Buparlisib (BKM120)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

157 publications

Buparlisib (BKM120) Chemical Structure

CAS No. 944396-07-0

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. Buparlisib induces apoptosis. Phase 2.

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Selleck's Buparlisib (BKM120) has been cited by 157 publications

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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. Buparlisib induces apoptosis. 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 MVHDfZRwfG:6aXOgRZN{[Xl? NIPuV2Y4OiCq M2XvNGROW09? M4PmOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFiRUW0OWshdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFE2QCEQvF2= M2XkVVI1QTByMk[2
DU145 MVnDfZRwfG:6aXOgRZN{[Xl? NHvZ[Gk4OiCq MlnmSG1UVw>? M1PIOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiTFvCNUBufXSjboSge4l1cCCJSUWwJI9nKDBwMECwOFM2KM7:TR?= MlPJNlQ6ODB{Nk[=
A2780 NYfIWGhtS3m2b4TvfIlkKEG|c3H5 NYfoNZhRPzJiaB?= NYDKemJmTE2VTx?= M4PvXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2= MlTnNlQ6ODB{Nk[=
U87MG MVLDfZRwfG:6aXOgRZN{[Xl? MmDRO|IhcA>? NYPWWoR4TE2VTx?= MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh|ryP NYHkTo94OjR7MECyOlY>
A2780 MXLGeY5kfGmxbjDBd5NigQ>? MWixJIg> MXrEUXNQ MmqyTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkC1OUDPxE1? MlvBNlQ6ODB{Nk[=
DU145 M{LXd2Z2dmO2aX;uJGF{e2G7 NVXGS|lzOSCq NIq1c2dFVVOR MmL0TY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? MlX0NlQ6ODB{Nk[=
A2780 M1:1S2Z2dmO2aX;uJGF{e2G7 MXGxJIg> NUfofHVITE2VTx?= M3\HZ2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP MnqzNlQ6ODB{Nk[=
MCF7 MYTGeY5kfGmxbjDBd5NigQ>? MnT2NUBp NVO3VWdLTE2VTx?= M4PyemlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFW1OFVMKG23dHHueE1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6xJO69VQ>? M{H0R|I1QTByMk[2
U87MG Mo\hSpVv[3Srb36gRZN{[Xl? MUSxJIg> M4TSVmROW09? NVvGWYw2UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJHU5P02JIHPlcIx{KHerdHigSWM2OCCxZjCwMlE{KM7:TR?= NI\5Rm4zPDlyMEK2Oi=>
A2780 NIjpfJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXI[nhOPzJiaB?= MYLEUXNQ MnTySWM2OD1yLkWyJO69VQ>? MVuyOFkxODJ4Nh?=
SKMES-1 MWjDfZRwfG:6aXOgRZN{[Xl? MoLSNUDPxE1? NF7xVWY4OiCq NUPidGhNUW6mdXPld{Bk\WyuIHTlZZRp MWCyOlAyOzNzOB?=
H596 MkjlSpVv[3Srb36gRZN{[Xl? M{j0dVEh|ryP NXvF[XA6UW2yYXnyd{Bk\WyuIH3p[5JifGmxbh?= MUKyOlAyOzNzOB?=
HCC2450 MljrSpVv[3Srb36gRZN{[Xl? MXexJO69VQ>? NWmwfHF6UW2yYXnyd{Bk\WyuIHnueoF{cW:w NH:4PYMzPjBzM{OxPC=>
A549 M{D5NGZ2dmO2aX;uJGF{e2G7 NYX3Z3lDPTByIH7N NI\6cVk1QCCq NH7RZoNFVVOR M{LMcGlvcGmkaYTzJGFsfCCjY4TpeoF1cW:w MYGyOVk{PzJ7OR?=
A549 NIPtVHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO0SJYyKM7:TR?= MlzZO|IhcA>? Ml\YSG1UVw>? M2LlemlvcGmkaYTzJINmdGxiZ4Lve5Rp NX3GbVRVOjV7M{eyPVk>
H522 NETHR5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[3dY0yKM7:TR?= MnTmO|IhcA>? M4XvbGROW09? MVzJcohq[mm2czDj[YxtKGe{b4f0bC=> MWKyOVk{PzJ7OR?=
LNCaP M1TncmZ2dmO2aX;uJGF{e2G7 NU\j[W91OSEQvF2= NUPhSGw3W3WycILld5NmeyCyLVHLWEBt\X[nbIO= NITSUVEzPTN4MEe5PS=>
LNCaP95 M4X5PGZ2dmO2aX;uJGF{e2G7 MVqxJO69VQ>? MYXTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? NYG4WVF5OjV|NkC3PVk>
HCT-15 NX6zSmFjSXCxdH;zbZMhSXO|YYm= M4rNflExKM7:TR?= NIHNbHE1QCCq NFf0OG1FVVOR MkfaTY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUG1JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? NV63cotGOjVzNUKyOFU>
HCT-116 M2PYTWFxd3Sxc3nzJGF{e2G7 NHPlW5YyOCEQvF2= NXnySI9vPDhiaB?= MXzEUXNQ MWTJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MoLWNlUyPTJ{NEW=
NCI-H460 M2T2Z2Fxd3Sxc3nzJGF{e2G7 MmDpNVAh|ryP MYG0PEBp MWDEUXNQ NYjITHNHUW6mdXPld{BieG:ydH;zbZMhcW5iTlPJMWg1PjBiY3XscJMhcGG{Yn;1dolv\yCSSVuzR2EhcG:2c4DveEBufXSjdHnvci=> MVGyOVE2OjJ2NR?=
SKOV-3 NX;ueHR7SXCxdH;zbZMhSXO|YYm= MoHyNVAh|ryP MoTYOFghcA>? MnvySG1UVw>? NUTRc49QUW6mdXPld{BieG:ydH;zbZMhcW5iU1vPWk0{KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= MnrlNlUyPTJ{NEW=
BSY-1 MoDxRZBwfG:|aYOgRZN{[Xl? M3HK[lExKM7:TR?= MlXLOFghcA>? MnH1SG1UVw>? MUPJcoR2[2W|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NGnkOW8zPTF3MkK0OS=>
MKN-1 NWfv[GdZSXCxdH;zbZMhSXO|YYm= NIHoc3cyOCEQvF2= NGX0[ZM1QCCq NYm5dGpNTE2VTx?= MUHJcoR2[2W|IHHwc5B1d3OrczDpckBOU05vMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NXfLeW5MOjVzNUKyOFU>
NCI-H522 NV[2NGZVSXCxdH;zbZMhSXO|YYm= NUiyTFRNOTBizszN NITpeFM1QCCq NF3BdFBFVVOR NWjROotPUW6mdXPld{BieG:ydH;zbZM> MUCyOVE2OjJ2NR?=
OVCAR-3 Ml\jRZBwfG:|aYOgRZN{[Xl? MV:xNEDPxE1? M2HpXFQ5KGh? MXTEUXNQ MlvLTY5lfWOnczDhdI9xfG:|aYO= NYfYPGF7OjVzNUKyOFU>
HBC-5 M1rvNmFxd3Sxc3nzJGF{e2G7 NFPQbnMyOCEQvF2= NVTwfmtsPDhiaB?= MljHSG1UVw>? Mk\kTY5lfWOnczDhdI9xfG:|aYO= M17WWFI2OTV{MkS1
RXF-631L NFXLN|ZCeG:2b4Ppd{BCe3OjeR?= MVSxNEDPxE1? MYe0PEBp MUjEUXNQ NFjQOIFKdmS3Y3XzJIFxd3C2b4Ppdy=> MnPXNlUyPTJ{NEW=
MKN-45 NYm2VopLSXCxdH;zbZMhSXO|YYm= NY[0eG5pOTBizszN NEm1Um01QCCq MmK5SG1UVw>? NUPQSZFDUW6mdXPld{BieG:ydH;zbZM> M1XYNFI2OTV{MkS1
BON-1 NHvBfVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfTOVAxKG6P M{HOU|ExKGR? MVfEUXNQ MX3Jcohq[mm2czDj[YxtKGe{b4f0bC=> MoLSNlUxOjZ{OUK=
BON-1 NV;QfI5wTnWwY4Tpc44hSXO|YYm= NVHrO4E4PTByIH7N MXq0JIg> NIfxZXlFVVOR MmLQTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= M{HHWlI2ODJ4Mkmy
QGP-1 Ml;NSpVv[3Srb36gRZN{[Xl? NGfCU242ODBibl2= NUOzVFZJPCCq NFf5ToxFVVOR NIf6S|RKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez NF\1TIwzPTB{NkK5Ni=>
Huh7 NX7BOpF5TnWwY4Tpc44hSXO|YYm= NHvPXHoyKM7:TR?= MV:xJIg> MX\EUXNQ NE\1[W5KdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHNmejR5NB?= NUDlfJNQOjVyMES0NFM>
BNL MnqzSpVv[3Srb36gRZN{[Xl? Mn\zNUDPxE1? MU[xJIg> M3rUcWROW09? M3ixbmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>? MYOyOVAxPDRyMx?=
MDA-MB-175 NGTn[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\ZWXAzOSEQvF2= NXGy[nJpPSCm NU\pd29CTE2VTx?= NIPsV|lKSzVyPEGg{txO MXSyOFg4QTd7Nh?=
MDA-MB-134 NF30cJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvNOZcyKM7:TR?= NUCxXoRzPSCm M4nNNGROW09? NVLL[pBPUUN3MEyxJO69VQ>? MV2yOFg4QTd7Nh?=
HCC1500 MlXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2xJO69VQ>? NF\zWI02KGR? NEK5ToZFVVOR MV7JR|UxRDFizszN NXLScZRXOjR6N{m3PVY>
EFM-19 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:xJO69VQ>? NGftUVI2KGR? NGLjc2RFVVOR MVXJR|UxRDFizszN M3XrVFI1QDd7N{m2
ZR-75-30 NGGwPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;lfmdoOSEQvF2= M1:2TVUh\A>? NWraV3lYTE2VTx?= NW\6TJN2UUN3MEyxJO69VQ>? NFnUe|gzPDh5OUe5Oi=>
MDA-MB-361 NX\TT|h4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKxJO69VQ>? MoTlOUBl MVnEUXNQ NVfOXlNTUUN3MEyxJO69VQ>? MnnJNlQ5Pzl5OU[=
T-47D NF7FfVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\Yd3JwOSEQvF2= MVG1JIQ> MkLoSG1UVw>? NIHQem5KSzVyPEGg{txO NHnDb5EzPDh5OUe5Oi=>
SK-BR-3 NHn4OmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxJO69VQ>? NULS[JpwPSCm M3myZmROW09? Mn;HTWM2ODxzIN88US=> MUCyOFg4QTd7Nh?=
UACC-732 MlO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1GwXFEh|ryP MX61JIQ> NIH1RnVFVVOR MYXJR|UxRDFizszN MYqyOFg4QTd7Nh?=
BT-474 NGHhd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi1RYpvOSEQvF2= NXXKSVBVPSCm NGn0OnVFVVOR M2eyemlEPTB:MTFOwG0> M{DX[lI1QDd7N{m2
HCC202 NXqwVYd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUexJO69VQ>? MnSwOUBl Mn\wSG1UVw>? NWm0NJpVUUN3MEyxJO69VQ>? M{X6WFI1QDd7N{m2
MCF7 M1rWbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{POTFEh|ryP MkjUOUBl M1ftNmROW09? NHG4XpJKSzVyPEGg{txO MWOyOFg4QTd7Nh?=
MDA-MB-415 NUPGTG5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fDXVEh|ryP MVK1JIQ> NVzremxyTE2VTx?= NUnISIFUUUN3MEyxJO69VQ>? M{T3UFI1QDd7N{m2
MDA-MB-453 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\INUDPxE1? NHP1R|Y2KGR? MkH3SG1UVw>? NWLtSHV6UUN3MEyxJO69VQ>? M1:yc|I1QDd7N{m2
ZR-75-1 NELrcIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe0W5JuOSEQvF2= NIrxXlc2KGR? MmLDSG1UVw>? NY\McoJwUUN3MEyxJO69VQ>? MVKyOFg4QTd7Nh?=
HCC38 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDTSIUyKM7:TR?= NVqxeGw2PSCm NUDXVYVpTE2VTx?= NHjCPHNKSzVyPEGg{txO M{G0ZVI1QDd7N{m2
HCC1419 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmxJO69VQ>? MmfwOUBl MlfZSG1UVw>? Mk\BTWM2ODxzIN88US=> M{jMc|I1QDd7N{m2
UACC-812 NITEW4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4n0N|Eh|ryP MXe1JIQ> MWHEUXNQ Mn;WTWM2ODxzIN88US=> NYHDU5RXOjR6N{m3PVY>
HCC1187 NIXDXXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj4RWFSOSEQvF2= MXG1JIQ> MWHEUXNQ MnrkTWM2ODxzIN88US=> MWmyOFg4QTd7Nh?=
KPL-1 MmfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOxJO69VQ>? M4eyS|Uh\A>? Ml32SG1UVw>? MUTJR|UxRDFizszN MWeyOFg4QTd7Nh?=
SUM-225 M1faSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILTNpkyKM7:TR?= M4roZlUh\A>? M4jGRmROW09? M1\lVWlEPTB:MTFOwG0> MlPQNlQ5Pzl5OU[=
EFM-192A M3GwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XlZ|Eh|ryP NXnnRo5MPSCm NXzqcog1TE2VTx?= NFrRToJKSzVyPEGg{txO NV7peGZEOjR6N{m3PVY>
JIMT-1 M3XpTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGxJO69VQ>? NXzNVo0yPSCm NIHFVpVFVVOR NWC4WodyUUN3MEyxJO69VQ>? NWHVXoJlOjR6N{m3PVY>
HCC1143 NYT0SG5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLYcW1LOSEQvF2= NXPUVI06PSCm M4Tjc2ROW09? M2\YTWlEPTB:MTFOwG0> M1\zPFI1QDd7N{m2
HCC2218 NXz4NZJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HUR|Eh|ryP NUf1[pVPPSCm M3XFTWROW09? NWrWdpNtUUN3MEyxJO69VQ>? NYDoVoZ5OjR6N{m3PVY>
MDA-MB-468 MnrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;3[4RGOSEQvF2= MV:1JIQ> NUH3XnpYTE2VTx?= MVvJR|UxRDFizszN MmDyNlQ5Pzl5OU[=
BT-20 NH;wZ5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3ONWcyKM7:TR?= M1nJUFUh\A>? NF7CRm5FVVOR MYLJR|UxRDFizszN MUiyOFg4QTd7Nh?=
MDA-MB-435 NIfHZ2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUexJO69VQ>? MWe1JIQ> M4[1SmROW09? MlHkTWM2ODxzIN88US=> NX7MfmpTOjR6N{m3PVY>
BT-549 MnLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHDNUDPxE1? MmTkOUBl M4DE[mROW09? NV\me49nUUN3MEyxJO69VQ>? M2XYSVI1QDd7N{m2
HCC1806 NFfPdFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:xJO69VQ>? MkPiOUBl MkLtSG1UVw>? NIHVeVJKSzVyPEGg{txO M{fDV|I1QDd7N{m2
HCC1937 NVLJVGJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[xJO69VQ>? M4HoeVUh\A>? MWfEUXNQ NYfpRVJHUUN3MEyxJO69VQ>? MkD4NlQ5Pzl5OU[=
Hs578T NUXzZWtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\ieJlQOSEQvF2= NXrGTWhRPSCm M2\rbGROW09? NETtZZRKSzVyPEGg{txO Mm\lNlQ5Pzl5OU[=
LN18 M2jrV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nMVVIxKM7:TR?= NInOfYI4OiCq M{jhO2ROW09? Ml7FTWM2ODx3IN88US=> M{T0bVI1PzRzMEe0
LN229 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXOyNEDPxE1? NX[1[XE4PzJiaB?= MXfEUXNQ M3TSPGlEPTB:NTFOwG0> MkD5NlQ4PDFyN{S=
LNZ308 M4PDbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fBSVIxKM7:TR?= NWrrZlJyPzJiaB?= MXXEUXNQ NGnXdoZKSzVyPEWg{txO NUjvXFF6OjR5NEGwO|Q>
T98G NFTPZWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrYTFdmOjBizszN MYq3NkBp NF7FWo1FVVOR NGTWSVVKSzVyPEWg{txO NID0UnQzPDd2MUC3OC=>
U87 M3j6NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{K3W|IxKM7:TR?= MmLLO|IhcA>? MljBSG1UVw>? NHv2NIZKSzVyPEWg{txO MlfFNlQ4PDFyN{S=
LN18 MXnGeY5kfGmxbjDBd5NigQ>? MVq1JO69VQ>? M2K4RVI1KGh? NXzIPJczTE2VTx?= NFjmcnpKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuW MUKyOFc1OTB5NB?=
LNZ308 NFXZUIJHfW6ldHnvckBCe3OjeR?= M2H5N|Uh|ryP NYe0e3BQOjRiaB?= M1LNNWROW09? MnThTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? Mnm0NlQ4PDFyN{S=
Saos-2 NHX0eYRHfW6ldHnvckBCe3OjeR?= NX7XNGhGPTBizszN MlzSOFghcA>? NIS5dWlKdmirYnn0d{Bk\WyuIHnueoF{cW:w M{LYdlI1PzJ5Nk[w
MG-63 NULoV3ZyTnWwY4Tpc44hSXO|YYm= MoDWOVAh|ryP M4DYSlQ5KGh? NY\WZWJ1UW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MnfmNlQ4Ojd4NkC=
SJSA-1 MmruSpVv[3Srb36gRZN{[Xl? NHz6eo02OCEQvF2= M17jRVQ5KGh? M17pV2lvcGmkaYTzJINmdGxiaX72ZZNqd25? MVOyOFczPzZ4MB?=
Saos-2 MoKzSpVv[3Srb36gRZN{[Xl? M2TZTVUxKM7:TR?= MkXqOFghcA>? NFWzVYVKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v NYrV[|RpOjR5Mke2OlA>
MG-63 MlXvSpVv[3Srb36gRZN{[Xl? NHvCUWk2OCEQvF2= MU[0PEBp Ml;UTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> M3jjU|I1PzJ5Nk[w
SJSA-1 NHXSVVJHfW6ldHnvckBCe3OjeR?= NF33Rm82OCEQvF2= MX60PEBp MnrBTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> MmnMNlQ4Ojd4NkC=
Saos-2 M2C5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT0bHo2OCEQvF2= NHO5SYo1QCCq NV3YOmJOUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= MXWyOFczPzZ4MB?=
MG-63 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHqycXE2OCEQvF2= MV20PEBp NGjWUXhKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MXWyOFczPzZ4MB?=
SJSA-1 MnfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLENVdrPTBizszN NX[y[oJ1PDhiaB?= NWfiNXNbUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= M3XWclI1PzJ5Nk[w
FaDu NW\4XWh1TnWwY4Tpc44hSXO|YYm= NHuzbYk2KM7:TR?= NF71T4gzPCCq NHP0PI5FVVOR NETTdYRT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> Mn;lNlQ3OzFzNEe=
EMT6 NEXjbm1HfW6ldHnvckBCe3OjeR?= Ml\UOUDPxE1? MWiyOEBp NFfSUGZFVVOR MXnS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= M4jkcVI1PjNzMUS3
HCT116 NF[1fnlHfW6ldHnvckBCe3OjeR?= MVe1JO69VQ>? M4CzbVI1KGh? M{jq[mROW09? NWft[JVsWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MVWyOFY{OTF2Nx?=
U87 NID1NJJHfW6ldHnvckBCe3OjeR?= MV61JO69VQ>? NX65XplTOjRiaB?= NX\l[WpoTE2VTx?= NIr3W2xT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> M4i0XVI1PjNzMUS3
GBM NW\JOYRnSXCxcITvd4l{KEG|c3H5 NYDhRnZPOs7:TR?= NUG1SmNpPDiq M4fEZ2ROW09? MmnPbY5lfWOnZDDobYdp\XJibHX2[Yx{KG:oIHHwc5B1d3OrczygZY5lKGSnY4LlZZNm\CClZXzsJJZq[WKrbHn0fS=> NFLxUG0zPDVyMES5Ni=>
BON M3Xz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLDT4h2OS13zszN M4\pTVczcA>? MlG1[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> Mn:xNlQ1PDN3MkO=
BON NWTqWJJrSXCxcITvd4l{KEG|c3H5 NG\HblUyNTYQvF2= NInhbYgzPGh? NVP3SZlZcW6lcnXhd4V{KGGyb4D0c5Nqew>? NXvEcItzOjR2NEO1NlM>
H1975 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOwMlMuQS54zszN NYrvfZRzPzKq M1PRXGROW09? MnLETWM2OD1zLkO4Oe69VQ>? NVfVV|YxOjR|M{e4OFY>
H1975 MnLVRZBweHSxc3nzJGF{e2G7 NXXLcpo3Os7:TR?= MmPmNlRp MXLEUXNQ NHLPVG1qdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>? MX6yOFM{Pzh2Nh?=
T-ALL MVrBdI9xfG:|aYOgRZN{[Xl? M2LwV4JmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= Ml;oNlQhd3JiNEjo M4nWSmROW09? M4Dv[YFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz M3XkdlI1OzFyN{O2
BCR-ABL NX3wdVlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;BNE4zPS1zMN88US=> M4[3W|Rl M4nCSJNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? M1\oelI1OjR2NkGy
LC-1/SQSF MXvGeY5kfGmxbjDBd5NigQ>? NXHiT2VOO87:TR?= NHPGcXkzPGh? NHXtR5JFVVOR NFjYVGJl\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw> MUSyN|k5ODB7Mx?=
Primary CLL cells MUjBdI9xfG:|aYOgRZN{[Xl? NYnuT3VZOS1zMN88US=> NW[3V2NTPDiq MnzhbY5lfWOnczDhdI9xfG:|aYOgbY4hS0yOIHPlcIx{KGmwZHXw[Y5l\W62IH;mJJBzd2ewb4P0bYMhdWG{a3Xydy=> NUPoelJHOjN6NUC4NFc>
Primary CLL cells M3TLeWtqdmG|ZTDBd5NigQ>? MlW4Nu69VQ>? Mm\1N|BucW5? M1[yTYRm[3KnYYPl[EBRUTONIHHjeIl3cXS7 NUHh[WF4OjN6NUC4NFc>
Primary CLL cells NXLZb3M3S3m2b4TvfIlkKEG|c3H5 NHjlXm8z|ryP NIDMbGUzPGh? MY\pcoR2[2W|IHPlcIwh[3m2b4TvfIlkcXS7 MoP0NlM5PTB6MEe=
human NSCLC cell lines MV3BdI9xfG:|aYOgRZN{[Xl? MnL0NE4yOjVvNN88US=> M2TNWVI1cA>? NXjDWW14TE2VTx?= MYDJR|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?= NH\zc5ozOzV4MkS3Ni=>
human HCC cell lines NH:3VJhE\WyuII\pZYJqdGm2eTDhd5NigQ>? NIDjRowxNjByNT2x{txO M3TLR|Q5cA>? NFHzbXZKSzVyPUJOwG0> MYKyN|Q5QTl7OR?=
Huh7 MnXYT4lv[XOnIFHzd4F6 NUfhVY11Oc7:TR?= NYfKToxnPDiq Mmfjd4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NHW0cFMzOzR6OUm5PS=>
SK-HEP1 NIL2TJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuxMVIx|ryP MWe3Nog> MYTEUXNQ NULscpl2UUN3MP-8oFHPxE1? MnO0NlM1PzlzM{[=
786-0 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfTNU0zOM7:TR?= Mn;DO|Jp NY[5T3B[TE2VTx?= MlyzTWM2OO,:nEJOwG0> MkXvNlM1PzlzM{[=
JVM2 NUjCVFZDS3m2b4TvfIlkcXS7IHHzd4F6 NIXFS5QxNjJvMkFOwG0> NF3NUmI4Omh? NIPuN|lFVVOR Mmn4TWM2OD1yLkpOwG0> NV3nPItrOjN{M{i2N|k>
EHEB M{CwTmN6fG:2b4jpZ4l1gSCjc4PhfS=> MVGwMlIuOjEQvF2= M4\ld|czcA>? MkjOSG1UVw>? MmC2TWM2OD1yLkhOwG0> MorCNlMzOzh4M{m=
MEC2 NFjFZXpEgXSxdH;4bYNqfHliYYPzZZk> NEnWeYcxNjJvMkFOwG0> NVr5UWNpPzKq NXWwVoZPTE2VTx?= MmDWTWM2OD1yLkhOwG0> M4nNV|I{OjN6NkO5
primary B-CLL lymphocytes MULBdI9xfG:|aYOgRZN{[Xl? MmPYTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MorPNlRp Mn3BSG1UVw>? NXvVdJJYUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>? NX\wemFyOjN{M{i2N|k>
primary B-CLL lymphocytes Ml7DT4lv[XOnIFHzd4F6 MUjJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m MX[yOIg> MVLpcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= NVj5SoNQOjN{M{i2N|k>
human NSCLC NXPjVnduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnYNE42NTMQvF2= M4m2NVczcA>? NWjCNWFGUUN3ME2x{txO NITlXoozOjd6MUO5Ny=>
human NSCLC NXK0TJV6U2mwYYPlJGF{e2G7 NITBO4Ey|ryP M1n4dlI1cA>? NYi1TVNEcW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=> MWiyNlc5OTN7Mx?=
Y1 cell line MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjLcG9UOC5zzszNM|HPxE1? MWWyOIg> MkLSSG1UVw>? M2GwdYlvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy| NEfYUmIzOjZ7MkmwOC=>
PIK3CA-mutant MCF7 NFX4SnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzFV5VIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= M{TPW|czcA>? M1n2bmdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P NGXMZVIzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 MVfLbY5ie2ViQYPzZZk> NIXsSHdKSzVyPUGxOOKyO26P MVO3Nog> NG\KN3dKSzVyPUGxOOKyO26PIHnuJJJm\HWlaX7nJGFsfCCyaH;zdIhwenmuYYTpc44hdGW4ZXzz M1TCVVIzPjV|OU[3
MCF7-myr-Akt NFG1OlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? MmjVO|Jp NFzsZ4dIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= NU\JZWE4OjJ4NUO5Olc>
colon cancer cell lines NHvMbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3FNE0yOM7:TR?= MX[3Nog> M4jZSWROW09? NITUZVZKSzVyPUJOwG0> MmPBNlI2PDN6NUe=
gastric cancer cell lines MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL2dFhROC1zMN88US=> MVG3Nog> MX;EUXNQ M2HhRWlEPTB;Mj21{txO NYTQ[5lqOjJ3NEO4OVc>
HCT-116/HT-29/MKN-45 MlyzRZBweHSxc3nzJGF{e2G7 NXrO[2M2Os7:TR?= MUK0PIg> M2\UO5NpcW[2IHnuJGczKHCqYYPl NVzHUXJSOjJ3NEO4OVc>
HT-29 and HCT-116 MXjDZZNx[XOnIHHzd4F6 M3XNOlXPxE1? MmDjNlRp MlTobY5lfWOnczDjZZNx[XOnIHHjeIl3cXS7 MY[yNlU1Ozh3Nx?=
MM cell lines M4KxOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M36zc|Ex|ryP NVj0WnpLOjSq MXfEUXNQ NYjxc5dYUUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn MkS0NlIzODd2OEW=
ARP-1 MV\BdI9xfG:|aYOgRZN{[Xl? NWTyeXBKOTEQvF2= MlfjNlRp M2r6eWROW09? NGPXSIlqdmS3Y3XzJG1OKGOnbHygZZBweHSxc3nzJJRpem:3Z3igZ4F{eGG|ZTDhZ5RqfmG2aX;u MXKyNlIxPzR6NR?=
SNU-601 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MluzO|Jp NIfodlNFVVOR M{nMXmlEPTB;MD64NVbDuTBwME[z{txO MlHhNlIyPTl6MUS=
SNU-1 Mlf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HTb|czcA>? NILMVo1FVVOR M17LWWlEPTB;MT6wPFLDuTBwMEK4{txO MmWyNlIyPTl6MUS=
SNU-668 NFO2T|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVO3Nog> MWXEUXNQ MojKTWM2OD1zLkW3PeKyOC5yN{VOwG0> NW\4eFJ4OjJzNUm4NVQ>
AGS M1naVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnQR29mPzKq NUnwSno{TE2VTx?= NH;1bnFKSzVyPUGuO|E1yrFyLkGxO:69VQ>? NX\1SGRuOjJzNUm4NVQ>
SNU-216 M4raPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{WzO|czcA>? M321b2ROW09? MoOwTWM2OD1{Lk[5NuKyOC5yOENOwG0> NWPhb|dTOjJzNUm4NVQ>
SNU-5 M2\0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vXWlczcA>? NHfrb|dFVVOR NXzENpRvUUN3ME2xMlM2OcLzMD6wPVHPxE1? Ml;3NlIyPTl6MUS=
SNU-638 NI\yZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTNO|Jp MmHzSG1UVw>? M4L2N2lEPTB;Mj6yPFLDuTBwMEWz{txO NHPWcpAzOjF3OUixOC=>
SNU-16 NHK1WHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj5O|Jp NEPhUVFFVVOR M1TvZWlEPTB;MT61O|PDuTBwMECx{txO NGrVRZYzOjF3OUixOC=>
SNU-484 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD2cnV4PzKq NXTSWWk6TE2VTx?= M2CwcWlEPTB;MT63NljDuTBwMES1{txO MXGyNlE2QThzNB?=
SNU-620 MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[3Nog> M4DH[mROW09? NEn5XFFKSzVyPUKuPVM6yrFyLkCwNe69VQ>? Mnr3NlIyPTl6MUS=
SNU-719 NXmzTZp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYK3Nog> M2m2PGROW09? NYW1VGFpUUN3ME2zMlA{P8LzMD6wN|LPxE1? MmC0NlIyPTl6MUS=
glioma cell lines MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH70PI44Omh? MUXJR|UxRTFvMt88US=> M4DkUlIzODZ3MEiw
U87 MXXBdI9xfG:|aYOgRZN{[Xl? MojiNu69VQ>? NUP4b2YzPzKq MorvbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= NHT4UY0zOjB4NUC4NC=>

... 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]
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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]
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  • 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.
  • 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)
Water Insoluble
Ethanol '2 mg/mL
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 C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

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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
NCT04338399 Not yet recruiting Drug: Buparlisib & Paclitaxel Head and Neck Cancer Adlai Nortye Biopharma Co. Ltd. July 31 2020 Phase 3
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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID