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 NGiwV29EgXSxdH;4bYMhSXO|YYm= MmruO|IhcA>? Mly0SG1UVw>? NF;Cc4pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN NXPqZ|lFOjR7MECyOlY>
DU145 MV;DfZRwfG:6aXOgRZN{[Xl? M3uwRlczKGh? M{nOSmROW09? M3vo[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiTFvCNUBufXSjboSge4l1cCCJSUWwJI9nKDBwMECwOFM2KM7:TR?= MoLkNlQ6ODB{Nk[=
A2780 NYnCTpZ4S3m2b4TvfIlkKEG|c3H5 MoPkO|IhcA>? MVzEUXNQ NHnU[JREgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN MlGyNlQ6ODB{Nk[=
U87MG NWH3WpFQS3m2b4TvfIlkKEG|c3H5 M3zEe|czKGh? MWnEUXNQ M1znV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY6QCEQvF2= NWf2TXlYOjR7MECyOlY>
A2780 M37rTGZ2dmO2aX;uJGF{e2G7 M2L1dFEhcA>? MlvuSG1UVw>? MVnJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>? MoHONlQ6ODB{Nk[=
DU145 MXfGeY5kfGmxbjDBd5NigQ>? MXyxJIg> MUjEUXNQ NFXHfGhKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hTFVzNEWgZ4VtdHNiaHHyZo9zcW6pIFzLRlEhdXW2YYTpc44hf2m2aDDFR|UxKG:oIECuNFc{KM7:TR?= MXqyOFkxODJ4Nh?=
A2780 M3nN[mZ2dmO2aX;uJGF{e2G7 NFjKd2MyKGh? MlK1SG1UVw>? M1e3S2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP MUSyOFkxODJ4Nh?=
MCF7 NGTafY9HfW6ldHnvckBCe3OjeR?= NF7HfGMyKGh? NF;IR|BFVVOR NGK0dlZKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNUDPxE1? MV6yOFkxODJ4Nh?=
U87MG NHvFVZhHfW6ldHnvckBCe3OjeR?= NFfvbHkyKGh? MnXxSG1UVw>? NXLUepgxUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJHU5P02JIHPlcIx{KHerdHigSWM2OCCxZjCwMlE{KM7:TR?= M1TKSFI1QTByMk[2
A2780 M4f0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHR[284OiCq NGHjbGhFVVOR NHLRZ5BGSzVyPUCuOVIh|ryP MUSyOFkxODJ4Nh?=
SKMES-1 M17jUGN6fG:2b4jpZ{BCe3OjeR?= MVyxJO69VQ>? MWS3NkBp Moi2TY5lfWOnczDj[YxtKGSnYYTo NIHC[oYzPjBzM{OxPC=>
H596 MUXGeY5kfGmxbjDBd5NigQ>? NUjWUWFzOSEQvF2= MmHPTY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>? MmXPNlYxOTN|MUi=
HCC2450 MlT3SpVv[3Srb36gRZN{[Xl? Mne1NUDPxE1? NFryUVZKdXCjaYLzJINmdGxiaX72ZZNqd25? NXTtR49GOjZyMUOzNVg>
A549 MXvGeY5kfGmxbjDBd5NigQ>? Mn;pOVAxKG6P M4jTO|Q5KGh? NGezTIZFVVOR MoTWTY5pcWKrdIOgRYt1KGGldHn2ZZRqd25? M17Lc|I2QTN5Mkm5
A549 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXkPJRIOSEQvF2= MmG1O|IhcA>? MkLuSG1UVw>? NG\TZolKdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3LjeFI2QTN5Mkm5
H522 MkDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSxJO69VQ>? MYW3NkBp MX\EUXNQ MV7Jcohq[mm2czDj[YxtKGe{b4f0bC=> MlnwNlU6Ozd{OUm=
LNCaP NFjJV2JHfW6ldHnvckBCe3OjeR?= MV[xJO69VQ>? NIn2UZBUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?= MU[yOVM3ODd7OR?=
LNCaP95 MmPPSpVv[3Srb36gRZN{[Xl? MV2xJO69VQ>? MVHTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? MWOyOVM3ODd7OR?=
HCT-15 MYrBdI91d3OrczDBd5NigQ>? NHK3VFkyOCEQvF2= NFXXRWM1QCCq NF3vbY9FVVOR NECy[2pKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVUh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NHW3N2wzPTF3MkK0OS=>
HCT-116 NYriTm5bSXCxdH;zbZMhSXO|YYm= MXixNEDPxE1? MYC0PEBp NHvNPJlFVVOR NUHIXXFQUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVEyPiClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u NU\LbWduOjVzNUKyOFU>
NCI-H460 M2LnRWFxd3Sxc3nzJGF{e2G7 NWf3XpRmOTBizszN M3fqdlQ5KGh? NWLPS2VmTE2VTx?= MnnlTY5lfWOnczDhdI9xfG:|aYOgbY4hVkOLLVi0OlAh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= MkOwNlUyPTJ{NEW=
SKOV-3 NV30V3lxSXCxdH;zbZMhSXO|YYm= NEDXWWcyOCEQvF2= MVS0PEBp MnTSSG1UVw>? MlHiTY5lfWOnczDhdI9xfG:|aYOgbY4hW0uRVj2zJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? NIXJUFAzPTF3MkK0OS=>
BSY-1 MWPBdI91d3OrczDBd5NigQ>? M4Ox[lExKM7:TR?= NGnORYw1QCCq MoWySG1UVw>? NVTFRndGUW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NFXufWszPTF3MkK0OS=>
MKN-1 M2W4UGFxd3Sxc3nzJGF{e2G7 MUexNEDPxE1? MW[0PEBp NYrkR4VNTE2VTx?= NE\0TY5KdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w M1S5[|I2OTV{MkS1
NCI-H522 M3q4fWFxd3Sxc3nzJGF{e2G7 MX2xNEDPxE1? MkS1OFghcA>? NXPBc|NrTE2VTx?= M{Tpc2lv\HWlZYOgZZBweHSxc3nz M3;6VVI2OTV{MkS1
OVCAR-3 MY\BdI91d3OrczDBd5NigQ>? MYGxNEDPxE1? MVS0PEBp M3vWdWROW09? Mnv3TY5lfWOnczDhdI9xfG:|aYO= M4rX[lI2OTV{MkS1
HBC-5 MlnVRZBwfG:|aYOgRZN{[Xl? NVLMbVJqOTBizszN M4DVelQ5KGh? MXvEUXNQ NX;pO3k1UW6mdXPld{BieG:ydH;zbZM> NUfN[YFiOjVzNUKyOFU>
RXF-631L MV7BdI91d3OrczDBd5NigQ>? MVGxNEDPxE1? Mn;pOFghcA>? NWTicFdmTE2VTx?= MYjJcoR2[2W|IHHwc5B1d3Orcx?= M13qNlI2OTV{MkS1
MKN-45 MUHBdI91d3OrczDBd5NigQ>? MlSyNVAh|ryP Mk\YOFghcA>? MkW4SG1UVw>? NYrVVmZNUW6mdXPld{BieG:ydH;zbZM> M{LuflI2OTV{MkS1
BON-1 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXOOVAxKG6P NVvYOVZ3OTBiZB?= MkXJSG1UVw>? NIjaXW5KdmirYnn0d{Bk\WyuIHfyc5d1cA>? M1zybFI2ODJ4Mkmy
BON-1 MkXHSpVv[3Srb36gRZN{[Xl? MnvIOVAxKG6P M3jsT|QhcA>? MV7EUXNQ MmnHTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= NWLje243OjVyMk[yPVI>
QGP-1 NEHOfmdHfW6ldHnvckBCe3OjeR?= M1PQblUxOCCwTR?= MorKOEBp MVnEUXNQ MWTJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| MUOyOVAzPjJ7Mh?=
Huh7 NEDoZ29HfW6ldHnvckBCe3OjeR?= NEHrXFYyKM7:TR?= MnfGNUBp Ml3BSG1UVw>? MlzVTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR? MnPLNlUxODR2MEO=
BNL NITwZYNHfW6ldHnvckBCe3OjeR?= MlXBNUDPxE1? M{\3NlEhcA>? M{Sy[WROW09? M2nwOGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>? M3vqUFI2ODB2NECz
MDA-MB-175 M3LpRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYixJO69VQ>? M3rldFUh\A>? Mk[2SG1UVw>? NIjwT2lKSzVyPEGg{txO NV21cG0{OjR6N{m3PVY>
MDA-MB-134 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;vNUDPxE1? NEXRblI2KGR? NHW5dFFFVVOR NEfOWJVKSzVyPEGg{txO MlvnNlQ5Pzl5OU[=
HCC1500 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3TTZUyKM7:TR?= NFLyTHk2KGR? MY\EUXNQ NI\LOo5KSzVyPEGg{txO NYTxc5pSOjR6N{m3PVY>
EFM-19 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LFeFEh|ryP M4ixRVUh\A>? MYDEUXNQ NFPLSINKSzVyPEGg{txO NFzpNmMzPDh5OUe5Oi=>
ZR-75-30 NFzDR5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEC4flIyKM7:TR?= M4q2T|Uh\A>? MUHEUXNQ M3fVXGlEPTB:MTFOwG0> MnraNlQ5Pzl5OU[=
MDA-MB-361 M3PhWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTpVYdYOSEQvF2= NFnHVoo2KGR? M2rkSmROW09? Mn7BTWM2ODxzIN88US=> M{\JOlI1QDd7N{m2
T-47D MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3mxblEh|ryP NGq4bVg2KGR? NX3sOWpjTE2VTx?= NXr6NGpLUUN3MEyxJO69VQ>? M4DmW|I1QDd7N{m2
SK-BR-3 NY\CcHR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFG1cngyKM7:TR?= NUDyZ|dSPSCm MXrEUXNQ NH:wNHpKSzVyPEGg{txO NHrn[W4zPDh5OUe5Oi=>
UACC-732 MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDJSmVLOSEQvF2= NWfDb203PSCm Mm[4SG1UVw>? M3rTcWlEPTB:MTFOwG0> NFziO3ozPDh5OUe5Oi=>
BT-474 NWHjXlI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vlVlEh|ryP M4nEVFUh\A>? M2P5NWROW09? MXPJR|UxRDFizszN NFP0UG4zPDh5OUe5Oi=>
HCC202 NXfmZVRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUCxJO69VQ>? Mmm1OUBl NHHUOoxFVVOR NWXNTm1FUUN3MEyxJO69VQ>? NWnEUpBPOjR6N{m3PVY>
MCF7 NGPJV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHzVJYyKM7:TR?= MVm1JIQ> NIq0[3BFVVOR Mn7oTWM2ODxzIN88US=> NV\COWttOjR6N{m3PVY>
MDA-MB-415 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYWxJO69VQ>? M2PvOFUh\A>? MU\EUXNQ M1;wfWlEPTB:MTFOwG0> M4jHdlI1QDd7N{m2
MDA-MB-453 NF[zXXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xJO69VQ>? M2\UTlUh\A>? MlXGSG1UVw>? M2qyfWlEPTB:MTFOwG0> MX6yOFg4QTd7Nh?=
ZR-75-1 NWjYTnJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[xJO69VQ>? NE\NPWU2KGR? NF\tWXlFVVOR NYHUS5l{UUN3MEyxJO69VQ>? M1i1WFI1QDd7N{m2
HCC38 NEHMSGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmxJO69VQ>? NXXXW2gzPSCm NU\6V4JrTE2VTx?= M3zqcGlEPTB:MTFOwG0> NYmxV3hPOjR6N{m3PVY>
HCC1419 NG\YeohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTONUDPxE1? NGTQRYc2KGR? MkPESG1UVw>? NXPyNFdpUUN3MEyxJO69VQ>? NF23S4szPDh5OUe5Oi=>
UACC-812 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zVbVEh|ryP NISxNHc2KGR? NU[0b3U1TE2VTx?= MlzOTWM2ODxzIN88US=> MlHxNlQ5Pzl5OU[=
HCC1187 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqxJO69VQ>? MWe1JIQ> NXf1dJVRTE2VTx?= NHjkWolKSzVyPEGg{txO NWD6dHdtOjR6N{m3PVY>
KPL-1 NVTTS4dsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS1ZYcyKM7:TR?= MWK1JIQ> MX;EUXNQ NUHB[oQ4UUN3MEyxJO69VQ>? MXiyOFg4QTd7Nh?=
SUM-225 MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn0[INsOSEQvF2= NVTsOHZTPSCm NFXOd|RFVVOR Mn23TWM2ODxzIN88US=> NX6ydVFmOjR6N{m3PVY>
EFM-192A MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3e1RlEh|ryP M4nSbVUh\A>? M1e0SmROW09? NV\MSZFvUUN3MEyxJO69VQ>? NWf2UpJVOjR6N{m3PVY>
JIMT-1 M4L4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13hWFEh|ryP NYmzZoRuPSCm MXvEUXNQ NY\0WFBoUUN3MEyxJO69VQ>? M{HuUVI1QDd7N{m2
HCC1143 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjzSnAyKM7:TR?= MXe1JIQ> M33OU2ROW09? M3;6bWlEPTB:MTFOwG0> M2LtWlI1QDd7N{m2
HCC2218 M2DT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrpVHUyKM7:TR?= M1XnNVUh\A>? M{LZN2ROW09? MYHJR|UxRDFizszN NGTYW5ozPDh5OUe5Oi=>
MDA-MB-468 NYfFU3NbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWexJO69VQ>? M3TSdFUh\A>? MXTEUXNQ M1XhS2lEPTB:MTFOwG0> MXeyOFg4QTd7Nh?=
BT-20 NHTZfFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfDPG0yKM7:TR?= M4OxeVUh\A>? M1i2W2ROW09? M1ThfmlEPTB:MTFOwG0> MmrDNlQ5Pzl5OU[=
MDA-MB-435 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWqxJO69VQ>? NVj5cWlJPSCm MX3EUXNQ NU\veFU2UUN3MEyxJO69VQ>? MU[yOFg4QTd7Nh?=
BT-549 M{nTdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGxJO69VQ>? M4\vZlUh\A>? NWTCZ4hFTE2VTx?= M3;UNmlEPTB:MTFOwG0> MkTGNlQ5Pzl5OU[=
HCC1806 NWPiTVhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULkenFyOSEQvF2= NXvySIc3PSCm M3nGSmROW09? MUfJR|UxRDFizszN MV:yOFg4QTd7Nh?=
HCC1937 NHnDdohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmOzNUDPxE1? M2fUbVUh\A>? MlLWSG1UVw>? NUX2OHY1UUN3MEyxJO69VQ>? MlziNlQ5Pzl5OU[=
Hs578T MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrmWIgyKM7:TR?= M4ftWFUh\A>? MYXEUXNQ MVnJR|UxRDFizszN NVzQ[HBwOjR6N{m3PVY>
LN18 NVjpZWxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{OwfVIxKM7:TR?= MlLHO|IhcA>? MWrEUXNQ NUfTZXNlUUN3MEy1JO69VQ>? NWTnXY1[OjR5NEGwO|Q>
LN229 M1G3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6yNEDPxE1? M3vLPVczKGh? NIr2UHZFVVOR MnPlTWM2ODx3IN88US=> MlTKNlQ4PDFyN{S=
LNZ308 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnNNlAh|ryP NFjzfXc4OiCq NGK4d3JFVVOR NYLkZ4ZWUUN3MEy1JO69VQ>? MmHINlQ4PDFyN{S=
T98G MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\LNVIxKM7:TR?= NULw[XEyPzJiaB?= NHS2RYJFVVOR M1\RWWlEPTB:NTFOwG0> NGP2OpEzPDd2MUC3OC=>
U87 MlXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnL4NlAh|ryP NE\s[Ig4OiCq MX\EUXNQ M4[wdmlEPTB:NTFOwG0> Ml7PNlQ4PDFyN{S=
LN18 Mm\iSpVv[3Srb36gRZN{[Xl? NF\LZXM2KM7:TR?= M3;V[|I1KGh? Ml7USG1UVw>? NUTJe5VbUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NXXoWXJ5OjR5NEGwO|Q>
LNZ308 NELrVFVHfW6ldHnvckBCe3OjeR?= NHnQOnY2KM7:TR?= M3r2flI1KGh? NVTnSVlbTE2VTx?= NXPKWpMzUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= M3S3cVI1PzRzMEe0
Saos-2 M3fhR2Z2dmO2aX;uJGF{e2G7 M37SbFUxKM7:TR?= MnvBOFghcA>? NIXPWXpKdmirYnn0d{Bk\WyuIHnueoF{cW:w MX2yOFczPzZ4MB?=
MG-63 NIfnUFZHfW6ldHnvckBCe3OjeR?= NGPGNJM2OCEQvF2= MVK0PEBp MYHJcohq[mm2czDj[YxtKGmwdnHzbY9v MVWyOFczPzZ4MB?=
SJSA-1 NUfX[W9wTnWwY4Tpc44hSXO|YYm= NH3mNWM2OCEQvF2= NH7MZ4o1QCCq MljLTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? MWiyOFczPzZ4MB?=
Saos-2 MlrpSpVv[3Srb36gRZN{[Xl? MVW1NEDPxE1? NGjVR2I1QCCq M1\xPGlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MlrINlQ4Ojd4NkC=
MG-63 NIn1ZYFHfW6ldHnvckBCe3OjeR?= MVW1NEDPxE1? M3\z[FQ5KGh? NHr6e2JKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v NXrV[pNWOjR5Mke2OlA>
SJSA-1 NWfTWnVTTnWwY4Tpc44hSXO|YYm= NXfRd5R[PTBizszN MW[0PEBp MXrJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u M4LvZVI1PzJ5Nk[w
Saos-2 NWnoOVZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG4XpY2OCEQvF2= NGOye2Q1QCCq NVTqVlhPUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= NHX2VXEzPDd{N{[2NC=>
MG-63 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLNOVAh|ryP NFi0Nmo1QCCq NFzHXmRKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MnzINlQ4Ojd4NkC=
SJSA-1 NVr2UpZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe1NEDPxE1? M1vqdVQ5KGh? NHywcJVKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NWHFeFJuOjR5Mke2OlA>
FaDu MVTGeY5kfGmxbjDBd5NigQ>? NHTLTpg2KM7:TR?= NUjN[mdFOjRiaB?= MoHaSG1UVw>? MVLS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NILXd44zPDZ|MUG0Oy=>
EMT6 NV\IUXRsTnWwY4Tpc44hSXO|YYm= MlPCOUDPxE1? M{HDNFI1KGh? MnztSG1UVw>? M1P2bXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u M2\uUFI1PjNzMUS3
HCT116 NFzieJJHfW6ldHnvckBCe3OjeR?= MX[1JO69VQ>? Mnz2NlQhcA>? M3\5TmROW09? MWLS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NVLLW3Z[OjR4M{GxOFc>
U87 NGjPNppHfW6ldHnvckBCe3OjeR?= NWnMSo5OPSEQvF2= M1PzfFI1KGh? NV2z[nRCTE2VTx?= MVTS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= MlfzNlQ3OzFzNEe=
GBM M3jkU2Fxd3C2b4Ppd{BCe3OjeR?= MXqy{txO M4n5PVQ5cA>? NYXuUo91TE2VTx?= Ml\wbY5lfWOnZDDobYdp\XJibHX2[Yx{KG:oIHHwc5B1d3OrczygZY5lKGSnY4LlZZNm\CClZXzsJJZq[WKrbHn0fS=> MXuyOFUxODR7Mh?=
BON M3zuXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;xNU02|ryP NHqySpk4Omh? Mmjj[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NX7qbldkOjR2NEO1NlM>
BON NVXtSYM2SXCxcITvd4l{KEG|c3H5 MV6xMVXPxE1? NHTn[I4zPGh? MX\pcoNz\WG|ZYOgZZBweHSxc3nz NVS1[4plOjR2NEO1NlM>
H1975 NH7XV4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:5e2FNOC5|LUmuOu69VQ>? Mn\JO|Jp NX3STllKTE2VTx?= MmLDTWM2OD1zLkO4Oe69VQ>? MmKyNlQ{Ozd6NE[=
H1975 M1zMeWFxd3C2b4Ppd{BCe3OjeR?= MoPtNu69VQ>? NHnE[nAzPGh? MVvEUXNQ M4X3dYlv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6 M3HNS|I1OzN5OES2
T-ALL NIfsNplCeG:ydH;zbZMhSXO|YYm= MlS5ZoV1f2WnbjCxMlQh[W6mIEWuN{BuVSCjdDCyOIgh[W6mIECuPUBidmRiNT61JI1OKGG2IES4bEBqdiCmaX\m[ZJmdnRiY3XscEBtcW6n MX6yOEBweiB2OHi= NGTlfHBFVVOR M3S1coFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz NGH0XW8zPDNzMEezOi=>
BCR-ABL NGrXXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\lVmIxNjJ3LUGw{txO M2nDdFRl M{nnWZNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? NWiwcIVKOjR{NES2NVI>
LC-1/SQSF Mn:4SpVv[3Srb36gRZN{[Xl? MUez{txO M4rCdVI1cA>? M1PMV2ROW09? M2rFbYRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> NX36SJNvOjN7OECwPVM>
Primary CLL cells NFnKelRCeG:ydH;zbZMhSXO|YYm= M3uwNlEuOTEQvF2= M17VNVQ5cA>? MWPpcoR2[2W|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz MoDsNlM5PTB6MEe=
Primary CLL cells MlrjT4lv[XOnIFHzd4F6 M2fofFLPxE1? NWL6VYh3OzCvaX6= MmTJ[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? NGnMSlMzOzh3MEiwOy=>
Primary CLL cells NHq5WmFEgXSxdH;4bYMhSXO|YYm= NGjrWFkz|ryP M3XCOFI1cA>? NXTXXnlQcW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=> M3;Qb|I{QDVyOEC3
human NSCLC cell lines MlfyRZBweHSxc3nzJGF{e2G7 M2P1XlAvOTJ3LUVOwG0> NHPte44zPGh? MlrCSG1UVw>? M3TjOWlEPTC|IILhcodmeyCocn;tJFAvPC1{zszN M3nIcVI{PTZ{NEey
human HCC cell lines M4Sw[2NmdGxidnnhZoltcXS7IHHzd4F6 NWP5N2ZzOC5yMEWtNe69VQ>? M3zlZ|Q5cA>? MXfJR|UxRTIQvF2= MoL3NlM1QDl7OUm=
Huh7 MkjxT4lv[XOnIFHzd4F6 NFz3cHUy|ryP M{W4fVQ5cA>? NVrxPWZle2mpbnpvsKFk[W62bImgdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gRYt1 M3vGV|I{PDh7OUm5
SK-HEP1 M1jneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWxMVIx|ryP MmDzO|Jp MlPRSG1UVw>? NULLfGlOUUN3MP-8oFHPxE1? M3LsUVI{PDd7MUO2
786-0 NX60VXcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jnZ|EuOjEQvF2= MV63Nog> MnnvSG1UVw>? NFrVdm9KSzVy78{cNe69VQ>? Mnq3NlM1PzlzM{[=
JVM2 MnnxR5l1d3SxeHnjbZR6KGG|c3H5 NHTsZ3oxNjJvMkFOwG0> MUO3Nog> NFL2[HNFVVOR MX3JR|UxRTBwOd88US=> NELpR|QzOzJ|OE[zPS=>
EHEB NH\kenpEgXSxdH;4bYNqfHliYYPzZZk> M3XBflAvOi1{MN88US=> MXK3Nog> NWC5TG5qTE2VTx?= MWfJR|UxRTBwN988US=> MX2yN|I{QDZ|OR?=
MEC2 NWfhfno5S3m2b4TvfIlkcXS7IHHzd4F6 MnznNE4zNTJyzszN MknuO|Jp MXjEUXNQ NHi5NnBKSzVyPUCuO:69VQ>? M3W5OVI{OjN6NkO5
primary B-CLL lymphocytes M3:2OWFxd3C2b4Ppd{BCe3OjeR?= MUPJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m M1nxSVI1cA>? NHLpVW9FVVOR M3LndmlEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM> M33JOlI{OjN6NkO5
primary B-CLL lymphocytes NF;tZVZMcW6jc3WgRZN{[Xl? M{HiT2lEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? Mny0NlRp MWTpcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= NF3sOpozOzJ|OE[zPS=>
human NSCLC MkT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\YWnI4OC53LUNOwG0> NF7iVHM4Omh? NFzlTVRKSzVyPUJOwG0> NXzqTpN3OjJ5OEGzPVM>
human NSCLC MlLZT4lv[XOnIFHzd4F6 Mmi3Ne69VQ>? NELydHIzPGh? MkPsbY5pcWKrdIOgeIhmKEGtdD;tWG9TKHOrZ37hcIlv\yCyYYToe4F6KGG2IEPoJIFnfGW{IITy[YF1dWWwdB?= NX\RWpFyOjJ5OEGzPVM>
Y1 cell line NXvSXIxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PPfFAvOc7:TT:x{txO MmG5NlRp M1zE[GROW09? NFXHPVZqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?= NVjnOWNJOjJ4OUK5NFQ>
PIK3CA-mutant MCF7 NFjXZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLHfZhbT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= MUi3Nog> NHWxbGpIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= NFXncYQzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 NVXnXHVJU2mwYYPlJGF{e2G7 NEjGOIRKSzVyPUGxOOKyO26P MU[3Nog> MUfJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| MXWyNlY2Ozl4Nx?=
MCF7-myr-Akt NVm5SZdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEP5RpRIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= NFPUeHY4Omh? M13L[mdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P NFvPTGQzOjZ3M{m2Oy=>
colon cancer cell lines M3XZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmmyNE0yOM7:TR?= MWO3Nog> M1LkOWROW09? MmnzTWM2OD1zzszN M{C5WFIzPTR|OEW3
gastric cancer cell lines NUXYT3FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn2NE0yOM7:TR?= MUS3Nog> NILPTJdFVVOR NFvEOGVKSzVyPUKtOe69VQ>? Mmf2NlI2PDN6NUe=
HCT-116/HT-29/MKN-45 MUPBdI9xfG:|aYOgRZN{[Xl? MUOy{txO NHrPWYk1QGh? M2nnZ5NpcW[2IHnuJGczKHCqYYPl NXjXbIxSOjJ3NEO4OVc>
HT-29 and HCT-116 M{PYeGNie3Cjc3WgZZN{[Xl? NXfXVolLPc7:TR?= MlGzNlRp Mk[wbY5lfWOnczDjZZNx[XOnIHHjeIl3cXS7 NUHHcWU2OjJ3NEO4OVc>
MM cell lines MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXISoVMOTEQvF2= MY[yOIg> MUDEUXNQ M4TGT2lEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? MX2yNlIxPzR6NR?=
ARP-1 NHnad|hCeG:ydH;zbZMhSXO|YYm= NHPQOXcyOM7:TR?= MXiyOIg> M1ruWmROW09? M2LHZolv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= MoPSNlIzODd2OEW=
SNU-601 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTnO|Jp NUXG[4QzTE2VTx?= Ml22TWM2OD1yLkixOuKyOC5yNkROwG0> M2LBSlIzOTV7OEG0
SNU-1 MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYW3Nog> NFfDXpdFVVOR MVvJR|UxRTFwMEiyxtExNjB{ON88US=> NHva[VUzOjF3OUixOC=>
SNU-668 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf0O|Jp Mk\xSG1UVw>? MV7JR|UxRTFwNUe5xtExNjB5NN88US=> NXvmc|lUOjJzNUm4NVQ>
AGS NWjxcXRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDhO|Jp MXnEUXNQ Ml\PTWM2OD1zLkexOOKyOC5zMUhOwG0> M2LFc|IzOTV7OEG0
SNU-216 NWLZ[lVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjnO4E4Omh? NEX3dWlFVVOR NGj2XIFKSzVyPUKuOlkzyrFyLkC4Nu69VQ>? MYSyNlE2QThzNB?=
SNU-5 MmjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVW3Nog> M1PaXmROW09? MYPJR|UxRTFwM{WxxtExNjB7Md88US=> MUeyNlE2QThzNB?=
SNU-638 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnqc|A4Omh? MUTEUXNQ NYP6R3cxUUN3ME2yMlI5OsLzMD6wOVPPxE1? M4flPFIzOTV7OEG0
SNU-16 M4fxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DhU|czcA>? NHjqcJZFVVOR Mn36TWM2OD1zLkW3N:KyOC5yMEJOwG0> Mk\uNlIyPTl6MUS=
SNU-484 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXoUo5PPzKq NY\PU5lVTE2VTx?= M1LvbWlEPTB;MT63NljDuTBwMES1{txO MUOyNlE2QThzNB?=
SNU-620 M1rhd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj6N4tOPzKq NXjtb|NTTE2VTx?= NFzQRXlKSzVyPUKuPVM6yrFyLkCwNe69VQ>? NWj0bpNmOjJzNUm4NVQ>
SNU-719 NIrQUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHYUVEyPzKq NW\FNnlzTE2VTx?= NX\UeohpUUN3ME2zMlA{P8LzMD6wN|LPxE1? NEjtNoYzOjF3OUixOC=>
glioma cell lines M1K1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj4O|Jp M3mzNGlEPTB;MT2y{txO NVf1U3NKOjJyNkWwPFA>
U87 MnjLRZBweHSxc3nzJGF{e2G7 NVnUVWp[Os7:TR?= NWG5bpVCPzKq MWDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?= NUTjR2hZOjJyNkWwPFA>

... 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.

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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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    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147)

    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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