MEyxJO69VQ>? M325ZlI1QDd7N{m2
MDA-MB-453 NVXpTW83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfPNUDPxE1? NVO5V5BLPSCm MkHvSG1UVw>? NYf1VHlqUUN3MEyxJO69VQ>? MoHHNlQ5Pzl5OU[=
ZR-75-1 NW\JbYl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nwe|Eh|ryP Mn20OUBl MlTiSG1UVw>? NH;TZmhKSzVyPEGg{txO MkTpNlQ5Pzl5OU[=
HCC38 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLMNUDPxE1? NV;iW4lbPSCm M33aSWROW09? NWrJboxmUUN3MEyxJO69VQ>? MUWyOFg4QTd7Nh?=
HCC1419 NF3RflhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXEZYE{OSEQvF2= M4KzRVUh\A>? MWXEUXNQ Mn;zTWM2ODxzIN88US=> NV;FVItmOjR6N{m3PVY>
UACC-812 NHHVS|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\iRlEh|ryP M2DDelUh\A>? MoDLSG1UVw>? MlXmTWM2ODxzIN88US=> Mnf4NlQ5Pzl5OU[=
HCC1187 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TNbFEh|ryP MX:1JIQ> MXrEUXNQ NFy3WWxKSzVyPEGg{txO MVeyOFg4QTd7Nh?=
KPL-1 MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqxJO69VQ>? MUK1JIQ> M17UV2ROW09? NYLz[246UUN3MEyxJO69VQ>? M1i0U|I1QDd7N{m2
SUM-225 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDOcoZzOSEQvF2= M13DXVUh\A>? NHXjNIxFVVOR MXzJR|UxRDFizszN M3u1O|I1QDd7N{m2
EFM-192A MmfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTwNUDPxE1? Ml7OOUBl NIH4eIJFVVOR M3LwWWlEPTB:MTFOwG0> M{T1cFI1QDd7N{m2
JIMT-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\O[FEh|ryP NWXIUoZQPSCm NXnVOIgyTE2VTx?= M3jIcmlEPTB:MTFOwG0> MV:yOFg4QTd7Nh?=
HCC1143 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHiNUDPxE1? MkjtOUBl MUPEUXNQ M3e3NmlEPTB:MTFOwG0> NIXUPVczPDh5OUe5Oi=>
HCC2218 NXzRZ2R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4WwcVEh|ryP M2HDeFUh\A>? NVHyOHl5TE2VTx?= NHXBVYJKSzVyPEGg{txO MVSyOFg4QTd7Nh?=
MDA-MB-468 NFj5Tm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuxJO69VQ>? NFfHRnY2KGR? M4XCUWROW09? NW\scG5NUUN3MEyxJO69VQ>? M4XYPVI1QDd7N{m2
BT-20 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnj0NUDPxE1? NGPRRZY2KGR? M2G3WmROW09? M4jP[mlEPTB:MTFOwG0> MVKyOFg4QTd7Nh?=
MDA-MB-435 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnOc4UyKM7:TR?= M{Xoc|Uh\A>? NVG3eJNOTE2VTx?= NILIe21KSzVyPEGg{txO MonjNlQ5Pzl5OU[=
BT-549 NGjzW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVGxJO69VQ>? M1HqXlUh\A>? NXLoXnM3TE2VTx?= NFKzUWVKSzVyPEGg{txO NVLDOm1rOjR6N{m3PVY>
HCC1806 M2DLNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXz6WG1QOSEQvF2= NH3ndHg2KGR? NULvc2JZTE2VTx?= MV7JR|UxRDFizszN NFOwRpEzPDh5OUe5Oi=>
HCC1937 NFTRbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXixJO69VQ>? NV3nSHNVPSCm Mn7iSG1UVw>? NWXoSYZHUUN3MEyxJO69VQ>? NXL4Vo1ZOjR6N{m3PVY>
Hs578T M2DlV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLYNUDPxE1? M4SzeVUh\A>? NGTvTlhFVVOR M364SmlEPTB:MTFOwG0> M4P3eVI1QDd7N{m2
LN18 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP1PJpoOjBizszN Mli4O|IhcA>? NXL2TpNXTE2VTx?= NH[4ZmdKSzVyPEWg{txO NXewR3p1OjR5NEGwO|Q>
LN229 NEjadGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXYNlAh|ryP MXK3NkBp M3fGbGROW09? MnTtTWM2ODx3IN88US=> MUiyOFc1OTB5NB?=
LNZ308 NI\xdnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVqyNEDPxE1? M1zpNFczKGh? MVjEUXNQ M{fnVmlEPTB:NTFOwG0> NYHiUWdlOjR5NEGwO|Q>
T98G NED4bHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnyOG11OjBizszN NEXwd3Y4OiCq MlXFSG1UVw>? MWrJR|UxRDVizszN MmLzNlQ4PDFyN{S=
U87 M2rCVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvWNVl3OjBizszN NHfzdlM4OiCq M4PEPWROW09? NYK4XZN2UUN3MEy1JO69VQ>? MoOxNlQ4PDFyN{S=
LN18 NEnPbIJHfW6ldHnvckBCe3OjeR?= MUi1JO69VQ>? MnTXNlQhcA>? M1TGUGROW09? MYnJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV NVLycIZkOjR5NEGwO|Q>
LNZ308 NYDaW3lxTnWwY4Tpc44hSXO|YYm= NUjq[Y9WPSEQvF2= M1m5WlI1KGh? NWnwT4hzTE2VTx?= M1;N[WlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? MVGyOFc1OTB5NB?=
Saos-2 MY\GeY5kfGmxbjDBd5NigQ>? MW[1NEDPxE1? MmexOFghcA>? NInJdFlKdmirYnn0d{Bk\WyuIHnueoF{cW:w MW[yOFczPzZ4MB?=
MG-63 M1LjW2Z2dmO2aX;uJGF{e2G7 NEK3SWk2OCEQvF2= Mlr2OFghcA>? NHvLWpVKdmirYnn0d{Bk\WyuIHnueoF{cW:w NYnSTZYzOjR5Mke2OlA>
SJSA-1 Mny2SpVv[3Srb36gRZN{[Xl? NVLyT5BPPTBizszN MWC0PEBp MYfJcohq[mm2czDj[YxtKGmwdnHzbY9v M1LBU|I1PzJ5Nk[w
Saos-2 MnX3SpVv[3Srb36gRZN{[Xl? M3XBN|UxKM7:TR?= MW[0PEBp M{ThNGlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MoHVNlQ4Ojd4NkC=
MG-63 MVHGeY5kfGmxbjDBd5NigQ>? M3HxWVUxKM7:TR?= M175NFQ5KGh? MXXJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NWjy[W9jOjR5Mke2OlA>
SJSA-1 M33RbWZ2dmO2aX;uJGF{e2G7 NYXNXndRPTBizszN NI\6Wok1QCCq MlvKTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> M4\IRlI1PzJ5Nk[w
Saos-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;JfnA2PTBizszN M{ftUlQ5KGh? M3LofWlvcGmkaYTzJINmdGxidnnhZoltcXS7 MUmyOFczPzZ4MB?=
MG-63 MmTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjNTGU2OCEQvF2= MVq0PEBp NUPzVJlZUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= NHXZSHIzPDd{N{[2NC=>
SJSA-1 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT2cVg2OCEQvF2= NWTOSYMxPDhiaB?= NYnkXHZUUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= Mn;oNlQ4Ojd4NkC=
FaDu M3vkTWZ2dmO2aX;uJGF{e2G7 NVztfoRUPSEQvF2= M1jTZ|I1KGh? NIW2dotFVVOR NVvFOXJVWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> M1zoZ|I1PjNzMUS3
EMT6 NGTPU5RHfW6ldHnvckBCe3OjeR?= NFr6Z4U2KM7:TR?= NGnzUFYzPCCq MWPEUXNQ Mn\6VoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= NYP4fWdiOjR4M{GxOFc>
HCT116 NUfmbm1kTnWwY4Tpc44hSXO|YYm= Moq1OUDPxE1? NWLDZoh5OjRiaB?= MkG1SG1UVw>? NVjNOlRsWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NFmxZnMzPDZ|MUG0Oy=>
U87 NFjyS2FHfW6ldHnvckBCe3OjeR?= MlexOUDPxE1? NYW4bHlzOjRiaB?= Ml3GSG1UVw>? M1XwcXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u MYGyOFY{OTF2Nx?=
GBM MnjrRZBweHSxc3nzJGF{e2G7 NInyT28z|ryP NXjsU2dHPDiq NEKxUFJFVVOR NFrHboVqdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6 M3LJ[FI1PTByNEmy
BON MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUixMVXPxE1? NWnZRY1uPzKq NYDu[pFo\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NGjKco4zPDR2M{WyNy=>
BON MXXBdI9xfG:|aYOgRZN{[Xl? M2nWdlEuPc7:TR?= Mmi0NlRp NIO3TXFqdmO{ZXHz[ZMh[XCxcITvd4l{ NWPkUFZnOjR2NEO1NlM>
H1975 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zPUlAvOy17LkdOwG0> MUe3Nog> MVHEUXNQ MVjJR|UxRTFwM{i1{txO NXTDZ|VJOjR|M{e4OFY>
H1975 MWHBdI9xfG:|aYOgRZN{[Xl? NFvZOIYz|ryP NYjEcml2OjSq NEKxdXZFVVOR NWjMVHBicW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl? MWeyOFM{Pzh2Nh?=
T-ALL NV3XZXNnSXCxcITvd4l{KEG|c3H5 M3:z[oJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= NFLUbo8zPCCxcjC0PIg> MkfDSG1UVw>? NYexZW1i[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM> M4XjRVI1OzFyN{O2
BCR-ABL M3P2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvxNE4zPS1zMN88US=> NUG0PZlSPGR? M3f1e5Nq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? MlPFNlQzPDR4MUK=
LC-1/SQSF M2\tV2Z2dmO2aX;uJGF{e2G7 MmnWN:69VQ>? MorpNlRp M3PzdWROW09? M3TjUIRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> MVqyN|k5ODB7Mx?=
Primary CLL cells MXnBdI9xfG:|aYOgRZN{[Xl? NXPPXXZOOS1zMN88US=> NV\kRWlCPDiq MVTpcoR2[2W|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz MVSyN|g2ODhyNx?=
Primary CLL cells NH;jTXNMcW6jc3WgRZN{[Xl? NFjqe44z|ryP MU[zNI1qdg>? Mlvm[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? MlXJNlM5PTB6MEe=
Primary CLL cells MX7DfZRwfG:6aXOgRZN{[Xl? NVH5bnA1Os7:TR?= MoCzNlRp M3H0WIlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= M2S4ZVI{QDVyOEC3
human NSCLC cell lines NW\Ke5p{SXCxcITvd4l{KEG|c3H5 NYTjcYtQOC5zMkWtOO69VQ>? Ml7hNlRp MmfwSG1UVw>? M1qxRmlEPTC|IILhcodmeyCocn;tJFAvPC1{zszN NYrZWZRKOjN3NkK0O|I>
human HCC cell lines NUDZZoFJS2WubDD2bYFjcWyrdImgZZN{[Xl? MXGwMlAxPS1zzszN MXi0PIg> M4PSdWlEPTB;Md88US=> M37yV|I{PDh7OUm5
Huh7 MUnLbY5ie2ViQYPzZZk> M1mweVHPxE1? M{HEOlQ5cA>? M2ewZpNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NXfyR|hYOjN2OEm5PVk>
SK-HEP1 NITqXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTaXlIyNTJyzszN MXe3Nog> NGfNV|RFVVOR NH;TOYFKSzVy78{cNe69VQ>? NFrJOIozOzR5OUGzOi=>
786-0 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3RNU0zOM7:TR?= MU[3Nog> MUPEUXNQ MlfhTWM2OO,:nEJOwG0> Mo\GNlM1PzlzM{[=
JVM2 NU[wO5FmS3m2b4TvfIlkcXS7IHHzd4F6 MlXmNE4zNTJyzszN MVe3Nog> MlnQSG1UVw>? NITWW|VKSzVyPUCuPe69VQ>? NUDvOIJLOjN{M{i2N|k>
EHEB MX\DfZRwfG:6aXPpeJkh[XO|YYm= NH\0d3IxNjJvMkFOwG0> MW[3Nog> MlTuSG1UVw>? M2LRdGlEPTB;MD63{txO NWnPU|BIOjN{M{i2N|k>
MEC2 MUXDfZRwfG:6aXPpeJkh[XO|YYm= NXnLcpc4OC5{LUKw{txO NHjBUVE4Omh? NVe1fnZWTE2VTx?= MYTJR|UxRTBwN988US=> MYeyN|I{QDZ|OR?=
primary B-CLL lymphocytes MXXBdI9xfG:|aYOgRZN{[Xl? NYDHRZc5UUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= M1L5TFI1cA>? MkDvSG1UVw>? MlT0TWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> M{fkRVI{OjN6NkO5
primary B-CLL lymphocytes MXTLbY5ie2ViQYPzZZk> NWT5VWQ4UUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= NIfSO4QzPGh? M1jsfolvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u M3LDSFI{OjN6NkO5
human NSCLC MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnRRWVyOC53LUNOwG0> NHuyOXI4Omh? NXzpOWNkUUN3ME2x{txO MYCyNlc5OTN7Mx?=
human NSCLC M2TycmtqdmG|ZTDBd5NigQ>? M3nXVVHPxE1? M2LweVI1cA>? M{fmcIlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= NVvMflJiOjJ5OEGzPVM>
Y1 cell line M1TIUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvGNE4y|ryPL{JOwG0> Mn6wNlRp NUPBeWxOTE2VTx?= MWDpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>? NWDr[JNZOjJ4OUK5NFQ>
PIK3CA-mutant MCF7 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? NUf1eXM6PzKq M2SyWmdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P NIjifo8zOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 MXjLbY5ie2ViQYPzZZk> NYjhdHhyUUN3ME2xNVTDuTOwTR?= M{nsV|czcA>? Mnq2TWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= M3j4dFIzPjV|OU[3
MCF7-myr-Akt NVz5eYZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnXdHFIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= Mo\qO|Jp NVjvboVXT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= NHey[2UzOjZ3M{m2Oy=>
colon cancer cell lines NG\jTo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDmU3IxNTFyzszN Mmj6O|Jp MmHWSG1UVw>? MY\JR|UxRTIQvF2= MVmyNlU1Ozh3Nx?=
gastric cancer cell lines MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrzU5F1OC1zMN88US=> MWO3Nog> NXzsZmJoTE2VTx?= NGriUmdKSzVyPUKtOe69VQ>? MoHPNlI2PDN6NUe=
HCT-116/HT-29/MKN-45 M1:xPGFxd3C2b4Ppd{BCe3OjeR?= MVGy{txO Ml\oOFhp NVzLPXhye2irZoSgbY4hTzJicHjhd4U> M3Ts[VIzPTR|OEW3
HT-29 and HCT-116 MmTsR4F{eGG|ZTDhd5NigQ>? MXu1{txO NYrBToMzOjSq NIT6fmVqdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm= M{njPVIzPTR|OEW3
MM cell lines M3PpSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonvNVDPxE1? MmXXNlRp MWjEUXNQ M3vmcGlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? M3O3VVIzOjB5NEi1
ARP-1 NF2yc5pCeG:ydH;zbZMhSXO|YYm= NYfhNotHOTEQvF2= NULLO3BoOjSq MX;EUXNQ M4LEbolv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= MVGyNlIxPzR6NR?=
SNU-601 M17JeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i0ZVczcA>? NYTDT2Z{TE2VTx?= NX73NZY3UUN3ME2wMlgyPsLzMD6wOlPPxE1? MkDpNlIyPTl6MUS=
SNU-1 M1HpOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIe5cJA4Omh? Ml7PSG1UVw>? M{XNOGlEPTB;MT6wPFLDuTBwMEK4{txO NV3kcnp4OjJzNUm4NVQ>
SNU-668 M3Lhe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\sd2M4Omh? NHvZ[3lFVVOR MlPMTWM2OD1zLkW3PeKyOC5yN{VOwG0> NIm5SnkzOjF3OUixOC=>
AGS NYO3c2NjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYW3Nog> MonHSG1UVw>? Moe0TWM2OD1zLkexOOKyOC5zMUhOwG0> M1zEflIzOTV7OEG0
SNU-216 NVLwVWw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjXO|Jp NYXNdoVVTE2VTx?= NHr5V2tKSzVyPUKuOlkzyrFyLkC4Nu69VQ>? MWSyNlE2QThzNB?=
SNU-5 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK0TIg4PzKq NGrib3BFVVOR M3LKeGlEPTB;MT6zOVHDuTBwMEmx{txO NXrVO|Z1OjJzNUm4NVQ>
SNU-638 MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWC3Nog> NVnKN5A3TE2VTx?= NVL3NnZbUUN3ME2yMlI5OsLzMD6wOVPPxE1? MorvNlIyPTl6MUS=
SNU-16 NHfqZ|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnENGs4Omh? M4LI[2ROW09? Ml7RTWM2OD1zLkW3N:KyOC5yMEJOwG0> NILVPHUzOjF3OUixOC=>
SNU-484 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3PSHdxPzKq MUXEUXNQ NWWxeZZtUUN3ME2xMlczQMLzMD6wOFXPxE1? MnrqNlIyPTl6MUS=
SNU-620 M{DqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnJXIhvPzKq MULEUXNQ NHLzVYpKSzVyPUKuPVM6yrFyLkCwNe69VQ>? NInJXnQzOjF3OUixOC=>
SNU-719 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS3Nog> NYPGcXZKTE2VTx?= NGW2c4xKSzVyPUOuNFM4yrFyLkCzNu69VQ>? MY[yNlE2QThzNB?=
glioma cell lines NXf2Z25LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK3Nog> NVrvSJRzUUN3ME2xMVLPxE1? M1vOfFIzODZ3MEiw
U87 NH3XbVVCeG:ydH;zbZMhSXO|YYm= NHvpbIUz|ryP MX:3Nog> MYTpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?= MlniNlIxPjVyOEC=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT (T308) / p-AKT (S473) / AKT; 

PubMed: 27283525     


Left western blots showing levels of pAkt (T308), pAkt (S473) and total Akt in U87 cells exposed to buparlisib for 72 h. Right densitometric assessment of western blots, showing relative changes in phosphorylation.

p-FOXO3a (S253) / FOXO3a; 

PubMed: 28036259     


Cells were treated with 0.5 μM BKM120 for 24 h and cell lysates were immunoblotted with the indicated antibodies. Actin was used as the loading control.

Nuclear NF-κB p65 / NF-κB p65; 

PubMed: 26673665     


Western blots show BKM120 downregulating pAKT, nuclear NF-κB p65 and total NF-κB p65 in MDR and their parental cells. β-actin was used as a loading control for pAKT, AKT and total NF-κB p65. Lamin B was used as a loading control for nuclear NF-κB p65. 

p-ERK / ERK / LC3; 

PubMed: 27572309     


The indicated cell lines were exposed to different concentrations of BKM120 as indicated for 8 h A. or with 2 μM BKM120 for the indicated times B. The cells were then harvested for preparation of whole-cell protein lysates and subsequent Western blot analysis to detect the given proteins.

p-STAT3 / STAT3 / p-ERK / ERK / p-S6; 

PubMed: 29928341     


Western blot analysis of H460 and H2126 cell lysates using specific antibodies to phosphorylated or total proteins of STAT3, ERK1/2, AKT, S6 or GAPDH (loading control). The cells were treated with increasing concentrations of BKM120 for 24 h.

p-MET / MET; 

PubMed: 29928341     


The expression of phosphorylated or total forms of MET protein was analyzed by western blotting. 

27283525 28036259 26673665 27572309 29928341
Immunofluorescence
FOXO3a; 

PubMed: 28036259     


Cells were cultured on coverslips to approximately 60% confluency and then treated with 1 μM BKM120 for an additional 24 h. Immunofluorescence staining was performed using an anti-FOXO3a antibody and the nuclei were stained with DAPI. Scale bar, 20 μm.

28036259
Growth inhibition assay
Cell viability; 

PubMed: 26673665     


Dose-response curves were used to calculate the IC50 of BKM120 for MCs of MCF-7/A02 cells (upper) and CALDOX cells (lower).

26673665
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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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 NVP-BKM120
Smiles NC1=CC(=C(C=N1)C2=NC(=NC(=C2)N3CCOCC3)N4CCOCC4)C(F)(F)F

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02614508 Terminated Drug: Buparlisib|Drug: Ibrutinib|Biological: Ofatumumab 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 Drug: BKM120 Treatment for Metastatic or Locally Advanced Cervical Cancer Novartis Pharmaceuticals|Novartis November 2015 Phase 2
NCT01953445 Withdrawn Drug: paclitaxel|Drug: BKM120 Breast Neoplasms Washington University School of Medicine August 2014 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

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

Tags: buy Buparlisib (BKM120) | Buparlisib (BKM120) supplier | purchase Buparlisib (BKM120) | Buparlisib (BKM120) cost | Buparlisib (BKM120) manufacturer | order Buparlisib (BKM120) | Buparlisib (BKM120) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID