BKM120 (NVP-BKM120, Buparlisib) 化学構造
分子量: 410.39

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Quality Control & MSDS

製品説明

  • Compare PI3K Inhibitors
    PI3K製品生物活性の比較
  • 研究分野
  • BKM120 (NVP-BKM120, Buparlisib)のメカニズム

製品の説明

生物活性

製品説明 BKM120 (NVP-BKM120, Buparlisib)は、p110α、p110β、p110δとp110γの選択的なPI3K阻害剤で、IC50 がそれぞれ 52-99 nM、166 nM、 116 nM、 262 nMです。
ターゲット p110α p110β p110δ p110γ
IC50 52-99 nM 166 nM 116 nM 262 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MCF7 NF75WVNEgXSxdH;4bYMhSXO|YYm= NUf0NYpGPzJiaB?= MUjEUXNQ M2O4PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFiRUW0OWshdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFE2QCEQvF2= M{HaZVI1QTByMk[2
DU145 MY\DfZRwfG:6aXOgRZN{[Xl? MoW4O|IhcA>? MYTEUXNQ NVP6NpZjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN MmTINlQ6ODB{Nk[=
A2780 NXHpUIdHS3m2b4TvfIlkKEG|c3H5 MmPpO|IhcA>? NV3IepF[TE2VTx?= MkDsR5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlM2KM7:TR?= MWCyOFkxODJ4Nh?=
U87MG NHPsRoFEgXSxdH;4bYMhSXO|YYm= M1:0eFczKGh? M{DKemROW09? Mle1R5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlk5KM7:TR?= NV7GV3h2OjR7MECyOlY>
A2780 NHXnR2pHfW6ldHnvckBCe3OjeR?= M3HQVFEhcA>? Ml3MSG1UVw>? NWLHboNpUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlA2PSEQvF2= Ml;wNlQ6ODB{Nk[=
DU145 MkKySpVv[3Srb36gRZN{[Xl? M3vGV|EhcA>? M13sfWROW09? M3nNO2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBFXTF2NTDj[YxteyCqYYLic5JqdmdiTFvCNUBufXSjdHnvckB4cXSqIFXDOVAhd2ZiMD6wO|Mh|ryP M4TEZVI1QTByMk[2
A2780 MY\GeY5kfGmxbjDBd5NigQ>? NULoT2NHOSCq NYjUN4RkTE2VTx?= NWH0[lBEUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2= NWfQOmhHOjR7MECyOlY>
MCF7 NWLhPZdUTnWwY4Tpc44hSXO|YYm= NWHIXYx[OSCq Mmi2SG1UVw>? MVHJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCHNUS1T{BufXSjboStcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMTFOwG0> M3jj[VI1QTByMk[2
U87MG NYHne4xyTnWwY4Tpc44hSXO|YYm= NHHHN3cyKGh? NFG1d3lFVVOR NYXBcGN[UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJHU5P02JIHPlcIx{KHerdHigSWM2OCCxZjCwMlE{KM7:TR?= NHv3dIwzPDlyMEK2Oi=>
A2780 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz0Z5F2PzJiaB?= NH73NmtFVVOR NUKwdVN7TUN3ME2wMlUzKM7:TR?= NXi3N5N6OjR7MECyOlY>
SKMES-1 M2DrfGN6fG:2b4jpZ{BCe3OjeR?= M3v6flEh|ryP MUi3NkBp MYPJcoR2[2W|IHPlcIwh\GWjdHi= MXeyOlAyOzNzOB?=
H596 MlrXSpVv[3Srb36gRZN{[Xl? NIGwTVUyKM7:TR?= MYjJcZBicXK|IHPlcIwhdWmpcnH0bY9v MUCyOlAyOzNzOB?=
HCC2450 MVfGeY5kfGmxbjDBd5NigQ>? MnXkNUDPxE1? Ml:1TY1x[Wm{czDj[YxtKGmwdnHzbY9v M4TNTFI3ODF|M{G4
A549 MWjGeY5kfGmxbjDBd5NigQ>? MYS1NFAhdk1? MlftOFghcA>? NGjxVpZFVVOR NVfINW11UW6qaXLpeJMhSWu2IHHjeIl3[XSrb36= M3uzZlI2QTN5Mkm5
A549 M{mxcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X6dVEh|ryP MXS3NkBp M3zZNGROW09? M13WcWlvcGmkaYTzJINmdGxiZ4Lve5Rp MV:yOVk{PzJ7OR?=
H522 M2jUeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfwSWR5OSEQvF2= M4\YUlczKGh? M4nRZWROW09? MX\Jcohq[mm2czDj[YxtKGe{b4f0bC=> MX[yOVk{PzJ7OR?=
LNCaP MUjGeY5kfGmxbjDBd5NigQ>? NHjXWYgyKM7:TR?= NEXmZmNUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?= MXyyOVM3ODd7OR?=
LNCaP95 NH7KTnBHfW6ldHnvckBCe3OjeR?= MoTCNUDPxE1? NYD6SoxNW3WycILld5NmeyCyLVHLWEBt\X[nbIO= NEXweXczPTN4MEe5PS=>
HCT-15 NYmzUIR6SXCxdH;zbZMhSXO|YYm= M13NfVExKM7:TR?= NULrdWtKPDhiaB?= MnfGSG1UVw>? MWfJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MnvUNlUyPTJ{NEW=
HCT-116 NXnsOZlFSXCxdH;zbZMhSXO|YYm= MVmxNEDPxE1? MXK0PEBp Mnn6SG1UVw>? MnHmTY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUGxOkBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MUOyOVE2OjJ2NR?=
NCI-H460 NInteJlCeG:2b4Ppd{BCe3OjeR?= MV:xNEDPxE1? NFLzfmE1QCCq M{nNNGROW09? NYT4Om5VUW6mdXPld{BieG:ydH;zbZMhcW5iTlPJMWg1PjBiY3XscJMhcGG{Yn;1dolv\yCSSVuzR2EhcG:2c4DveEBufXSjdHnvci=> MWCyOVE2OjJ2NR?=
SKOV-3 NFnicJpCeG:2b4Ppd{BCe3OjeR?= MnLhNVAh|ryP NFvMXVI1QCCq NXLQNZNvTE2VTx?= NVnWdm5TUW6mdXPld{BieG:ydH;zbZMhcW5iU1vPWk0{KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NGTUOZQzPTF3MkK0OS=>
BSY-1 NUfBbWlPSXCxdH;zbZMhSXO|YYm= NWjtUnNiOTBizszN M4O0VlQ5KGh? M4Ptc2ROW09? NV\3e29EUW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= MYGyOVE2OjJ2NR?=
MKN-1 M2PaO2Fxd3Sxc3nzJGF{e2G7 MVexNEDPxE1? M3TlN|Q5KGh? NWW3dZVFTE2VTx?= NG\N[VFKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NV\IXnllOjVzNUKyOFU>
NCI-H522 NHXGSZRCeG:2b4Ppd{BCe3OjeR?= NF7DRVcyOCEQvF2= Mn;hOFghcA>? NITGVopFVVOR Mkn3TY5lfWOnczDhdI9xfG:|aYO= M2jMelI2OTV{MkS1
OVCAR-3 NGjC[GRCeG:2b4Ppd{BCe3OjeR?= NE\lfoQyOCEQvF2= M1XIcVQ5KGh? NH\xR4RFVVOR M3G5XWlv\HWlZYOgZZBweHSxc3nz MUmyOVE2OjJ2NR?=
HBC-5 MmnBRZBwfG:|aYOgRZN{[Xl? NWH1ToVHOTBizszN MVO0PEBp MkX5SG1UVw>? NV;1eFV3UW6mdXPld{BieG:ydH;zbZM> NXjGSZF6OjVzNUKyOFU>
RXF-631L NYCzNmlPSXCxdH;zbZMhSXO|YYm= MofWNVAh|ryP NYH5S3BsPDhiaB?= MmD3SG1UVw>? NInVU4ZKdmS3Y3XzJIFxd3C2b4Ppdy=> MYOyOVE2OjJ2NR?=
MKN-45 NEe3W4xCeG:2b4Ppd{BCe3OjeR?= MX6xNEDPxE1? NF[0UY81QCCq M1HiemROW09? NHnD[nlKdmS3Y3XzJIFxd3C2b4Ppdy=> M1ThRlI2OTV{MkS1
BON-1 M37jVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYq1NFAhdk1? MXqxNEBl MUnEUXNQ NUTSeWZEUW6qaXLpeJMh[2WubDDndo94fGh? NYPU[mxPOjVyMk[yPVI>
BON-1 MlLxSpVv[3Srb36gRZN{[Xl? M33JS|UxOCCwTR?= MWO0JIg> M3PrTmROW09? NFvXcGpKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez MX2yOVAzPjJ7Mh?=
QGP-1 MoDjSpVv[3Srb36gRZN{[Xl? MmTnOVAxKG6P NYi4ZXF2PCCq MUfEUXNQ MVPJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| MWmyOVAzPjJ7Mh?=
Huh7 MonhSpVv[3Srb36gRZN{[Xl? MlnUNUDPxE1? M3nOelEhcA>? NXT2bItKTE2VTx?= NHnIUI1KdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHNmejR5NB?= MWmyOVAxPDRyMx?=
BNL MXjGeY5kfGmxbjDBd5NigQ>? NYnKcI1TOSEQvF2= M4H2eFEhcA>? MWXEUXNQ M{jsc2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>? MWGyOVAxPDRyMx?=
MDA-MB-175 NV73bI5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfvcGcyKM7:TR?= M1HwcVUh\A>? M2PTT2ROW09? NXzBVW5IUUN3MEyxJO69VQ>? MYmyOFg4QTd7Nh?=
MDA-MB-134 NVPpXFBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULyRppFOSEQvF2= NFLlVpg2KGR? Mn3CSG1UVw>? MVfJR|UxRDFizszN M{C0fVI1QDd7N{m2
HCC1500 M{S3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\SNUDPxE1? NFLKb4E2KGR? M2nJVmROW09? M4fMUGlEPTB:MTFOwG0> MmDvNlQ5Pzl5OU[=
EFM-19 MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXqWmR7OSEQvF2= NEDMNHI2KGR? NVf0O3h1TE2VTx?= Mo[1TWM2ODxzIN88US=> Mof0NlQ5Pzl5OU[=
ZR-75-30 MlPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKxJO69VQ>? MVW1JIQ> M17jR2ROW09? NWrEdoF2UUN3MEyxJO69VQ>? NVHCTG1KOjR6N{m3PVY>
MDA-MB-361 M3z2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[xJO69VQ>? M1;NeVUh\A>? NFfJSWNFVVOR NILlS|JKSzVyPEGg{txO NYnmUmoyOjR6N{m3PVY>
T-47D MluwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[xJO69VQ>? MkjkOUBl MmTrSG1UVw>? M4nB[2lEPTB:MTFOwG0> NUO2eYpCOjR6N{m3PVY>
SK-BR-3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGxJO69VQ>? MlfmOUBl NH70PYhFVVOR NWjrXpcxUUN3MEyxJO69VQ>? NYXGR|dbOjR6N{m3PVY>
UACC-732 MlzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUixJO69VQ>? MY[1JIQ> NE\kcWhFVVOR NXLpboFFUUN3MEyxJO69VQ>? NWi2fnJvOjR6N{m3PVY>
BT-474 NWr0W5NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOxJO69VQ>? MkDZOUBl MXXEUXNQ MnmwTWM2ODxzIN88US=> M1;1elI1QDd7N{m2
HCC202 NU\5PXJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfwSZA5OSEQvF2= MYO1JIQ> M{XWRmROW09? M2fCU2lEPTB:MTFOwG0> M2jTOVI1QDd7N{m2
MCF7 NIjnXW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPDd4pQOSEQvF2= MnjZOUBl NWXxOI1KTE2VTx?= MlrCTWM2ODxzIN88US=> MoPENlQ5Pzl5OU[=
MDA-MB-415 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK4NUDPxE1? NFi1PVY2KGR? M2[yOGROW09? NX;pXoJOUUN3MEyxJO69VQ>? MUOyOFg4QTd7Nh?=
MDA-MB-453 M1Xa[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn5NUDPxE1? M1vTbVUh\A>? MnntSG1UVw>? MonRTWM2ODxzIN88US=> MoTHNlQ5Pzl5OU[=
ZR-75-1 NFjVWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHrNUDPxE1? NF;jVVY2KGR? MnHISG1UVw>? MVnJR|UxRDFizszN Ml7iNlQ5Pzl5OU[=
HCC38 NV;TcolNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7oN4JZOSEQvF2= MWS1JIQ> NYP4WGk1TE2VTx?= MVTJR|UxRDFizszN NV7U[G1IOjR6N{m3PVY>
HCC1419 NHzMemZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;2NUDPxE1? MYe1JIQ> M1TV[mROW09? NIP1OJFKSzVyPEGg{txO M1P4e|I1QDd7N{m2
UACC-812 M{C1fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml6wNUDPxE1? MW[1JIQ> M{ToR2ROW09? M3nqbmlEPTB:MTFOwG0> M2LFXFI1QDd7N{m2
HCC1187 NWLuU|VDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrU[XpqOSEQvF2= Ml3TOUBl MXzEUXNQ NEP3fJNKSzVyPEGg{txO NXvMRoM2OjR6N{m3PVY>
KPL-1 M3[3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP1NUDPxE1? MWW1JIQ> MULEUXNQ Ml3LTWM2ODxzIN88US=> MVSyOFg4QTd7Nh?=
SUM-225 NVz1XYdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2xJO69VQ>? NVrzU4pJPSCm MYHEUXNQ M1HTOWlEPTB:MTFOwG0> NYDHNFJbOjR6N{m3PVY>
EFM-192A NGTHWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjUNUDPxE1? NXLy[2hFPSCm NFLQcG9FVVOR NUXScYlHUUN3MEyxJO69VQ>? MVmyOFg4QTd7Nh?=
JIMT-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DSPFEh|ryP NV7qfmM6PSCm NXqyN3hrTE2VTx?= MkLvTWM2ODxzIN88US=> NF7BbIMzPDh5OUe5Oi=>
HCC1143 NIDwSnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmxJO69VQ>? Mm[1OUBl MmqxSG1UVw>? M3j1NWlEPTB:MTFOwG0> MXKyOFg4QTd7Nh?=
HCC2218 NWja[2JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPhNUDPxE1? M4nMUFUh\A>? M3XBcWROW09? MYTJR|UxRDFizszN M3e2VFI1QDd7N{m2
MDA-MB-468 NH\JRZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDCc|FOOSEQvF2= NGflXlM2KGR? NI\KdZVFVVOR NXL2e2ZQUUN3MEyxJO69VQ>? NUHLdVJjOjR6N{m3PVY>
BT-20 NIXHblRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDZ[|YyKM7:TR?= Mnv3OUBl M3PibGROW09? M1zDemlEPTB:MTFOwG0> NIX0SWMzPDh5OUe5Oi=>
MDA-MB-435 Moq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrNZZUzOSEQvF2= Ml\1OUBl M4\5WGROW09? MUTJR|UxRDFizszN NX35cItjOjR6N{m3PVY>
BT-549 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjLRocyKM7:TR?= NFv2XZI2KGR? NFLwXIxFVVOR NV[zRnhnUUN3MEyxJO69VQ>? NVzVWJplOjR6N{m3PVY>
HCC1806 MmTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TGdFEh|ryP M1KzeVUh\A>? NWLzcI97TE2VTx?= NEn6epFKSzVyPEGg{txO MXmyOFg4QTd7Nh?=
HCC1937 M3Kzc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmxJO69VQ>? MUS1JIQ> MonISG1UVw>? NHHDWnBKSzVyPEGg{txO MY[yOFg4QTd7Nh?=
Hs578T NUPCT2ltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\xSIEyKM7:TR?= MW[1JIQ> NIDXbINFVVOR MV3JR|UxRDFizszN Ml7kNlQ5Pzl5OU[=
LN18 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\vNlAh|ryP Ml3zO|IhcA>? MmnuSG1UVw>? MkL5TWM2ODx3IN88US=> NWT2Ro54OjR5NEGwO|Q>
LN229 MoX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWqyNEDPxE1? MV63NkBp MlHoSG1UVw>? MWDJR|UxRDVizszN MoTsNlQ4PDFyN{S=
LNZ308 NE\5e5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXKepFiOjBizszN Mn3HO|IhcA>? M3LyOWROW09? NUDyUZpZUUN3MEy1JO69VQ>? NIfGPWUzPDd2MUC3OC=>
T98G NGrnU2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\nemNuOjBizszN NVPTSoxmPzJiaB?= M3TYNGROW09? MlTUTWM2ODx3IN88US=> MY[yOFc1OTB5NB?=
U87 M1ToOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjIWWwzOCEQvF2= M3vWPFczKGh? MoX2SG1UVw>? Mle4TWM2ODx3IN88US=> NH7YUWQzPDd2MUC3OC=>
LN18 MVfGeY5kfGmxbjDBd5NigQ>? NYnq[HgxPSEQvF2= MlPaNlQhcA>? Mn7nSG1UVw>? NIHyTIVKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuW MmXyNlQ4PDFyN{S=
LNZ308 NWn4VGlZTnWwY4Tpc44hSXO|YYm= MXS1JO69VQ>? MVGyOEBp MoLRSG1UVw>? NX7TTY5kUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NFjHSZkzPDd2MUC3OC=>
Saos-2 M2XUTmZ2dmO2aX;uJGF{e2G7 NF2wb5A2OCEQvF2= NV7GOGVNPDhiaB?= MUfJcohq[mm2czDj[YxtKGmwdnHzbY9v NVzGXlY3OjR5Mke2OlA>
MG-63 MX7GeY5kfGmxbjDBd5NigQ>? M3fCVVUxKM7:TR?= M3HNVFQ5KGh? M2XxcGlvcGmkaYTzJINmdGxiaX72ZZNqd25? NUTxfXplOjR5Mke2OlA>
SJSA-1 MlmwSpVv[3Srb36gRZN{[Xl? MW[1NEDPxE1? NEXpSlE1QCCq NF61flRKdmirYnn0d{Bk\WyuIHnueoF{cW:w MVeyOFczPzZ4MB?=
Saos-2 MmfNSpVv[3Srb36gRZN{[Xl? NELrNYc2OCEQvF2= M{T2blQ5KGh? MnPLTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> Mki4NlQ4Ojd4NkC=
MG-63 M4LKO2Z2dmO2aX;uJGF{e2G7 NFXsUGk2OCEQvF2= M4PYb|Q5KGh? M2ThPGlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MViyOFczPzZ4MB?=
SJSA-1 MYXGeY5kfGmxbjDBd5NigQ>? NFPMWJY2OCEQvF2= M4LzVlQ5KGh? NEHvS5VKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v M1HsV|I1PzJ5Nk[w
Saos-2 NXO3XY8yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof1OVAh|ryP MV[0PEBp NGj1PWNKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MX:yOFczPzZ4MB?=
MG-63 MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\Hdmo2OCEQvF2= M4TnOFQ5KGh? M2m4cGlvcGmkaYTzJINmdGxidnnhZoltcXS7 NIDpNFYzPDd{N{[2NC=>
SJSA-1 NU\nOlBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXQeHRjPTBizszN NIXtboY1QCCq NIL1UJdKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NHnQN3YzPDd{N{[2NC=>
FaDu MoLWSpVv[3Srb36gRZN{[Xl? M2Hh[lUh|ryP NIXkSGwzPCCq NI\seHNFVVOR MknUVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= NHn4[ZkzPDZ|MUG0Oy=>
EMT6 MVHGeY5kfGmxbjDBd5NigQ>? M{HkdlUh|ryP NUPNS|NLOjRiaB?= NHLqN5dFVVOR MX7S[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NHLRTpMzPDZ|MUG0Oy=>
HCT116 NYnnTpI4TnWwY4Tpc44hSXO|YYm= M3fSPFUh|ryP MXOyOEBp MXTEUXNQ NYr6ZYdxWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NFi5VngzPDZ|MUG0Oy=>
U87 NIH1THdHfW6ldHnvckBCe3OjeR?= Mn3uOUDPxE1? NVH5e2k6OjRiaB?= MlXZSG1UVw>? NXXiOYJ6WmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> Mkn0NlQ3OzFzNEe=
GBM MWHBdI9xfG:|aYOgRZN{[Xl? MU[y{txO MXu0PIg> MonMSG1UVw>? Mn3UbY5lfWOnZDDobYdp\XJibHX2[Yx{KG:oIHHwc5B1d3OrczygZY5lKGSnY4LlZZNm\CClZXzsJJZq[WKrbHn0fS=> Mn\JNlQ2ODB2OUK=
BON M3vV[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TPTFEuPc7:TR?= Mlv4O|Jp M{jLcYRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NFvQXpYzPDR2M{WyNy=>
BON MXPBdI9xfG:|aYOgRZN{[Xl? NInwSJAyNTYQvF2= Mlz2NlRp M4PweYlv[3KnYYPld{BieG:ydH;zbZM> MUKyOFQ1OzV{Mx?=
H1975 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjoNE4{NTlwNt88US=> MWC3Nog> NEDIVJlFVVOR M1XZTWlEPTB;MT6zPFXPxE1? NXW2WoxNOjR|M{e4OFY>
H1975 NEWzTm5CeG:ydH;zbZMhSXO|YYm= NVLEXFJNOs7:TR?= M3P3TVI1cA>? NUTvNG9FTE2VTx?= M{fGVYlv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6 Ml\ENlQ{Ozd6NE[=
T-ALL MmnrRZBweHSxc3nzJGF{e2G7 M4jpbIJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= NWOzOJFjOjRib4KgOFhp NULzOnFOTE2VTx?= NF\3cHpi\m[nY4TzJJRp\SCSSUPLJJBifGi5YYmgbY4hXC2DTFygZ4VtdCCuaX7ldy=> NYe3dHJuOjR|MUC3N|Y>
BCR-ABL M3;BUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvL[mUxNjJ3LUGw{txO MkLwOIQ> NF;qOHF{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w MVOyOFI1PDZzMh?=
LC-1/SQSF M{TrU2Z2dmO2aX;uJGF{e2G7 Mo\qN:69VQ>? NXzh[2p{OjSq MkHESG1UVw>? NH7m[45l\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw> Ml3kNlM6QDByOUO=
Primary CLL cells NV\vNpNzSXCxcITvd4l{KEG|c3H5 MWixMVEx|ryP Mmn3OFhp NV7r[JFDcW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>? MkPjNlM5PTB6MEe=
Primary CLL cells M4DXU2tqdmG|ZTDBd5NigQ>? MoDENu69VQ>? NWLlTHdmOzCvaX6= Mont[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? NIDp[48zOzh3MEiwOy=>
Primary CLL cells NW\FRWtwS3m2b4TvfIlkKEG|c3H5 MofzNu69VQ>? MoSwNlRp M4TsfIlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= NIe2fGMzOzh3MEiwOy=>
human NSCLC cell lines MWnBdI9xfG:|aYOgRZN{[Xl? NF61OoIxNjF{NT20{txO NVP6T29mOjSq NUPKN3R5TE2VTx?= Mo[zTWM2OHNicnHu[4V{KG[{b32gNE41NTMQvF2= MmHQNlM2PjJ2N{K=
human HCC cell lines NF\kdYZE\WyuII\pZYJqdGm2eTDhd5NigQ>? M2LQV|AvODB3LUJOwG0> NXzscZVIPDiq MVfJR|UxRTIQvF2= MXeyN|Q5QTl7OR?=
Huh7 NWTQS2dDU2mwYYPlJGF{e2G7 MVix{txO NV30N4J{PDiq M{XlZZNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MUiyN|Q5QTl7OR?=
SK-HEP1 NYT1fIZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vjWVEuOjEQvF2= M33zZlczcA>? NEjtSYdFVVOR NVzadFc3UUN3MP-8oFHPxE1? NILqTIszOzR5OUGzOi=>
786-0 NXTiV5lsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGxMVIx|ryP NVP4[nE3PzKq MmPaSG1UVw>? M3\JZ2lEPTExvKyx{txO NXfLRXppOjN2N{mxN|Y>
JVM2 MWLDfZRwfG:6aXPpeJkh[XO|YYm= MXiwMlIuOjEQvF2= NYnLelB7PzKq NYn4S413TE2VTx?= MmPLTWM2OD1yLkpOwG0> M{PZPFI{OjN6NkO5
EHEB MYrDfZRwfG:6aXPpeJkh[XO|YYm= M4Dmc|AvOi1{MN88US=> NHvHS3A4Omh? MmHESG1UVw>? MkTtTWM2OD1yLkhOwG0> NFfQcIMzOzJ|OE[zPS=>
MEC2 MnzXR5l1d3SxeHnjbZR6KGG|c3H5 M{TEXVAvOi1{MN88US=> M3HOUlczcA>? M1Lpc2ROW09? NHi1boxKSzVyPUCuO:69VQ>? M32y[VI{OjN6NkO5
primary B-CLL lymphocytes MULBdI9xfG:|aYOgRZN{[Xl? NFzDXpNKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n MXiyOIg> NXXZXm0xTE2VTx?= Mk\yTWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> MmDDNlMzOzh4M{m=
primary B-CLL lymphocytes Mkn2T4lv[XOnIFHzd4F6 M1\LUmlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? M4fIelI1cA>? Ml7IbY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36= NXq1UnVyOjN{M{i2N|k>
human NSCLC M3jRT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\nNE42NTMQvF2= M2nlVVczcA>? NEOwbZZKSzVyPUJOwG0> NVPoUpI{OjJ5OEGzPVM>
human NSCLC MYHLbY5ie2ViQYPzZZk> NFzyZYUy|ryP M{PvPFI1cA>? M3\TfIlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= NYqzZnlnOjJ5OEGzPVM>
Y1 cell line MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;HdFcxNjIQvF2vNe69VQ>? NUT4OXlrOjSq NFPRN|lFVVOR MmTVbY5pcWKrdIOgOlDwxIViY3XscEB3cWGkaXzpeJkhcW5iTYnjMXNkfHJvdILhcpNn\WO2ZXSgZ4VtdHN? NWPLOlBLOjJ4OUK5NFQ>
PIK3CA-mutant MCF7 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? M3WyTVczcA>? M3zk[mdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P M4WwbVIzPjV|OU[3
PIK3CA-mutant MCF7 MnjxT4lv[XOnIFHzd4F6 NUn4WpY1UUN3ME2xNVTDuTOwTR?= NV25cYd6PzKq MXHJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| NWDRZYc6OjJ4NUO5Olc>
MCF7-myr-Akt NH;JZXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2f0fGdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P MVi3Nog> NUO1TVFET0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= M1n2OFIzPjV|OU[3
colon cancer cell lines NGfPNVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfXNE0yOM7:TR?= MlfsO|Jp NGfRO4RFVVOR MX7JR|UxRTIQvF2= Ml\pNlI2PDN6NUe=
gastric cancer cell lines M33XWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3mNE0yOM7:TR?= NXSyR|RMPzKq NEXYfZdFVVOR MXvJR|UxRTJvNd88US=> M4jwc|IzPTR|OEW3
HCT-116/HT-29/MKN-45 NGDiW3pCeG:ydH;zbZMhSXO|YYm= NInT[poz|ryP MVu0PIg> NW\Ndm01e2irZoSgbY4hTzJicHjhd4U> MXuyNlU1Ozh3Nx?=
HT-29 and HCT-116 NGf6V21E[XOyYYPlJIF{e2G7 NH;wdVQ2|ryP NWfGeHhHOjSq NV7OSmJFcW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5 Moi1NlI2PDN6NUe=
MM cell lines M1XJNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUixNO69VQ>? M1e3NFI1cA>? NIDFSnJFVVOR MmC1TWM2OCC4YYLp[ZMh[W2xbneg[Iln\mW{ZX70JINmdGxibHnu[ZMhcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcoNm NIL2WZozOjJyN{S4OS=>
ARP-1 MVfBdI9xfG:|aYOgRZN{[Xl? NYPkV|RVOTEQvF2= Mn3XNlRp NEK2TWVFVVOR Mnu1bY5lfWOnczDNUUBk\WyuIHHwc5B1d3OrczD0bJJwfWeqIHPhd5Bie2ViYXP0bZZifGmxbh?= MlHuNlIzODd2OEW=
SNU-601 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXezWVRuPzKq MUTEUXNQ Ml;aTWM2OD1yLkixOuKyOC5yNkROwG0> MYmyNlE2QThzNB?=
SNU-1 M4nXbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV6xS4hwPzKq Mn3ZSG1UVw>? M37yfWlEPTB;MT6wPFLDuTBwMEK4{txO NG\je|czOjF3OUixOC=>
SNU-668 M4fJR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Twb|czcA>? NFSyfpJFVVOR Mmi1TWM2OD1zLkW3PeKyOC5yN{VOwG0> MXSyNlE2QThzNB?=
AGS M3izO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[wNlM4Omh? MUDEUXNQ MV7JR|UxRTFwN{G0xtExNjFzN988US=> MUeyNlE2QThzNB?=
SNU-216 NFu0SW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;G[lczcA>? NYLZd5lWTE2VTx?= M332[mlEPTB;Mj62PVLDuTBwMEiy{txO MmLYNlIyPTl6MUS=
SNU-5 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\5XVczcA>? M4ixV2ROW09? MYXJR|UxRTFwM{WxxtExNjB7Md88US=> NFTtSmwzOjF3OUixOC=>
SNU-638 NUGxVlNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWq3Nog> M3LHU2ROW09? NUnr[YdGUUN3ME2yMlI5OsLzMD6wOVPPxE1? MnG0NlIyPTl6MUS=
SNU-16 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO2O|Jp NX;ibVc4TE2VTx?= NVzqZ2Q4UUN3ME2xMlU4O8LzMD6wNFHPxE1? MkjtNlIyPTl6MUS=
SNU-484 NXXQb4lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrBO|Jp NHjjUIFFVVOR MWDJR|UxRTFwN{K4xtExNjB2Nd88US=> MVuyNlE2QThzNB?=
SNU-620 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3GO|Jp MWLEUXNQ NFWwNFFKSzVyPUKuPVM6yrFyLkCwNe69VQ>? MXSyNlE2QThzNB?=
SNU-719 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jufVczcA>? M{fZdWROW09? MWHJR|UxRTNwMEO3xtExNjB|Mt88US=> M4XPWFIzOTV7OEG0
glioma cell lines MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUf5[GxkPzKq M1;XeWlEPTB;MT2y{txO NH7zVIczOjB4NUC4NC=>
U87 Ml[2RZBweHSxc3nzJGF{e2G7 MVSy{txO MUi3Nog> MXPpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?= MnLONlIxPjVyOEC=

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Current under Phase II in men with metastatic castration-resistant prostate cancer.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.
PI3K biochemical assay (filter binding assay) 50 µL/well of a 1:1 mixture of 100 µL/mL L-α-phosphatidylinositol and L-α-phosphatidylserine dissolved in chloroform:ethanol (2.2:7.8) is pipetted into 96-well MaxiSorpTM plates. The solvents are evaporated at room temperature and plates are wa

細胞アッセイ: [1]

細胞株 A2780 cells.
濃度 0-6.6 μM
反応時間 3 days.
実験の流れ 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.

動物実験: [1]

動物モデル U87MG and A2780 xenografts are established in female nu/nu mice.
製剤 In 15% Captisol.
投薬量 ~60 mg/kg.
投与方法 Dosed orally daily (q.d.).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download BKM120 (NVP-BKM120, Buparlisib) SDF
分子量 410.39
化学式

C18H21F3N6O2

CAS No. 944396-07-0
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 82 mg/mL (199.8 mM)
エタノール 2 mg/mL (4.87 mM)
<1 mg/mL (<1 mM)
In vivo 0.5% CMC Na 6 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine

カスタマーフィードバック (3)


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Rating
Source Dr. Zhang of Tianjin Medical University. BKM120 (NVP-BKM120, Buparlisib) purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-10 μM
Incubation Time 3 h
Results BKM120 treatment resulted in a reduction of Akt-308 phosphorylation in A549 cells.

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Rating
Source One customer. BKM120 (NVP-BKM120, Buparlisib) purchased from Selleck
Method Cell growth inhibition assay
Cell Lines Melanoma cell lines
Concentrations 0.00000512-10 μM
Incubation Time 72 h
Results BKM120 treatment inhibited Melanoma cells growth in a does-dependent manner.

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Rating
Source Dr. Pilar Eroles of INCLIVA Biomedical Research Institute.. BKM120 (NVP-BKM120, Buparlisib) purchased from Selleck
Method MTT assay
Cell Lines JIMT-1 cells
Concentrations 1-1000 nM
Incubation Time 48 h
Results JIMT-1 cells were seeded in 96 well plates (8x10<SUP>3</SUP>cells per well) andtreated with medium containing DMSO as a control and inhibitor BKM-120 (1nM, 5nM, 10nM, 50nM, 100nM, 500nM, 1000nM). Cell growth was measured after 48 hours by MTT assay.Results are expressed as a percent over DMSO control.

文献中の引用 (34)

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    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • GNE-317

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • PI-3065

    PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.

  • LY294002

    LY294002は、p110α、p110δとp110βのPI3K阻害剤で、IC50 がそれぞれ 0.5 μM、0.57 μM、0.97 μMです。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) は選択の自噬とリン酸イノシトール3キナーゼ(キナーゼ)阻害剤、Vps34 と PI3Kγ に作用する時、 IC50 がそれぞれ 25 nM と 60 nM になる。自動食物胞の形成を妨害すること。

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101)は、2.5nMのIC50によるp110δの選択的なPI3KクラスI阻害剤です。

  • Wortmannin

    ワートマニンはミオシン軽鎖キナーゼ(MLCK)のマルチターゲットの阻害剤、IC50がぞれぞれ0.17μMと3nMになる。自動食物胞の形成を妨害すること。

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235, Dactolisib)は競争性的なPI3K、mTOR 阻害剤、 p110α, p110γ, p110δ と p110β を作用すると、 IC50 がぞれぞれ 4 nM, 5 nM, 7 nM と 75 nMになる.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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