Buparlisib (BKM120)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

178 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 178 publications

Purity & Quality Control

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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 NXL1[Yl{S3m2b4TvfIlkKEG|c3H5 M4HSUFczKGh? M{\WXWROW09? NFrVSJREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN NG\J[GUzPDlyMEK2Oi=>
DU145 MnXmR5l1d3SxeHnjJGF{e2G7 MlHDO|IhcA>? NW\DUINSTE2VTx?= NFjUZ2dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2= NF6xS2ozPDlyMEK2Oi=>
A2780 M3TJ[WN6fG:2b4jpZ{BCe3OjeR?= M4PTbFczKGh? MVHEUXNQ M4r0SmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2= MljONlQ6ODB{Nk[=
U87MG NXPqVpluS3m2b4TvfIlkKEG|c3H5 MXe3NkBp MXrEUXNQ Mnn2R5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlk5KM7:TR?= NVvkNot5OjR7MECyOlY>
A2780 MVPGeY5kfGmxbjDBd5NigQ>? Mkj5NUBp NVGybpp7TE2VTx?= M37MW2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6wOVUh|ryP MXOyOFkxODJ4Nh?=
DU145 NE\jSnVHfW6ldHnvckBCe3OjeR?= MUixJIg> MmO4SG1UVw>? MY\Jcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>? MlKxNlQ6ODB{Nk[=
A2780 NH75OZFHfW6ldHnvckBCe3OjeR?= M2GxUFEhcA>? M1m3RmROW09? NI\MdJRKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDFR|UxKG:oIECuNFc1KM7:TR?= NXHINGl6OjR7MECyOlY>
MCF7 NVvqc5Z{TnWwY4Tpc44hSXO|YYm= MVGxJIg> NEHsR2ZFVVOR MkXGTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO M2G5cFI1QTByMk[2
U87MG NF64ZllHfW6ldHnvckBCe3OjeR?= NX35OGFuOSCq MXHEUXNQ MXzJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO MUWyOFkxODJ4Nh?=
A2780 M3\CeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUOyOIkzPzJiaB?= NWPqPW5KTE2VTx?= MoDQSWM2OD1yLkWyJO69VQ>? NULhbWRPOjR7MECyOlY>
SKMES-1 MoHrR5l1d3SxeHnjJGF{e2G7 M3L1fFEh|ryP M4TpRVczKGh? NEXHV2NKdmS3Y3XzJINmdGxiZHXheIg> NF3IelMzPjBzM{OxPC=>
H596 NUXuUGtuTnWwY4Tpc44hSXO|YYm= MWSxJO69VQ>? NWnuNo53UW2yYXnyd{Bk\WyuIH3p[5JifGmxbh?= M1fwPVI3ODF|M{G4
HCC2450 M2TxO2Z2dmO2aX;uJGF{e2G7 M2fkdFEh|ryP MX7JcZBicXK|IHPlcIwhcW64YYPpc44> MXSyOlAyOzNzOB?=
A549 MlXRSpVv[3Srb36gRZN{[Xl? M13KTFUxOCCwTR?= MYW0PEBp NVPjNZcyTE2VTx?= NIWyTWdKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= NY[2TYVpOjV7M{eyPVk>
A549 NWfaRnZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\GVVEh|ryP Mn\MO|IhcA>? NEK0R2RFVVOR MVvJcohq[mm2czDj[YxtKGe{b4f0bC=> MVmyOVk{PzJ7OR?=
H522 NFjaTXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:xJO69VQ>? NWHlS2M6PzJiaB?= NILYXXFFVVOR MmrTTY5pcWKrdIOgZ4VtdCCpcn;3eIg> MorUNlU6Ozd{OUm=
LNCaP NH3oZZZHfW6ldHnvckBCe3OjeR?= NYfWWYd1OSEQvF2= M4nWPHN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| M1HGOlI2OzZyN{m5
LNCaP95 NEH2ToxHfW6ldHnvckBCe3OjeR?= M{TP[|Eh|ryP MmX6V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? M1\kVFI2OzZyN{m5
HCT-15 NEjyVJRCeG:2b4Ppd{BCe3OjeR?= MojUNVAh|ryP MoDJOFghcA>? MoL1SG1UVw>? MkK0TY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUG1JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? Ml34NlUyPTJ{NEW=
HCT-116 MUXBdI91d3OrczDBd5NigQ>? NXHsbpNvOTBizszN MnSzOFghcA>? M3rlUWROW09? MYnJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MXOyOVE2OjJ2NR?=
NCI-H460 M4TZWWFxd3Sxc3nzJGF{e2G7 M2jZXFExKM7:TR?= M3\UOlQ5KGh? NHvKdndFVVOR NETTPG1KdmS3Y3XzJIFxd3C2b4Ppd{BqdiCQQ1mtTFQ3OCClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u MU[yOVE2OjJ2NR?=
SKOV-3 NWDzOJA2SXCxdH;zbZMhSXO|YYm= NHjHTY8yOCEQvF2= NW\QfIJxPDhiaB?= Ml6wSG1UVw>? MYXJcoR2[2W|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NXXpN3dYOjVzNUKyOFU>
BSY-1 MUfBdI91d3OrczDBd5NigQ>? M1LpWFExKM7:TR?= Ml\qOFghcA>? MnHwSG1UVw>? NFfXNWtKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCEU2mtNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NITCSVgzPTF3MkK0OS=>
MKN-1 NXjRVIpOSXCxdH;zbZMhSXO|YYm= MVSxNEDPxE1? MXm0PEBp NGG4TFFFVVOR NWPsUYI2UW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NUL6R5FDOjVzNUKyOFU>
NCI-H522 MUPBdI91d3OrczDBd5NigQ>? MYKxNEDPxE1? M3\sUFQ5KGh? M2G0fWROW09? M4myUWlv\HWlZYOgZZBweHSxc3nz MmO3NlUyPTJ{NEW=
OVCAR-3 M2fHZWFxd3Sxc3nzJGF{e2G7 NIXibG0yOCEQvF2= NXTSS4k2PDhiaB?= M{HrT2ROW09? NHLEbXZKdmS3Y3XzJIFxd3C2b4Ppdy=> NV;Fe3dIOjVzNUKyOFU>
HBC-5 M2fRbGFxd3Sxc3nzJGF{e2G7 MW[xNEDPxE1? NHPRSIQ1QCCq MmnNSG1UVw>? Mn:4TY5lfWOnczDhdI9xfG:|aYO= M1fzTVI2OTV{MkS1
RXF-631L NX;iNYFQSXCxdH;zbZMhSXO|YYm= MUmxNEDPxE1? MWq0PEBp MXrEUXNQ MULJcoR2[2W|IHHwc5B1d3Orcx?= NHfwNJYzPTF3MkK0OS=>
MKN-45 M1e2bGFxd3Sxc3nzJGF{e2G7 M2jTRVExKM7:TR?= MmPCOFghcA>? NV76TVFoTE2VTx?= NWD2XHBwUW6mdXPld{BieG:ydH;zbZM> NETMcFAzPTF3MkK0OS=>
BON-1 M3vtPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfiOGY2ODBibl2= M4CyWlExKGR? M{naW2ROW09? M2jz[mlvcGmkaYTzJINmdGxiZ4Lve5Rp NF\ydFgzPTB{NkK5Ni=>
BON-1 M{PjZ2Z2dmO2aX;uJGF{e2G7 NEXwVHo2ODBibl2= NVfQZ2hHPCCq M4X0cWROW09? NWHzTI57UW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> MVKyOVAzPjJ7Mh?=
QGP-1 M{TwSGZ2dmO2aX;uJGF{e2G7 M4nid|UxOCCwTR?= NGPtSnY1KGh? MXLEUXNQ Mm\DTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= M1vMVVI2ODJ4Mkmy
Huh7 NHP2fIpHfW6ldHnvckBCe3OjeR?= NIHhN5YyKM7:TR?= Ml:yNUBp MUHEUXNQ NVLU[YhKUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S= MYSyOVAxPDRyMx?=
BNL MoLtSpVv[3Srb36gRZN{[Xl? NGH2c24yKM7:TR?= M2TSNFEhcA>? MXHEUXNQ M1fQbGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>? M{Lyb|I2ODB2NECz
MDA-MB-175 MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnH[ZkyKM7:TR?= MU[1JIQ> NX\XcIlrTE2VTx?= Ml\YTWM2ODxzIN88US=> NXfHWVlWOjR6N{m3PVY>
MDA-MB-134 NVTvXmhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTp[nIyKM7:TR?= Mn[yOUBl M4W3bGROW09? MYXJR|UxRDFizszN Mme3NlQ5Pzl5OU[=
HCC1500 M2\sNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[xJO69VQ>? NGrTdJU2KGR? M4XoPWROW09? NX:xOJp5UUN3MEyxJO69VQ>? NGTVbGMzPDh5OUe5Oi=>
EFM-19 MkjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLiNUDPxE1? MnLlOUBl M3jN[mROW09? M{LQO2lEPTB:MTFOwG0> NE\YSJozPDh5OUe5Oi=>
ZR-75-30 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T0fVEh|ryP MV21JIQ> NInPdXJFVVOR M2nGU2lEPTB:MTFOwG0> NGLF[|YzPDh5OUe5Oi=>
MDA-MB-361 MmT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3ne2w3OSEQvF2= MU[1JIQ> M2LxRmROW09? M2HsUmlEPTB:MTFOwG0> MYiyOFg4QTd7Nh?=
T-47D NFG5c3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXDdm04OSEQvF2= NX\BXIFwPSCm M1PpeGROW09? MnnBTWM2ODxzIN88US=> NVrG[WZLOjR6N{m3PVY>
SK-BR-3 M3PKSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILCdWYyKM7:TR?= NXrUd3lsPSCm M3;SOmROW09? NV64cHU4UUN3MEyxJO69VQ>? NXLTcmdlOjR6N{m3PVY>
UACC-732 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljvNUDPxE1? M1;GdFUh\A>? M2q5V2ROW09? M1vFb2lEPTB:MTFOwG0> NFP6VpIzPDh5OUe5Oi=>
BT-474 NYDtdmg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPSNUDPxE1? MWK1JIQ> M2S2V2ROW09? NHHHfmRKSzVyPEGg{txO M{TVeVI1QDd7N{m2
HCC202 NIX3THdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTWNUDPxE1? MYK1JIQ> NFz5ZYxFVVOR MoiyTWM2ODxzIN88US=> NHnCPVAzPDh5OUe5Oi=>
MCF7 NFLFbpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYqxJO69VQ>? MWO1JIQ> NWrIbVlyTE2VTx?= M3XqSGlEPTB:MTFOwG0> NYfFNWJ3OjR6N{m3PVY>
MDA-MB-415 NEjnVIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGracnoyKM7:TR?= M2rIPVUh\A>? NH63cFBFVVOR MWjJR|UxRDFizszN MlXpNlQ5Pzl5OU[=
MDA-MB-453 MlrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDnbIMyKM7:TR?= Mn;COUBl NUXUXYJGTE2VTx?= M2rubWlEPTB:MTFOwG0> MVGyOFg4QTd7Nh?=
ZR-75-1 MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\RNFEh|ryP M2nuSVUh\A>? M{PsT2ROW09? NYDVeWN2UUN3MEyxJO69VQ>? NWj4VnVmOjR6N{m3PVY>
HCC38 M3LFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\SNUDPxE1? NVTzdI1wPSCm NWXVd45OTE2VTx?= NGK4UGhKSzVyPEGg{txO NELYVI4zPDh5OUe5Oi=>
HCC1419 NFnPVmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3neXNsOSEQvF2= MXS1JIQ> MlTGSG1UVw>? MUDJR|UxRDFizszN NVWyXmdLOjR6N{m3PVY>
UACC-812 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCxJO69VQ>? NFX1cVA2KGR? NXj4dpE{TE2VTx?= NYHxZ|lsUUN3MEyxJO69VQ>? MWOyOFg4QTd7Nh?=
HCC1187 NFXJRm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M364e|Eh|ryP MWq1JIQ> NGDJVmFFVVOR MmXoTWM2ODxzIN88US=> NImwRXQzPDh5OUe5Oi=>
KPL-1 NETMeWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn2xNUDPxE1? NXLJWJhNPSCm MVrEUXNQ MXjJR|UxRDFizszN NXrFcYNiOjR6N{m3PVY>
SUM-225 NH7QRYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjP[G8yKM7:TR?= Mlj2OUBl MlvtSG1UVw>? NXju[IdjUUN3MEyxJO69VQ>? M{[xNVI1QDd7N{m2
EFM-192A M1f3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;RSppyOSEQvF2= MYe1JIQ> Ml2xSG1UVw>? MY\JR|UxRDFizszN MYeyOFg4QTd7Nh?=
JIMT-1 M2\x[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKxJO69VQ>? M2\mTFUh\A>? M122cGROW09? NX33NZJQUUN3MEyxJO69VQ>? NIHzXVIzPDh5OUe5Oi=>
HCC1143 NUnVXGlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1r6SFEh|ryP M{K0S|Uh\A>? NYPyc285TE2VTx?= M3O2cWlEPTB:MTFOwG0> MU[yOFg4QTd7Nh?=
HCC2218 NIP2b25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfRcYlLOSEQvF2= MY[1JIQ> NVTNe3RZTE2VTx?= M1\I[GlEPTB:MTFOwG0> NIC1b2EzPDh5OUe5Oi=>
MDA-MB-468 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXixJO69VQ>? MX21JIQ> NV\WTmlITE2VTx?= MW\JR|UxRDFizszN NIPvU|AzPDh5OUe5Oi=>
BT-20 NUDre2JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVu5SoxGOSEQvF2= MlrHOUBl M3PibGROW09? MYXJR|UxRDFizszN MWOyOFg4QTd7Nh?=
MDA-MB-435 M1\JfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvofFJtOSEQvF2= NYfweY9PPSCm M4jvUWROW09? NIPib2JKSzVyPEGg{txO M{P0WlI1QDd7N{m2
BT-549 MnjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6xJO69VQ>? NHLCTFg2KGR? M{HROWROW09? NWLtfWxjUUN3MEyxJO69VQ>? NH60UI8zPDh5OUe5Oi=>
HCC1806 NUPXe2plT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nLZ|Eh|ryP NHHzNWI2KGR? MWPEUXNQ M{P1d2lEPTB:MTFOwG0> NFSzdYgzPDh5OUe5Oi=>
HCC1937 NWnvN2ZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17jOlEh|ryP NEj4TGU2KGR? MnmxSG1UVw>? M{PlfGlEPTB:MTFOwG0> MlXrNlQ5Pzl5OU[=
Hs578T MlX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jOdVEh|ryP MWi1JIQ> NVXEW5I6TE2VTx?= M2TGc2lEPTB:MTFOwG0> M3GwWlI1QDd7N{m2
LN18 MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTiNlAh|ryP MlfSO|IhcA>? MnnMSG1UVw>? MmLFTWM2ODx3IN88US=> M13o[VI1PzRzMEe0
LN229 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7rPVQzOCEQvF2= MX23NkBp NX7VNI1PTE2VTx?= MoHZTWM2ODx3IN88US=> M1LLbVI1PzRzMEe0
LNZ308 NYDUdGhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTsUo0zOCEQvF2= M3ixSFczKGh? NFTZZ3dFVVOR NHzTXFNKSzVyPEWg{txO MorlNlQ4PDFyN{S=
T98G Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[yNEDPxE1? NHPSR4s4OiCq MYLEUXNQ NWnWZWx6UUN3MEy1JO69VQ>? NI\6XmIzPDd2MUC3OC=>
U87 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLRPWMzOCEQvF2= MlPQO|IhcA>? MVrEUXNQ NFq1U5hKSzVyPEWg{txO M1HOcFI1PzRzMEe0
LN18 MYTGeY5kfGmxbjDBd5NigQ>? M3XFelUh|ryP NV7GT4N3OjRiaB?= M4PabWROW09? MV7Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV MnHiNlQ4PDFyN{S=
LNZ308 MXzGeY5kfGmxbjDBd5NigQ>? MmDpOUDPxE1? M4\UfFI1KGh? MVHEUXNQ Mo\KTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MUeyOFc1OTB5NB?=
Saos-2 M{X5fGZ2dmO2aX;uJGF{e2G7 Mlr5OVAh|ryP NEGzc481QCCq NY\rU|U1UW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MnvKNlQ4Ojd4NkC=
MG-63 M3LafmZ2dmO2aX;uJGF{e2G7 M4jnTVUxKM7:TR?= NVnSPVR2PDhiaB?= NF76OZRKdmirYnn0d{Bk\WyuIHnueoF{cW:w MnXGNlQ4Ojd4NkC=
SJSA-1 NFjqVVhHfW6ldHnvckBCe3OjeR?= MUO1NEDPxE1? MmriOFghcA>? NVixOm5iUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MXmyOFczPzZ4MB?=
Saos-2 NUe1TYV1TnWwY4Tpc44hSXO|YYm= MXK1NEDPxE1? MnTqOFghcA>? NWTaZnhFUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? MlXQNlQ4Ojd4NkC=
MG-63 Moq2SpVv[3Srb36gRZN{[Xl? NYW0OG9oPTBizszN MmfKOFghcA>? M1e4SmlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MWqyOFczPzZ4MB?=
SJSA-1 MmPlSpVv[3Srb36gRZN{[Xl? MmPrOVAh|ryP NFPsdXc1QCCq M1;xe2lvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MY[yOFczPzZ4MB?=
Saos-2 NEjSZoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz2ZW9HPTBizszN NVy5N2poPDhiaB?= NHLiUopKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MUiyOFczPzZ4MB?=
MG-63 NXXNcXpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LlVVUxKM7:TR?= MV:0PEBp M1XjPGlvcGmkaYTzJINmdGxidnnhZoltcXS7 NIr2coIzPDd{N{[2NC=>
SJSA-1 NGrFdYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrJT4E2OCEQvF2= Ml61OFghcA>? MUjJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? M{TFcFI1PzJ5Nk[w
FaDu M4rKfGZ2dmO2aX;uJGF{e2G7 M17ZelUh|ryP NVzpUYVsOjRiaB?= Ml3kSG1UVw>? NWT1bYNoWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> M3ftWlI1PjNzMUS3
EMT6 M{\kOmZ2dmO2aX;uJGF{e2G7 M2noVVUh|ryP MW[yOEBp NHe1SlFFVVOR M{T2bXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u NXXJbmpiOjR4M{GxOFc>
HCT116 NUPiWWp2TnWwY4Tpc44hSXO|YYm= MkXBOUDPxE1? M{PaTVI1KGh? M4e4Z2ROW09? M4m0V3Jm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u NYTOU5lROjR4M{GxOFc>
U87 NWnnVFc4TnWwY4Tpc44hSXO|YYm= M{PhS|Uh|ryP MlXlNlQhcA>? NYH6ZVNbTE2VTx?= M2fLW3Jm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u MWWyOFY{OTF2Nx?=
GBM MWXBdI9xfG:|aYOgRZN{[Xl? MYmy{txO MkD6OFhp Mn;6SG1UVw>? Mn;QbY5lfWOnZDDobYdp\XJibHX2[Yx{KG:oIHHwc5B1d3OrczygZY5lKGSnY4LlZZNm\CClZXzsJJZq[WKrbHn0fS=> M1:0dVI1PTByNEmy
BON MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[xMVXPxE1? M1PmfFczcA>? MnG4[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NFu3bngzPDR2M{WyNy=>
BON M2PDUGFxd3C2b4Ppd{BCe3OjeR?= NGXlZYwyNTYQvF2= M3vCTVI1cA>? M4n6PYlv[3KnYYPld{BieG:ydH;zbZM> NWr5bFFnOjR2NEO1NlM>
H1975 NWrqd3hrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[wMlMuQS54zszN NUfWR5pKPzKq NIDPXpZFVVOR M1XFPGlEPTB;MT6zPFXPxE1? MXuyOFM{Pzh2Nh?=
H1975 MnrZRZBweHSxc3nzJGF{e2G7 M3Xtd|LPxE1? M3;ZdlI1cA>? NU\2OnJFTE2VTx?= NYPoblJscW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl? MVqyOFM{Pzh2Nh?=
T-ALL MnvaRZBweHSxc3nzJGF{e2G7 MUHi[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV? M{DYWFI1KG:{IES4bC=> Ml\zSG1UVw>? NYDyN5lN[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM> M3jrZVI1OzFyN{O2
BCR-ABL NIexd49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEX0VYYxNjJ3LUGw{txO NEfRN4U1\A>? MmT3d4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>? Mn;CNlQzPDR4MUK=
LC-1/SQSF NEXnemdHfW6ldHnvckBCe3OjeR?= NHXabpo{|ryP M4OwVVI1cA>? MoC4SG1UVw>? MVjk[YNz\WG|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy= MXqyN|k5ODB7Mx?=
Primary CLL cells NF7Ie5FCeG:ydH;zbZMhSXO|YYm= MkL1NU0yOM7:TR?= M3n5XFQ5cA>? NELwNYpqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ M173PVI{QDVyOEC3
Primary CLL cells MoniT4lv[XOnIFHzd4F6 NY[zW5dOOs7:TR?= NVP3VZJSOzCvaX6= MlzC[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? NF3ERpYzOzh3MEiwOy=>
Primary CLL cells NYLiVnZIS3m2b4TvfIlkKEG|c3H5 MXqy{txO NGjvb48zPGh? M{TxPYlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= MmW2NlM5PTB6MEe=
human NSCLC cell lines NXfl[YlqSXCxcITvd4l{KEG|c3H5 MoLtNE4yOjVvNN88US=> NXn1RmQzOjSq MYLEUXNQ NWrNW2JIUUN3MIOgdoFv\2W|IH\yc40hOC52LUNOwG0> Mlj6NlM2PjJ2N{K=
human HCC cell lines M4rqS2NmdGxidnnhZoltcXS7IHHzd4F6 NWO1eGs1OC5yMEWtNe69VQ>? NVT0SnJ[PDiq MorPTWM2OD1zzszN NYLoW|Y4OjN2OEm5PVk>
Huh7 MUDLbY5ie2ViQYPzZZk> M1nPeFHPxE1? NXXySZBPPDiq MWLzbYdvce,ugXPhcpRtgSC{ZXT1Z4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= MoTvNlM1QDl7OUm=
SK-HEP1 NGfpdoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULzZVdsOS1{MN88US=> NVzHb45DPzKq MYfEUXNQ NWK2eVg{UUN3MP-8oFHPxE1? NFXWXnYzOzR5OUGzOi=>
786-0 NV7RZXNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWexMVIx|ryP NF6we2I4Omh? MnvkSG1UVw>? Mn36TWM2OO,:nEJOwG0> MlHDNlM1PzlzM{[=
JVM2 NFfhWYlEgXSxdH;4bYNqfHliYYPzZZk> MlTGNE4zNTJyzszN NFvWfWs4Omh? NVW4NVJtTE2VTx?= MoDLTWM2OD1yLkpOwG0> MmHvNlMzOzh4M{m=
EHEB NXfMSG02S3m2b4TvfIlkcXS7IHHzd4F6 NFXZRYExNjJvMkFOwG0> M1\Jd|czcA>? MYfEUXNQ MkDlTWM2OD1yLkhOwG0> NUHzfIpnOjN{M{i2N|k>
MEC2 Mk\yR5l1d3SxeHnjbZR6KGG|c3H5 NUPxXFJIOC5{LUKw{txO NEXQPGM4Omh? NIXwTo5FVVOR M4HZ[2lEPTB;MD63{txO MkPNNlMzOzh4M{m=
primary B-CLL lymphocytes MnLrRZBweHSxc3nzJGF{e2G7 Mn;XTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MVyyOIg> M17EUGROW09? MVHJR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz MmDHNlMzOzh4M{m=
primary B-CLL lymphocytes MkXRT4lv[XOnIFHzd4F6 NF3sfWxKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n NHy1TW8zPGh? MYTpcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= NUi4XZg6OjN{M{i2N|k>
human NSCLC MmfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:1VJMxNjVvMt88US=> M4jwc|czcA>? NFfYOnJKSzVyPUJOwG0> M4HocVIzPzhzM{mz
human NSCLC NHP1UHlMcW6jc3WgRZN{[Xl? M2TFOVHPxE1? NGfVfHUzPGh? MV;pcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 MlrHNlI4QDF|OUO=
Y1 cell line MoC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrYSHUxNjIQvF2vNe69VQ>? M3HUV|I1cA>? MWfEUXNQ MmPNbY5pcWKrdIOgOlDwxIViY3XscEB3cWGkaXzpeJkhcW5iTYnjMXNkfHJvdILhcpNn\WO2ZXSgZ4VtdHN? NHniOWkzOjZ7MkmwOC=>
PIK3CA-mutant MCF7 NWK4e3Z4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVruTnFbT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= MXy3Nog> NI[3[3VIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= M4e2eVIzPjV|OU[3
PIK3CA-mutant MCF7 NULubY1bU2mwYYPlJGF{e2G7 MmfZTWM2OD1zMUVCtVNvVQ>? MnO5O|Jp MlrqTWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= M3rtbVIzPjV|OU[3
MCF7-myr-Akt MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInuXpRIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= NF\XRWs4Omh? M3vmfWdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P M3nZWFIzPjV|OU[3
colon cancer cell lines NHzzTFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSwMVEx|ryP MoO2O|Jp M4XlTWROW09? MYLJR|UxRTIQvF2= NUKwZ|BkOjJ3NEO4OVc>
gastric cancer cell lines MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLQNo8xNTFyzszN NVHNWoZFPzKq M4nyNmROW09? MkftTWM2OD1{LUZOwG0> NX62N5JkOjJ3NEO4OVc>
HCT-116/HT-29/MKN-45 M4LGR2Fxd3C2b4Ppd{BCe3OjeR?= MV:y{txO MYW0PIg> M4n2cZNpcW[2IHnuJGczKHCqYYPl M3PMd|IzPTR|OEW3
HT-29 and HCT-116 NXPP[YhJS2G|cHHz[UBie3OjeR?= MWO1{txO M1fSdlI1cA>? NHK5OnJqdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm= NHrQVXkzOjV2M{i1Oy=>
MM cell lines MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGxNO69VQ>? NFLYfXEzPGh? Mlf2SG1UVw>? NUTvTJdJUUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn M2e3NFIzOjB5NEi1
ARP-1 MYDBdI9xfG:|aYOgRZN{[Xl? MkDuNVDPxE1? NHLXeXozPGh? NHLG[HlFVVOR M{PYWIlv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= MlvTNlIzODd2OEW=
SNU-601 NGjHUZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUS0cJpvPzKq M332ZmROW09? MoL6TWM2OD1yLkixOuKyOC5yNkROwG0> M1zYOlIzOTV7OEG0
SNU-1 M3PVbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v5UFczcA>? M2jzW2ROW09? M3nTW2lEPTB;MT6wPFLDuTBwMEK4{txO MljRNlIyPTl6MUS=
SNU-668 M4O5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGKzVGc4Omh? NEj6SZZFVVOR M1zubGlEPTB;MT61O|nDuTBwMEe0{txO M4nXflIzOTV7OEG0
AGS MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jaNFczcA>? M3W0[mROW09? MoPSTWM2OD1zLkexOOKyOC5zMUhOwG0> MYWyNlE2QThzNB?=
SNU-216 MkXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVK3Nog> MV;EUXNQ NGXU[4dKSzVyPUKuOlkzyrFyLkC4Nu69VQ>? MnHHNlIyPTl6MUS=
SNU-5 M{jUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPDWJdxPzKq MlXJSG1UVw>? NEjUWphKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? MlfuNlIyPTl6MUS=
SNU-638 M1H4VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHy[2Q4Omh? M2HXTmROW09? M4TYbWlEPTB;Mj6yPFLDuTBwMEWz{txO NX7YO|hQOjJzNUm4NVQ>
SNU-16 MmT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3QXmxNPzKq MV\EUXNQ M33oVmlEPTB;MT61O|PDuTBwMECx{txO MWqyNlE2QThzNB?=
SNU-484 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHUO|Jp NEXySINFVVOR MXvJR|UxRTFwN{K4xtExNjB2Nd88US=> NXLScGh3OjJzNUm4NVQ>
SNU-620 MlnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HhOFczcA>? NULTUW42TE2VTx?= M{nxZWlEPTB;Mj65N|nDuTBwMECx{txO MoPxNlIyPTl6MUS=
SNU-719 MonwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXQb5I4Omh? NX[0c5dZTE2VTx?= NGjhUVRKSzVyPUOuNFM4yrFyLkCzNu69VQ>? MnX0NlIyPTl6MUS=
glioma cell lines MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjsRmRLPzKq M{HjXmlEPTB;MT2y{txO M2GxR|IzODZ3MEiw
U87 NFOwb2hCeG:ydH;zbZMhSXO|YYm= MoXuNu69VQ>? M2D0flczcA>? M2O2Wolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiYX7kJINt\WG4ZXSgVGFTWCCjbnSgZ4F{eGG|ZT2z M1f4flIzODZ3MEiw

... 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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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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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID