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 M2XD[WN6fG:2b4jpZ{BCe3OjeR?= M3Ow[FczKGh? M3LiTmROW09? MlTzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?= NVvnPVFbOjR7MECyOlY>
DU145 M1vLOWN6fG:2b4jpZ{BCe3OjeR?= NV7HdJlEPzJiaB?= NWnIWoNjTE2VTx?= NUPpeZhWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN M1PPeVI1QTByMk[2
A2780 NIDmVWtEgXSxdH;4bYMhSXO|YYm= MnTnO|IhcA>? NWf0PIFHTE2VTx?= M4LodGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2= NYT6T2szOjR7MECyOlY>
U87MG NX[3V5c{S3m2b4TvfIlkKEG|c3H5 MoXJO|IhcA>? MV;EUXNQ MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh|ryP NYP1T2RrOjR7MECyOlY>
A2780 MlHVSpVv[3Srb36gRZN{[Xl? MWSxJIg> NGTuWVFFVVOR M1XzRmlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6wOVUh|ryP MoqxNlQ6ODB{Nk[=
DU145 M3fnfGZ2dmO2aX;uJGF{e2G7 MkTZNUBp Mk\PSG1UVw>? MVHJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>? NFy2SmgzPDlyMEK2Oi=>
A2780 NFX6WndHfW6ldHnvckBCe3OjeR?= NWraWmNSOSCq NWDaWmdSTE2VTx?= NWr0do9XUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2= MX6yOFkxODJ4Nh?=
MCF7 MkjPSpVv[3Srb36gRZN{[Xl? MXOxJIg> MmqwSG1UVw>? NWnVSJdOUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh|ryP M1PVc|I1QTByMk[2
U87MG MYjGeY5kfGmxbjDBd5NigQ>? NXPodJNqOSCq NHK4fpNFVVOR MYXJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO MljQNlQ6ODB{Nk[=
A2780 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDHfW5xPzJiaB?= Ml3PSG1UVw>? NV;IfFJ6TUN3ME2wMlUzKM7:TR?= M3O3NlI1QTByMk[2
SKMES-1 M{P5NGN6fG:2b4jpZ{BCe3OjeR?= Mon5NUDPxE1? M3fnSVczKGh? MmjjTY5lfWOnczDj[YxtKGSnYYTo M3\Ne|I3ODF|M{G4
H596 NVXkW3hCTnWwY4Tpc44hSXO|YYm= M2fHT|Eh|ryP MoqzTY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>? MmG5NlYxOTN|MUi=
HCC2450 MUHGeY5kfGmxbjDBd5NigQ>? NVrCNG5kOSEQvF2= NEf1elZKdXCjaYLzJINmdGxiaX72ZZNqd25? MnLVNlYxOTN|MUi=
A549 NVrvT4FoTnWwY4Tpc44hSXO|YYm= MnL0OVAxKG6P NHvZUY41QCCq NEi5Xo1FVVOR NXyyXIdOUW6qaXLpeJMhSWu2IHHjeIl3[XSrb36= M1H6WVI2QTN5Mkm5
A549 NF;wS2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\uWWt{OSEQvF2= M1fm[FczKGh? M4PPO2ROW09? MlnBTY5pcWKrdIOgZ4VtdCCpcn;3eIg> MX6yOVk{PzJ7OR?=
H522 NEXlbIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvy[4IyKM7:TR?= M2DiWVczKGh? NHzYcXRFVVOR MW\Jcohq[mm2czDj[YxtKGe{b4f0bC=> M4qyVFI2QTN5Mkm5
LNCaP M4nzOGZ2dmO2aX;uJGF{e2G7 M3vnc|Eh|ryP MliyV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? MmnqNlU{PjB5OUm=
LNCaP95 NInweHZHfW6ldHnvckBCe3OjeR?= MXmxJO69VQ>? NV;KdpI3W3WycILld5NmeyCyLVHLWEBt\X[nbIO= NHrKO2wzPTN4MEe5PS=>
HCT-15 M1G4VWFxd3Sxc3nzJGF{e2G7 MlXHNVAh|ryP MnLBOFghcA>? M4nvNmROW09? M2nXTWlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xOUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MWWyOVE2OjJ2NR?=
HCT-116 MorkRZBwfG:|aYOgRZN{[Xl? MVuxNEDPxE1? M4rJeFQ5KGh? M{LCPWROW09? MnvyTY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUGxOkBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NYXvc5pTOjVzNUKyOFU>
NCI-H460 NV71UpdXSXCxdH;zbZMhSXO|YYm= NEfkZlQyOCEQvF2= NH[2Tpc1QCCq M2P2[mROW09? MlfZTY5lfWOnczDhdI9xfG:|aYOgbY4hVkOLLVi0OlAh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NUTKSmVFOjVzNUKyOFU>
SKOV-3 MmCwRZBwfG:|aYOgRZN{[Xl? NGLoSmgyOCEQvF2= NI\wPWQ1QCCq MVHEUXNQ MoP0TY5lfWOnczDhdI9xfG:|aYOgbY4hW0uRVj2zJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MV:yOVE2OjJ2NR?=
BSY-1 MmfsRZBwfG:|aYOgRZN{[Xl? M1zrTVExKM7:TR?= NILJe3M1QCCq NG[yRYlFVVOR NVnwfYFUUW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NHjiNogzPTF3MkK0OS=>
MKN-1 NWTibYxZSXCxdH;zbZMhSXO|YYm= NU\6S3hCOTBizszN NHv4UWs1QCCq NUfhZ2tkTE2VTx?= MYDJcoR2[2W|IHHwc5B1d3OrczDpckBOU05vMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NVTtO5dwOjVzNUKyOFU>
NCI-H522 M4nlSWFxd3Sxc3nzJGF{e2G7 Ml\nNVAh|ryP MnPVOFghcA>? NGTlfWdFVVOR M2rFO2lv\HWlZYOgZZBweHSxc3nz NFXZVIgzPTF3MkK0OS=>
OVCAR-3 M4TmSGFxd3Sxc3nzJGF{e2G7 NUKx[IlROTBizszN NEfVS3c1QCCq MY\EUXNQ MXXJcoR2[2W|IHHwc5B1d3Orcx?= MlP5NlUyPTJ{NEW=
HBC-5 MVnBdI91d3OrczDBd5NigQ>? MlvDNVAh|ryP MUm0PEBp NFrRVIxFVVOR MmnuTY5lfWOnczDhdI9xfG:|aYO= NImwZ5ozPTF3MkK0OS=>
RXF-631L MmTPRZBwfG:|aYOgRZN{[Xl? NITaR4UyOCEQvF2= MVy0PEBp MV\EUXNQ NFvncYlKdmS3Y3XzJIFxd3C2b4Ppdy=> MYGyOVE2OjJ2NR?=
MKN-45 NXKzbo1FSXCxdH;zbZMhSXO|YYm= M{f2blExKM7:TR?= NXTE[IFlPDhiaB?= MoTxSG1UVw>? NIjQVWZKdmS3Y3XzJIFxd3C2b4Ppdy=> NI\oXnkzPTF3MkK0OS=>
BON-1 NWq0OYg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH3OVAxKG6P MVixNEBl M4HBbmROW09? NHTEb|NKdmirYnn0d{Bk\WyuIHfyc5d1cA>? Mmf3NlUxOjZ{OUK=
BON-1 M4DQPGZ2dmO2aX;uJGF{e2G7 MVO1NFAhdk1? MX20JIg> MXvEUXNQ NHXJRnZKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez MXmyOVAzPjJ7Mh?=
QGP-1 NWG0S3NWTnWwY4Tpc44hSXO|YYm= NVHqb5EyPTByIH7N MX[0JIg> MXzEUXNQ NXfrSnZWUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> MVuyOVAzPjJ7Mh?=
Huh7 NF:zXWFHfW6ldHnvckBCe3OjeR?= NVzDVWhzOSEQvF2= MYSxJIg> NGq0ZWNFVVOR NX:2V5p5UW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S= NVHveog1OjVyMES0NFM>
BNL MYnGeY5kfGmxbjDBd5NigQ>? M4\WcFEh|ryP NHzD[mwyKGh? NXvTc4VNTE2VTx?= MY\Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Y> M1y0OVI2ODB2NECz
MDA-MB-175 M4m0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGxJO69VQ>? M1vWN|Uh\A>? Mkf2SG1UVw>? MljtTWM2ODxzIN88US=> M1rCc|I1QDd7N{m2
MDA-MB-134 NETFfVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHQNUDPxE1? NG\ZZVM2KGR? MUXEUXNQ Mn7ZTWM2ODxzIN88US=> M2TDWlI1QDd7N{m2
HCC1500 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTYWIlROSEQvF2= MXG1JIQ> NYHGNI1WTE2VTx?= MYrJR|UxRDFizszN NHfZe|UzPDh5OUe5Oi=>
EFM-19 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLFNUDPxE1? MlrnOUBl NFzRe3BFVVOR NYW5NXFrUUN3MEyxJO69VQ>? M3WxW|I1QDd7N{m2
ZR-75-30 M4PNS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[wNUDPxE1? NIjySVY2KGR? NELteYVFVVOR MXXJR|UxRDFizszN M{Gye|I1QDd7N{m2
MDA-MB-361 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XrUFEh|ryP M3rXPVUh\A>? NEi5eY1FVVOR NVvK[ZhRUUN3MEyxJO69VQ>? MoLnNlQ5Pzl5OU[=
T-47D MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX6xJO69VQ>? NIfqVXM2KGR? MX7EUXNQ MVjJR|UxRDFizszN NXr3OGViOjR6N{m3PVY>
SK-BR-3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPpcopvOSEQvF2= MX[1JIQ> MXLEUXNQ MmTZTWM2ODxzIN88US=> NXTofm1uOjR6N{m3PVY>
UACC-732 NUnZUJpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jBV|Eh|ryP NF62N|g2KGR? MYXEUXNQ NF7PUXZKSzVyPEGg{txO NVrtdWJIOjR6N{m3PVY>
BT-474 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxJO69VQ>? NIrxNow2KGR? MVPEUXNQ MXnJR|UxRDFizszN M4TTVlI1QDd7N{m2
HCC202 NV3vSolJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfl[plxOSEQvF2= M2W2OlUh\A>? MXXEUXNQ NVvjcHozUUN3MEyxJO69VQ>? MXuyOFg4QTd7Nh?=
MCF7 MnX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jIVlEh|ryP M4\yN|Uh\A>? MkLVSG1UVw>? NHnrempKSzVyPEGg{txO NYnRVXFSOjR6N{m3PVY>
MDA-MB-415 NWfFWIxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOxJO69VQ>? MmHOOUBl M4HIVWROW09? MUfJR|UxRDFizszN MVmyOFg4QTd7Nh?=
MDA-MB-453 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX60b2J[OSEQvF2= MorhOUBl NYrx[npnTE2VTx?= Ml3RTWM2ODxzIN88US=> NGe4TZMzPDh5OUe5Oi=>
ZR-75-1 NHW5SGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG4NUDPxE1? NEfRXFA2KGR? MWfEUXNQ MmD0TWM2ODxzIN88US=> MlfyNlQ5Pzl5OU[=
HCC38 NHSwZpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PWbVEh|ryP NFXQ[nQ2KGR? MXfEUXNQ MXrJR|UxRDFizszN MkDVNlQ5Pzl5OU[=
HCC1419 MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\EflEh|ryP MoTDOUBl M3\1dmROW09? M3nmcmlEPTB:MTFOwG0> MWiyOFg4QTd7Nh?=
UACC-812 NW[4RYluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSxJO69VQ>? NX7rSHQ{PSCm MX;EUXNQ M1zqOGlEPTB:MTFOwG0> NVzT[ZBwOjR6N{m3PVY>
HCC1187 MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnYOlg{OSEQvF2= Ml7XOUBl NYXTV25sTE2VTx?= Ml;rTWM2ODxzIN88US=> MXuyOFg4QTd7Nh?=
KPL-1 MkfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILDUG8yKM7:TR?= MY[1JIQ> NELtWZVFVVOR MmLOTWM2ODxzIN88US=> M{HpRVI1QDd7N{m2
SUM-225 MmLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;ZfWJ2OSEQvF2= NXHDdZdEPSCm NHL0fmlFVVOR Moj1TWM2ODxzIN88US=> NGO2dZIzPDh5OUe5Oi=>
EFM-192A NIPVV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LiXVEh|ryP MofMOUBl MUnEUXNQ M1LOUWlEPTB:MTFOwG0> Mn3mNlQ5Pzl5OU[=
JIMT-1 NF;5dnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHDe40yKM7:TR?= M1zTclUh\A>? NY\0XnhmTE2VTx?= M3O4WWlEPTB:MTFOwG0> NXTsOotuOjR6N{m3PVY>
HCC1143 NVj3UZN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnaNW8yKM7:TR?= MYO1JIQ> MXzEUXNQ NX7ubFlGUUN3MEyxJO69VQ>? M37WdVI1QDd7N{m2
HCC2218 M1uye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Wye|Eh|ryP M2LjSlUh\A>? M3HPRWROW09? MXHJR|UxRDFizszN M1vIPFI1QDd7N{m2
MDA-MB-468 NWH4WoNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[xJO69VQ>? MoGzOUBl MnvSSG1UVw>? MXvJR|UxRDFizszN MX2yOFg4QTd7Nh?=
BT-20 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn2SlIyKM7:TR?= NIK5clQ2KGR? MUfEUXNQ NHXXZ4tKSzVyPEGg{txO NYrkR3dmOjR6N{m3PVY>
MDA-MB-435 NFH2RplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PRdlEh|ryP MkHqOUBl NUnpNVJ{TE2VTx?= NVfZbYx5UUN3MEyxJO69VQ>? NHTINGwzPDh5OUe5Oi=>
BT-549 M{DaTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X2T|Eh|ryP M1W5XVUh\A>? MVfEUXNQ NV3xfoF[UUN3MEyxJO69VQ>? MWWyOFg4QTd7Nh?=
HCC1806 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zW[VEh|ryP NHu1NGw2KGR? MUHEUXNQ MX7JR|UxRDFizszN MoDuNlQ5Pzl5OU[=
HCC1937 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fDbVEh|ryP NXW5b4NHPSCm M1n0dGROW09? NEjUTWhKSzVyPEGg{txO MX[yOFg4QTd7Nh?=
Hs578T M4HVVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHvc4t5OSEQvF2= MorQOUBl M4LY[GROW09? MUDJR|UxRDFizszN MXyyOFg4QTd7Nh?=
LN18 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonCNlAh|ryP NH7oVoM4OiCq MUPEUXNQ M2qzPGlEPTB:NTFOwG0> MnizNlQ4PDFyN{S=
LN229 MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVqzSYFNOjBizszN M3ztPVczKGh? NX3FeppFTE2VTx?= MX\JR|UxRDVizszN NULheFVxOjR5NEGwO|Q>
LNZ308 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnyfJUzOCEQvF2= M4LmU|czKGh? NYDl[oFvTE2VTx?= MYXJR|UxRDVizszN MkHPNlQ4PDFyN{S=
T98G MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfCW|IzOCEQvF2= M3LSVFczKGh? NILwR2RFVVOR MV3JR|UxRDVizszN M2DFbVI1PzRzMEe0
U87 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTONlAh|ryP MVe3NkBp MUnEUXNQ MlXwTWM2ODx3IN88US=> NVu5W|BCOjR5NEGwO|Q>
LN18 Mn3HSpVv[3Srb36gRZN{[Xl? NF72XHg2KM7:TR?= NVq5OpRzOjRiaB?= MYXEUXNQ M2LkXGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? NEHQ[lMzPDd2MUC3OC=>
LNZ308 NF6zWFhHfW6ldHnvckBCe3OjeR?= NHvjbHo2KM7:TR?= M3zhb|I1KGh? M{mzfGROW09? MWLJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV Mn\INlQ4PDFyN{S=
Saos-2 NX\rd5FITnWwY4Tpc44hSXO|YYm= NEP2Smo2OCEQvF2= NGTH[|k1QCCq NEn1[XNKdmirYnn0d{Bk\WyuIHnueoF{cW:w NYnBcZpvOjR5Mke2OlA>
MG-63 MYHGeY5kfGmxbjDBd5NigQ>? MUi1NEDPxE1? NYrVXpNzPDhiaB?= MXnJcohq[mm2czDj[YxtKGmwdnHzbY9v M{nHV|I1PzJ5Nk[w
SJSA-1 NFXvfWZHfW6ldHnvckBCe3OjeR?= MX:1NEDPxE1? Mnu4OFghcA>? M33qeWlvcGmkaYTzJINmdGxiaX72ZZNqd25? NXX4NWdROjR5Mke2OlA>
Saos-2 M2PUb2Z2dmO2aX;uJGF{e2G7 NHPid3U2OCEQvF2= M3TvUVQ5KGh? NV:5TGlbUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? MYCyOFczPzZ4MB?=
MG-63 MkjBSpVv[3Srb36gRZN{[Xl? M4PnXFUxKM7:TR?= NFq0OXk1QCCq MlXHTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> MojBNlQ4Ojd4NkC=
SJSA-1 M3ztZmZ2dmO2aX;uJGF{e2G7 NFLFUFE2OCEQvF2= MkX5OFghcA>? NXrJd|dTUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? M1vPbFI1PzJ5Nk[w
Saos-2 M2[4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7mZlFxPTBizszN NITONo41QCCq MnXxTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? NI[1TFIzPDd{N{[2NC=>
MG-63 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXDOVAh|ryP MX60PEBp NYmwWG1XUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= NEj5R3gzPDd{N{[2NC=>
SJSA-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWO1NEDPxE1? NXrlPXllPDhiaB?= MUnJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? MWqyOFczPzZ4MB?=
FaDu MXPGeY5kfGmxbjDBd5NigQ>? Ml7TOUDPxE1? MX[yOEBp NIHseo9FVVOR MXvS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= Ml7KNlQ3OzFzNEe=
EMT6 NGH2c|JHfW6ldHnvckBCe3OjeR?= MVy1JO69VQ>? MofDNlQhcA>? MoHZSG1UVw>? NU\WfnZEWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NELrfmczPDZ|MUG0Oy=>
HCT116 MV7GeY5kfGmxbjDBd5NigQ>? MnjpOUDPxE1? M{\KeFI1KGh? MmLVSG1UVw>? MXvS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= MU[yOFY{OTF2Nx?=
U87 NXW1bJg6TnWwY4Tpc44hSXO|YYm= MUO1JO69VQ>? MYiyOEBp M2LSWWROW09? MUXS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NE\DZYczPDZ|MUG0Oy=>
GBM M2L2T2Fxd3C2b4Ppd{BCe3OjeR?= M3jnR|LPxE1? Mk\jOFhp MlPWSG1UVw>? MWrpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5 NVPJcmE1OjR3MEC0PVI>
BON NX3Oe2xnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HuSVEuPc7:TR?= MXW3Nog> NWWz[2Mz\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? MXWyOFQ1OzV{Mx?=
BON NGXwe4VCeG:ydH;zbZMhSXO|YYm= NEHFXnkyNTYQvF2= NUDrTVZZOjSq M3OyPYlv[3KnYYPld{BieG:ydH;zbZM> NX3FfGNEOjR2NEO1NlM>
H1975 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnP0NE4{NTlwNt88US=> NVjxWJN2PzKq NUXCdFJDTE2VTx?= M1T6ZmlEPTB;MT6zPFXPxE1? NI\QblMzPDN|N{i0Oi=>
H1975 M4j0UWFxd3C2b4Ppd{BCe3OjeR?= NWLjSoNROs7:TR?= NF;Q[IszPGh? NFzYS|hFVVOR MYnpcoNz\WG|ZYOgZZBweHSxc3nzJJJifGVic3nncolncWOjboTsfS=> MoLaNlQ{Ozd6NE[=
T-ALL NXnDNJRUSXCxcITvd4l{KEG|c3H5 M4\oZ4JmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= NWr6PY9vOjRib4KgOFhp NFfycJNFVVOR MVnh[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= NUS2WmlPOjR|MUC3N|Y>
BCR-ABL NW\LUnFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPadotnOC5{NT2xNO69VQ>? NFv1Z2Q1\A>? M4fRUpNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? NXrVRmpWOjR{NES2NVI>
LC-1/SQSF NIXnZpdHfW6ldHnvckBCe3OjeR?= MkLwN:69VQ>? M4nZb|I1cA>? MlP3SG1UVw>? M{DnfoRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> NYDtboE6OjN7OECwPVM>
Primary CLL cells NXO1VJFqSXCxcITvd4l{KEG|c3H5 MXWxMVEx|ryP NGT6S281QGh? MVHpcoR2[2W|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz NV3pW45NOjN6NUC4NFc>
Primary CLL cells M{HGb2tqdmG|ZTDBd5NigQ>? MnfFNu69VQ>? NEPTXJI{OG2rbh?= NEG0UoVl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= NHrKWpEzOzh3MEiwOy=>
Primary CLL cells NFXmNGtEgXSxdH;4bYMhSXO|YYm= NXPs[Gl6Os7:TR?= Mm\QNlRp NY\KVWZpcW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=> NGW3O|AzOzh3MEiwOy=>
human NSCLC cell lines MX3BdI9xfG:|aYOgRZN{[Xl? MVGwMlEzPS12zszN M4jXWVI1cA>? M4XwUWROW09? NXe5O4JqUUN3MIOgdoFv\2W|IH\yc40hOC52LUNOwG0> MYqyN|U3OjR5Mh?=
human HCC cell lines MnLIR4VtdCC4aXHibYxqfHliYYPzZZk> NHjERlAxNjByNT2x{txO M1\W[FQ5cA>? NWfSbpluUUN3ME2x{txO NWLCSJRnOjN2OEm5PVk>
Huh7 MmLqT4lv[XOnIFHzd4F6 NVz5XW9ROc7:TR?= MVK0PIg> M1jOXpNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M3rQW|I{PDh7OUm5
SK-HEP1 NXrTVo1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV35dmdNOS1{MN88US=> MV:3Nog> NXTiOVV6TE2VTx?= M2HreWlEPTExvKyx{txO NWPZNJdEOjN2N{mxN|Y>
786-0 NVTDXmZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfBN24yNTJyzszN M1XQc|czcA>? NHznVINFVVOR MonMTWM2OO,:nEJOwG0> MlrmNlM1PzlzM{[=
JVM2 MVLDfZRwfG:6aXPpeJkh[XO|YYm= MYWwMlIuOjEQvF2= MUe3Nog> MoTXSG1UVw>? MlvJTWM2OD1yLkpOwG0> NEHZfm0zOzJ|OE[zPS=>
EHEB NYDDPJlIS3m2b4TvfIlkcXS7IHHzd4F6 NV;uOZFUOC5{LUKw{txO MU[3Nog> NFHH[WxFVVOR MVTJR|UxRTBwN988US=> NYf3UXc1OjN{M{i2N|k>
MEC2 NHrpRW9EgXSxdH;4bYNqfHliYYPzZZk> MknkNE4zNTJyzszN MkLjO|Jp M1eyZ2ROW09? NVrKWGoxUUN3ME2wMlfPxE1? MmTyNlMzOzh4M{m=
primary B-CLL lymphocytes NVrJeI9YSXCxcITvd4l{KEG|c3H5 MVjJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m M{jK[FI1cA>? MVPEUXNQ MlLWTWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> NE\nepkzOzJ|OE[zPS=>
primary B-CLL lymphocytes MVTLbY5ie2ViQYPzZZk> MUjJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m NVvZUlNpOjSq NEjRXFFqdmirYnn0d{BxPzCVNlugKkA1TS2EUEGg[ZhxemW|c3nvci=> MX6yN|I{QDZ|OR?=
human NSCLC MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPhUXcxNjVvMt88US=> MlvRO|Jp NXHTO2g5UUN3ME2x{txO NH3FXoozOjd6MUO5Ny=>
human NSCLC M1ziZ2tqdmG|ZTDBd5NigQ>? NXPiZ4tyOc7:TR?= Mlu0NlRp M1zMRolvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= MmrDNlI4QDF|OUO=
Y1 cell line NHLNN49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHYNE4y|ryPL{JOwG0> MYeyOIg> MlTDSG1UVw>? MXfpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>? NWXhclFGOjJ4OUK5NFQ>
PIK3CA-mutant MCF7 NXrQS4lET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPOS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? M1rqdVczcA>? NUjaeZNjT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= M{DMPVIzPjV|OU[3
PIK3CA-mutant MCF7 MUfLbY5ie2ViQYPzZZk> MUjJR|UxRTFzNNMxN45O NUPnTYxPPzKq MUTJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| MXqyNlY2Ozl4Nx?=
MCF7-myr-Akt NWm1[GdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrqS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? NUPGblRwPzKq MnnzS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? NIr5N5YzOjZ3M{m2Oy=>
colon cancer cell lines Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7FdIdJOC1zMN88US=> NELv[IE4Omh? MVTEUXNQ MWTJR|UxRTIQvF2= NX\INFVwOjJ3NEO4OVc>
gastric cancer cell lines MoXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEOxcVQxNTFyzszN M{TSPFczcA>? M1q1Z2ROW09? NFS5VlRKSzVyPUKtOe69VQ>? MVKyNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45 NX65b4FQSXCxcITvd4l{KEG|c3H5 MVOy{txO MWW0PIg> M1viSpNpcW[2IHnuJGczKHCqYYPl MkPUNlI2PDN6NUe=
HT-29 and HCT-116 NGe4eGpE[XOyYYPlJIF{e2G7 M1vHVlXPxE1? MUWyOIg> M2DhZYlv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= NH3KT2kzOjV2M{i1Oy=>
MM cell lines MlXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNO69VQ>? NETEe28zPGh? NIewPYpFVVOR NF\Td2hKSzVyII\hdolmeyCjbX;u[{BlcW[oZYLlcpQh[2WubDDsbY5meyCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVv[2V? NYewVVREOjJ{MEe0PFU>
ARP-1 NETQbFhCeG:ydH;zbZMhSXO|YYm= MYWxNO69VQ>? NWn2RmpGOjSq M2SwU2ROW09? NVvFNYhWcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> M1zR[lIzOjB5NEi1
SNU-601 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWW3Nog> MXLEUXNQ Mkj2TWM2OD1yLkixOuKyOC5yNkROwG0> NWfJR2tSOjJzNUm4NVQ>
SNU-1 NHnycmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjBO|Jp NGS0fFlFVVOR MXnJR|UxRTFwMEiyxtExNjB{ON88US=> NXXTO|VNOjJzNUm4NVQ>
SNU-668 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWm3Nog> NIj0R5lFVVOR MWHJR|UxRTFwNUe5xtExNjB5NN88US=> MVyyNlE2QThzNB?=
AGS MoO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrGcow4Omh? MYPEUXNQ M4\mPWlEPTB;MT63NVTDuTBwMUG3{txO M1jqNFIzOTV7OEG0
SNU-216 MkjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX2cJFEPzKq Mn7mSG1UVw>? MoPWTWM2OD1{Lk[5NuKyOC5yOENOwG0> M2f1TFIzOTV7OEG0
SNU-5 NUPwV5pKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLifWg4Omh? NEHnS4FFVVOR NGricFNKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? MoLjNlIyPTl6MUS=
SNU-638 NFTEWGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzwOWlMPzKq Mn;MSG1UVw>? M17LVmlEPTB;Mj6yPFLDuTBwMEWz{txO NGLXW3YzOjF3OUixOC=>
SNU-16 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe3Nog> NU[3e5B3TE2VTx?= M4S1cmlEPTB;MT61O|PDuTBwMECx{txO MlX5NlIyPTl6MUS=
SNU-484 MkjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojNO|Jp MmnzSG1UVw>? MlvzTWM2OD1zLkeyPOKyOC5yNEZOwG0> MlXDNlIyPTl6MUS=
SNU-620 M2jtSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TuS|czcA>? M1u4bWROW09? MYXJR|UxRTJwOUO5xtExNjByMd88US=> MnrGNlIyPTl6MUS=
SNU-719 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj4O|Jp NGf6UIZFVVOR NEL4elJKSzVyPUOuNFM4yrFyLkCzNu69VQ>? NVrR[25POjJzNUm4NVQ>
glioma cell lines MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrvRnJYPzKq MX3JR|UxRTFvMt88US=> MXyyNlA3PTB6MB?=
U87 NGLRZldCeG:ydH;zbZMhSXO|YYm= MnvQNu69VQ>? NHrZ[4g4Omh? NV32NYNLcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> MWiyNlA3PTB6MB?=

... 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)


Click to enlarge
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.

Click to enlarge
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.

Click to enlarge
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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  • 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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