BKM120 (NVP-BKM120, Buparlisib)

BKM120 (NVP-BKM120, Buparlisib)は1種のセレクティブPI3K阻害剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は52 nM/166 nM/116 nM/262 nMそれぞれに分かれます。BKM120 (NVP-BKM120, Buparlisib)はVPS34、mTORとDNAPKに作用する効果が良くなくて、PI4Kβにほとんど活性を表しません。臨床2期。

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

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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1種のセレクティブPI3K阻害剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は52 nM/166 nM/116 nM/262 nMそれぞれに分かれます。BKM120 (NVP-BKM120, Buparlisib)はVPS34、mTORとDNAPKに作用する効果が良くなくて、PI4Kβにほとんど活性を表しません。臨床2期。
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 MnjWR5l1d3SxeHnjJGF{e2G7 MofyO|IhcA>? M{TDdWROW09? NVH1Wm43S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=> NEnOVHkzPDlyMEK2Oi=>
DU145 NVvKWYV4S3m2b4TvfIlkKEG|c3H5 NVq4SlRrPzJiaB?= MYrEUXNQ M13oSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiTFvCNUBufXSjboSge4l1cCCJSUWwJI9nKDBwMECwOFM2KM7:TR?= NVTIZZdEOjR7MECyOlY>
A2780 NGjMOnpEgXSxdH;4bYMhSXO|YYm= M2TlXlczKGh? NIDDOphFVVOR M33YU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2= M{DoRlI1QTByMk[2
U87MG NWricG56S3m2b4TvfIlkKEG|c3H5 NIPHS5I4OiCq M{jmeGROW09? MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh|ryP NXzxcms1OjR7MECyOlY>
A2780 MVLGeY5kfGmxbjDBd5NigQ>? MojtNUBp MnTsSG1UVw>? NIH1ZnJKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNFU2KM7:TR?= M4j0UlI1QTByMk[2
DU145 NHvMd5hHfW6ldHnvckBCe3OjeR?= MWWxJIg> MUfEUXNQ MnjPTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? NX\LUIh{OjR7MECyOlY>
A2780 NHnYT3FHfW6ldHnvckBCe3OjeR?= MUCxJIg> NIjiZppFVVOR M{e4NWlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP M{[3fFI1QTByMk[2
MCF7 NXTjeXNLTnWwY4Tpc44hSXO|YYm= MlTUNUBp M4Oxc2ROW09? M2L4TmlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFW1OFVMKG23dHHueE1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6xJO69VQ>? MmjHNlQ6ODB{Nk[=
U87MG MmfnSpVv[3Srb36gRZN{[Xl? NFjuOlQyKGh? M1\yO2ROW09? NEjOOIVKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR|UxKG:oIECuNVMh|ryP NGTldFczPDlyMEK2Oi=>
A2780 NFu5S2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPnOpE4OiCq NYT4ZVZGTE2VTx?= Mn\SSWM2OD1yLkWyJO69VQ>? MmTTNlQ6ODB{Nk[=
SKMES-1 M3TNT2N6fG:2b4jpZ{BCe3OjeR?= NVLVN5ExOSEQvF2= MV[3NkBp MkXiTY5lfWOnczDj[YxtKGSnYYTo NIPZeHMzPjBzM{OxPC=>
H596 M4[0S2Z2dmO2aX;uJGF{e2G7 NI[1bW4yKM7:TR?= MkDVTY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>? NXz5W5VlOjZyMUOzNVg>
HCC2450 MYXGeY5kfGmxbjDBd5NigQ>? Mlv5NUDPxE1? M{DiPWlueGGrcoOgZ4VtdCCrbo\hd4lwdg>? NGXiRnIzPjBzM{OxPC=>
A549 NFzJcZBHfW6ldHnvckBCe3OjeR?= NX3Pcmd[PTByIH7N NVv4UYg{PDhiaB?= NGXyOVhFVVOR NXvOfoJmUW6qaXLpeJMhSWu2IHHjeIl3[XSrb36= MU[yOVk{PzJ7OR?=
A549 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33scFEh|ryP NYTtRpB{PzJiaB?= M13uVmROW09? MVHJcohq[mm2czDj[YxtKGe{b4f0bC=> MYWyOVk{PzJ7OR?=
H522 Mm\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxJO69VQ>? NXzGe3k5PzJiaB?= MWPEUXNQ NFL4fGFKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NV7GRXZ6OjV7M{eyPVk>
LNCaP NIqwNpJHfW6ldHnvckBCe3OjeR?= NVfCfpJiOSEQvF2= Mlv3V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? MkDRNlU{PjB5OUm=
LNCaP95 NHzETo9HfW6ldHnvckBCe3OjeR?= MYWxJO69VQ>? NUTqd2h3W3WycILld5NmeyCyLVHLWEBt\X[nbIO= M2PXXVI2OzZyN{m5
HCT-15 MU\BdI91d3OrczDBd5NigQ>? NXjNPHU{OTBizszN NWPxZY1QPDhiaB?= M4LITGROW09? M4P0d2lv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xOUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NVKzV2JpOjVzNUKyOFU>
HCT-116 NFfhUpRCeG:2b4Ppd{BCe3OjeR?= NGPWfHcyOCEQvF2= Mkj6OFghcA>? NYjpeGx[TE2VTx?= MVzJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? M1H2WlI2OTV{MkS1
NCI-H460 MYfBdI91d3OrczDBd5NigQ>? NIX0SW0yOCEQvF2= Mk\QOFghcA>? NGj3c21FVVOR M2Lpdmlv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= M2\IVFI2OTV{MkS1
SKOV-3 MkHPRZBwfG:|aYOgRZN{[Xl? MWqxNEDPxE1? MlHSOFghcA>? NFXUPJBFVVOR NVvsUpBQUW6mdXPld{BieG:ydH;zbZMhcW5iU1vPWk0{KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= MYCyOVE2OjJ2NR?=
BSY-1 MljVRZBwfG:|aYOgRZN{[Xl? MXGxNEDPxE1? NF7ofmQ1QCCq M{DnNmROW09? MW\JcoR2[2W|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v M4XOPFI2OTV{MkS1
MKN-1 NGHsTVFCeG:2b4Ppd{BCe3OjeR?= MVOxNEDPxE1? MYe0PEBp MYfEUXNQ NVrhUJpHUW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= Mn3qNlUyPTJ{NEW=
NCI-H522 MnfQRZBwfG:|aYOgRZN{[Xl? M4L0S|ExKM7:TR?= MkTMOFghcA>? NX7MUoxHTE2VTx?= NVzZZmV5UW6mdXPld{BieG:ydH;zbZM> NIf5VHEzPTF3MkK0OS=>
OVCAR-3 M2LSbWFxd3Sxc3nzJGF{e2G7 Mmq3NVAh|ryP NVfHNVk6PDhiaB?= M4jHR2ROW09? NX\pTo1WUW6mdXPld{BieG:ydH;zbZM> M4D0T|I2OTV{MkS1
HBC-5 NVP5TII6SXCxdH;zbZMhSXO|YYm= MnS2NVAh|ryP Mo[0OFghcA>? M{XZVGROW09? M1qxVGlv\HWlZYOgZZBweHSxc3nz NHTNblYzPTF3MkK0OS=>
RXF-631L NYjEZVBvSXCxdH;zbZMhSXO|YYm= Mlm2NVAh|ryP NULjTFB2PDhiaB?= M4TGVWROW09? NXK5ZohtUW6mdXPld{BieG:ydH;zbZM> M3HLZ|I2OTV{MkS1
MKN-45 MVvBdI91d3OrczDBd5NigQ>? NEfQVW4yOCEQvF2= MWO0PEBp NFPDT4tFVVOR NUL3e5NuUW6mdXPld{BieG:ydH;zbZM> MV[yOVE2OjJ2NR?=
BON-1 NG[5ZnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;nNFUxOCCwTR?= NX;OUJRSOTBiZB?= NHjTOpFFVVOR M3LX[mlvcGmkaYTzJINmdGxiZ4Lve5Rp NYTnNm9wOjVyMk[yPVI>
BON-1 M1\OUGZ2dmO2aX;uJGF{e2G7 Mlf5OVAxKG6P MkjjOEBp MoH1SG1UVw>? MXrJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| NEfmUXMzPTB{NkK5Ni=>
QGP-1 NUPWdmk5TnWwY4Tpc44hSXO|YYm= NEXZdnQ2ODBibl2= MUi0JIg> NX\SdpFVTE2VTx?= NUf0[2h2UW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> MljJNlUxOjZ{OUK=
Huh7 NEHjcplHfW6ldHnvckBCe3OjeR?= MXmxJO69VQ>? MXOxJIg> M33DfGROW09? Ml3STY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR? MkjyNlUxODR2MEO=
BNL M3G3bWZ2dmO2aX;uJGF{e2G7 Mn3NNUDPxE1? MUixJIg> Mm[zSG1UVw>? M2TBOmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>? MlXSNlUxODR2MEO=
MDA-MB-175 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX65UFFoOSEQvF2= NX;MeIk1PSCm NWHMRWJDTE2VTx?= MWDJR|UxRDFizszN NW\0d3VoOjR6N{m3PVY>
MDA-MB-134 M4[5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;vcWxkOSEQvF2= M3nERVUh\A>? MkG5SG1UVw>? NF\LPVRKSzVyPEGg{txO MXiyOFg4QTd7Nh?=
HCC1500 M2juU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3FfnBjOSEQvF2= Ml7YOUBl M163cGROW09? NITvOlBKSzVyPEGg{txO MnPuNlQ5Pzl5OU[=
EFM-19 NFHGOXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXmxJO69VQ>? MXy1JIQ> NGnJUo1FVVOR M2DDT2lEPTB:MTFOwG0> MXSyOFg4QTd7Nh?=
ZR-75-30 NX;4bWR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj5NUDPxE1? NXjTeFhPPSCm MVfEUXNQ Moi0TWM2ODxzIN88US=> MWKyOFg4QTd7Nh?=
MDA-MB-361 NW\pNmpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL5NUDPxE1? NXrz[WNNPSCm M1Pmc2ROW09? NWD0NFFoUUN3MEyxJO69VQ>? M2P3flI1QDd7N{m2
T-47D MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVqxJO69VQ>? NUO3RodFPSCm MmDzSG1UVw>? NHrzNVBKSzVyPEGg{txO MX[yOFg4QTd7Nh?=
SK-BR-3 M3HFd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\ybGUyKM7:TR?= MYq1JIQ> NIDZTYRFVVOR NYC5OldnUUN3MEyxJO69VQ>? Mli3NlQ5Pzl5OU[=
UACC-732 MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[xJO69VQ>? NUSxWXVSPSCm MWXEUXNQ NH;pZnRKSzVyPEGg{txO NXXLRlcyOjR6N{m3PVY>
BT-474 NU\MSnVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKxJO69VQ>? Ml;mOUBl NEm5ZZpFVVOR MlnSTWM2ODxzIN88US=> NGfTV3kzPDh5OUe5Oi=>
HCC202 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\6NUDPxE1? MoTKOUBl M{HiSWROW09? NXT2NXZtUUN3MEyxJO69VQ>? M3rqS|I1QDd7N{m2
MCF7 NGDMe3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWxJO69VQ>? MorKOUBl NFzKSWlFVVOR M{H1OGlEPTB:MTFOwG0> MYSyOFg4QTd7Nh?=
MDA-MB-415 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DqR|Eh|ryP MVy1JIQ> NXu3dWh5TE2VTx?= NYn5VWhlUUN3MEyxJO69VQ>? MWiyOFg4QTd7Nh?=
MDA-MB-453 NFn5Ro5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL5RZVVOSEQvF2= NU\VR2VnPSCm NHzEcpRFVVOR MVLJR|UxRDFizszN NFLtOWYzPDh5OUe5Oi=>
ZR-75-1 NEDXUVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTkN3J3OSEQvF2= NHTO[4I2KGR? MlHUSG1UVw>? NWrIcmN5UUN3MEyxJO69VQ>? NEjJcGczPDh5OUe5Oi=>
HCC38 NF7uXVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3KNUDPxE1? NFLqWG82KGR? NVTVNox7TE2VTx?= MonaTWM2ODxzIN88US=> NVPmfnl{OjR6N{m3PVY>
HCC1419 M2DiTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;yTVEh|ryP M2f1fFUh\A>? M{TGRmROW09? MnXCTWM2ODxzIN88US=> Mn[1NlQ5Pzl5OU[=
UACC-812 NIGwPXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6xJO69VQ>? MnjuOUBl MmrTSG1UVw>? MlP2TWM2ODxzIN88US=> NWfpNG5GOjR6N{m3PVY>
HCC1187 MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Hb5p3OSEQvF2= NVLBWZFtPSCm MWfEUXNQ MUfJR|UxRDFizszN M4XuN|I1QDd7N{m2
KPL-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknJNUDPxE1? NGD6WlA2KGR? MmW3SG1UVw>? MWXJR|UxRDFizszN NV\scWc2OjR6N{m3PVY>
SUM-225 NED4SYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmzR2hLOSEQvF2= M1;3cFUh\A>? MWrEUXNQ MmDDTWM2ODxzIN88US=> NWDY[JlJOjR6N{m3PVY>
EFM-192A MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\PNUDPxE1? MV21JIQ> NUDrOXliTE2VTx?= M3fF[WlEPTB:MTFOwG0> M1SzXVI1QDd7N{m2
JIMT-1 NW\MOGpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVy0bYZ3OSEQvF2= NWnYb5lZPSCm MV3EUXNQ NH7OV|BKSzVyPEGg{txO NIKzV3IzPDh5OUe5Oi=>
HCC1143 NY\Nd3JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj0OGoyKM7:TR?= NGDOdGM2KGR? MXTEUXNQ MV\JR|UxRDFizszN M1XWWlI1QDd7N{m2
HCC2218 MmL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{S0OVEh|ryP MlvHOUBl Mn;LSG1UVw>? MkDqTWM2ODxzIN88US=> NXTaXnd6OjR6N{m3PVY>
MDA-MB-468 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[5NUDPxE1? MXS1JIQ> MlGxSG1UVw>? NX61cXQ6UUN3MEyxJO69VQ>? NIHTb4QzPDh5OUe5Oi=>
BT-20 M2fweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f4V|Eh|ryP M4H6VFUh\A>? M2f1RmROW09? NYPmdXJrUUN3MEyxJO69VQ>? MV:yOFg4QTd7Nh?=
MDA-MB-435 NYL5NFhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuxJO69VQ>? MYS1JIQ> NI\TcpZFVVOR NILB[IJKSzVyPEGg{txO MU[yOFg4QTd7Nh?=
BT-549 MoC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSxJO69VQ>? Mnr5OUBl NXzQW4RZTE2VTx?= M4m0[2lEPTB:MTFOwG0> NH3k[nUzPDh5OUe5Oi=>
HCC1806 NFfD[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGCye5MyKM7:TR?= NFziWWM2KGR? NUfSeWF7TE2VTx?= Mk\aTWM2ODxzIN88US=> M3uwflI1QDd7N{m2
HCC1937 M4nMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGxJO69VQ>? NIXqXnY2KGR? Mn3lSG1UVw>? NGjyRlVKSzVyPEGg{txO NEHTPHUzPDh5OUe5Oi=>
Hs578T NITnN|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HmeVEh|ryP M2f6ZVUh\A>? NUn0SmluTE2VTx?= MmHJTWM2ODxzIN88US=> NV65[YFUOjR6N{m3PVY>
LN18 NWW0WGkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;abXRWOjBizszN NWG0UphIPzJiaB?= NFfVUnZFVVOR MmT2TWM2ODx3IN88US=> NGfk[FIzPDd2MUC3OC=>
LN229 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHOZZozOCEQvF2= MVi3NkBp NX;ufIU2TE2VTx?= NHvic3BKSzVyPEWg{txO NV3I[GxrOjR5NEGwO|Q>
LNZ308 MkHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqyNEDPxE1? MVi3NkBp MWXEUXNQ NGTjZXpKSzVyPEWg{txO MkLtNlQ4PDFyN{S=
T98G NXjIVJE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HHSFIxKM7:TR?= M1rBNlczKGh? NIXNNXlFVVOR Mk\ETWM2ODx3IN88US=> NFfmW5ozPDd2MUC3OC=>
U87 NUnVdWRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPwNlAh|ryP NGjt[ng4OiCq MkXOSG1UVw>? MYHJR|UxRDVizszN MXmyOFc1OTB5NB?=
LN18 M3fQTmZ2dmO2aX;uJGF{e2G7 NHPtWHc2KM7:TR?= NHjL[VMzPCCq NYLIbmZJTE2VTx?= NXnUUVJnUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= MnPYNlQ4PDFyN{S=
LNZ308 MY\GeY5kfGmxbjDBd5NigQ>? NUiwdFhnPSEQvF2= MY[yOEBp MYHEUXNQ NH7aW45KdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuW NWTMZW9rOjR5NEGwO|Q>
Saos-2 MUHGeY5kfGmxbjDBd5NigQ>? NWrabIFDPTBizszN M1T2[lQ5KGh? NEnVW|NKdmirYnn0d{Bk\WyuIHnueoF{cW:w Mn;MNlQ4Ojd4NkC=
MG-63 MUHGeY5kfGmxbjDBd5NigQ>? NXfrWFdHPTBizszN NW\EWHZ{PDhiaB?= MX\Jcohq[mm2czDj[YxtKGmwdnHzbY9v NVnCN5U1OjR5Mke2OlA>
SJSA-1 NV3HNnh2TnWwY4Tpc44hSXO|YYm= NV3STJg1PTBizszN MX[0PEBp M2LqXWlvcGmkaYTzJINmdGxiaX72ZZNqd25? NV;FcXU3OjR5Mke2OlA>
Saos-2 MV7GeY5kfGmxbjDBd5NigQ>? Mmq1OVAh|ryP Mkn2OFghcA>? MX\Jcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NV3Rb2RjOjR5Mke2OlA>
MG-63 M1fvcmZ2dmO2aX;uJGF{e2G7 NYrxWJRWPTBizszN M4myRVQ5KGh? NGnMfZNKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v MUGyOFczPzZ4MB?=
SJSA-1 MojoSpVv[3Srb36gRZN{[Xl? MlLkOVAh|ryP MVi0PEBp NFHLVVlKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v NGHzRWEzPDd{N{[2NC=>
Saos-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf1NFNtPTBizszN MV60PEBp M2DNTGlvcGmkaYTzJINmdGxidnnhZoltcXS7 NWTNVHIzOjR5Mke2OlA>
MG-63 MmLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUC1NEDPxE1? NVTyVVFOPDhiaB?= NHfTN45KdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= M{TRd|I1PzJ5Nk[w
SJSA-1 NVnJ[nFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrTU2dEPTBizszN NVLHPJV5PDhiaB?= MnLpTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? NUfFdmZ3OjR5Mke2OlA>
FaDu MX3GeY5kfGmxbjDBd5NigQ>? MX:1JO69VQ>? MljiNlQhcA>? MV7EUXNQ MWTS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NXH5VJNHOjR4M{GxOFc>
EMT6 MmT3SpVv[3Srb36gRZN{[Xl? NVuyVnFFPSEQvF2= MUiyOEBp NF6wSWFFVVOR MV3S[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NVL2[5Y5OjR4M{GxOFc>
HCT116 NYrZXZhWTnWwY4Tpc44hSXO|YYm= MYO1JO69VQ>? MVWyOEBp NFqwW5BFVVOR NGXBcGFT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> MUGyOFY{OTF2Nx?=
U87 M{jyTWZ2dmO2aX;uJGF{e2G7 NV7wSFVnPSEQvF2= MkHKNlQhcA>? NXLQOmhkTE2VTx?= MkK3VoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= NGnmOFczPDZ|MUG0Oy=>
GBM MnH5RZBweHSxc3nzJGF{e2G7 NIPoRWcz|ryP MXG0PIg> NVXzellSTE2VTx?= NELoR4hqdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6 NF3PWGszPDVyMES5Ni=>
BON MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LLclEuPc7:TR?= Mm\3O|Jp Mn:1[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> MmXtNlQ1PDN3MkO=
BON NV75R5J4SXCxcITvd4l{KEG|c3H5 M{\i[lEuPc7:TR?= NVrEUlU3OjSq NFL6cpBqdmO{ZXHz[ZMh[XCxcITvd4l{ NFfDOoYzPDR2M{WyNy=>
H1975 NWnqOVBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[wMlMuQS54zszN MVG3Nog> MXrEUXNQ NFq1dY9KSzVyPUGuN|g2|ryP NV3NR|lFOjR|M{e4OFY>
H1975 MmK0RZBweHSxc3nzJGF{e2G7 NVm2fGlsOs7:TR?= NXfOR4NkOjSq NGTNblBFVVOR NF;qVWxqdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>? NIX5fIszPDN|N{i0Oi=>
T-ALL NUXLVJhlSXCxcITvd4l{KEG|c3H5 MWXi[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV? MkHiNlQhd3JiNEjo MoXGSG1UVw>? MkPzZYZn\WO2czD0bIUhWEl|SzDwZZRpf2G7IHnuJHQuSUyOIHPlcIwhdGmwZYO= NHnoSJIzPDNzMEezOi=>
BCR-ABL NGfKNJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjXSIUxNjJ3LUGw{txO MkjTOIQ> MWfzbYdvcW[rY3HueIx6KGmwaHnibZQh[2WubDDwdo9tcW[ncnH0bY9v NF\jOJkzPDJ2NE[xNi=>
LC-1/SQSF MoTPSpVv[3Srb36gRZN{[Xl? NHX5XXg{|ryP NGL1e3gzPGh? NWTneJlYTE2VTx?= NYL0dWhl\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt MUmyN|k5ODB7Mx?=
Primary CLL cells M{mxdWFxd3C2b4Ppd{BCe3OjeR?= NH3aTZEyNTFyzszN MYm0PIg> M3TVWIlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> MU[yN|g2ODhyNx?=
Primary CLL cells NFPYPFFMcW6jc3WgRZN{[Xl? MX[y{txO NVfGfIlqOzCvaX6= MkHZ[IVkemWjc3XkJHBKO0tiYXP0bZZqfHl? M1:0OlI{QDVyOEC3
Primary CLL cells M{KwVGN6fG:2b4jpZ{BCe3OjeR?= MlO4Nu69VQ>? Mk\ENlRp MYrpcoR2[2W|IHPlcIwh[3m2b4TvfIlkcXS7 M2LOd|I{QDVyOEC3
human NSCLC cell lines NXK2UFRLSXCxcITvd4l{KEG|c3H5 NYD1cIE3OC5zMkWtOO69VQ>? M4fpXlI1cA>? MoDtSG1UVw>? M3yzU2lEPTC|IILhcodmeyCocn;tJFAvPC1{zszN M1jlb|I{PTZ{NEey
human HCC cell lines MnLMR4VtdCC4aXHibYxqfHliYYPzZZk> M4XxZlAvODB3LUJOwG0> MWq0PIg> MknCTWM2OD1zzszN NYLjTW06OjN2OEm5PVk>
Huh7 NXfTPJBYU2mwYYPlJGF{e2G7 M1rzR|HPxE1? MmfGOFhp MU\zbYdvce,ugXPhcpRtgSC{ZXT1Z4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= MV6yN|Q5QTl7OR?=
SK-HEP1 M4HmPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqxMVIx|ryP NVLOR45EPzKq MnvJSG1UVw>? NGj1T2NKSzVy78{cNe69VQ>? MV6yN|Q4QTF|Nh?=
786-0 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXmNU0zOM7:TR?= NFTjeJY4Omh? M2TKU2ROW09? NIfJ[21KSzVy78{cNe69VQ>? M17hXFI{PDd7MUO2
JVM2 MVHDfZRwfG:6aXPpeJkh[XO|YYm= NIjmcHExNjJvMkFOwG0> MXm3Nog> NGXmXmhFVVOR NXn6TXVuUUN3ME2wMlnPxE1? NYXjdIc3OjN{M{i2N|k>
EHEB Mk\3R5l1d3SxeHnjbZR6KGG|c3H5 Ml;XNE4zNTJyzszN NViwWo9MPzKq M17UR2ROW09? NUO1colwUUN3ME2wMlfPxE1? MknnNlMzOzh4M{m=
MEC2 M3;wdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NX\SWXZOOC5{LUKw{txO M2T4[VczcA>? NWDqSZc2TE2VTx?= NF3rfJJKSzVyPUCuO:69VQ>? MnHJNlMzOzh4M{m=
primary B-CLL lymphocytes MlfBRZBweHSxc3nzJGF{e2G7 NHrhd5hKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n NXHpcVBmOjSq NIHzNXhFVVOR MYXJR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz MlXVNlMzOzh4M{m=
primary B-CLL lymphocytes MlviT4lv[XOnIFHzd4F6 NYPnZoViUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= M1G1[FI1cA>? Mk\TbY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36= M3:yS|I{OjN6NkO5
human NSCLC NFrhfIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6wMlUuOs7:TR?= MX63Nog> MXvJR|UxRTIQvF2= NFf0fVczOjd6MUO5Ny=>
human NSCLC NVzXVXpqU2mwYYPlJGF{e2G7 NUPyeI4zOc7:TR?= MYmyOIg> NUG5VIVrcW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=> MlzuNlI4QDF|OUO=
Y1 cell line MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;IdlAvOc7:TT:x{txO NF\wc2QzPGh? M4fTRmROW09? MorrbY5pcWKrdIOgOlDwxIViY3XscEB3cWGkaXzpeJkhcW5iTYnjMXNkfHJvdILhcpNn\WO2ZXSgZ4VtdHN? M2nve|IzPjl{OUC0
PIK3CA-mutant MCF7 M{GxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4i4fGdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P NXTU[|Y2PzKq MU\HTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? NUT1[YpCOjJ4NUO5Olc>
PIK3CA-mutant MCF7 MlvPT4lv[XOnIFHzd4F6 MYnJR|UxRTFzNNMxN45O NVHMNndJPzKq M{jNW2lEPTB;MUG0xtE{dk1iaX6gdoVlfWOrbnegRYt1KHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= MXOyNlY2Ozl4Nx?=
MCF7-myr-Akt NEG4N2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vKZ2dKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P MnziO|Jp NV;ETG5UT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= NXXzb|dsOjJ4NUO5Olc>
colon cancer cell lines MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnvUWsxNTFyzszN M4HDfFczcA>? NHzTb|FFVVOR NXewRppWUUN3ME2x{txO M1;yfVIzPTR|OEW3
gastric cancer cell lines Mk\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW5OoJGOC1zMN88US=> M2rkd|czcA>? MYTEUXNQ NWjEZ5Z{UUN3ME2yMVXPxE1? NF65R4szOjV2M{i1Oy=>
HCT-116/HT-29/MKN-45 M{H3RWFxd3C2b4Ppd{BCe3OjeR?= MXmy{txO M2jQclQ5cA>? M1XsOpNpcW[2IHnuJGczKHCqYYPl M{TCdlIzPTR|OEW3
HT-29 and HCT-116 Mn\KR4F{eGG|ZTDhd5NigQ>? MmLnOe69VQ>? MkS5NlRp MkO5bY5lfWOnczDjZZNx[XOnIHHjeIl3cXS7 MV6yNlU1Ozh3Nx?=
MM cell lines NWCwNJA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M16zbVEx|ryP MnjLNlRp NVqw[JB4TE2VTx?= Mle1TWM2OCC4YYLp[ZMh[W2xbneg[Iln\mW{ZX70JINmdGxibHnu[ZMhcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcoNm MnPZNlIzODd2OEW=
ARP-1 M2ryOWFxd3C2b4Ppd{BCe3OjeR?= MXWxNO69VQ>? MkizNlRp NYLDXHlSTE2VTx?= M2nIdYlv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= NH7kc4czOjJyN{S4OS=>
SNU-601 NHGzPWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHnS5RKPzKq NYPaVWpPTE2VTx?= MWPJR|UxRTBwOEG2xtExNjB4M988US=> M{niOVIzOTV7OEG0
SNU-1 Mn3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrqO|Jp NVHSdmFbTE2VTx?= NITQe5dKSzVyPUGuNFgzyrFyLkCyPO69VQ>? Ml;VNlIyPTl6MUS=
SNU-668 M{LYVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3j6PVczcA>? NYHFbYRjTE2VTx?= M13UeWlEPTB;MT61O|nDuTBwMEe0{txO M3rI[FIzOTV7OEG0
AGS NUKwZ3QzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVW3Nog> MVXEUXNQ MV\JR|UxRTFwN{G0xtExNjFzN988US=> M3PhO|IzOTV7OEG0
SNU-216 M{m1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojRO|Jp MVHEUXNQ MXzJR|UxRTJwNkmyxtExNjB6Mt88US=> MYKyNlE2QThzNB?=
SNU-5 MmqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDSO|Jp M2DFW2ROW09? NF65fXNKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? MX2yNlE2QThzNB?=
SNU-638 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PxNVczcA>? MVfEUXNQ MVvJR|UxRTJwMkiyxtExNjB3M988US=> Mkf0NlIyPTl6MUS=
SNU-16 NHvq[FlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[3Nog> NWrFSWtGTE2VTx?= MlPnTWM2OD1zLkW3N:KyOC5yMEJOwG0> MVGyNlE2QThzNB?=
SNU-484 NVXIO3l1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\tV4M4Omh? MYXEUXNQ NV7zN4VwUUN3ME2xMlczQMLzMD6wOFXPxE1? NF\UW4kzOjF3OUixOC=>
SNU-620 M4\yVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqwO|Jp M1HKTWROW09? NF7EfmxKSzVyPUKuPVM6yrFyLkCwNe69VQ>? M3PLb|IzOTV7OEG0
SNU-719 NYnNdFFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjibpk4Omh? MkHLSG1UVw>? MXjJR|UxRTNwMEO3xtExNjB|Mt88US=> M33p[VIzOTV7OEG0
glioma cell lines MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPLUHo6PzKq MkjnTWM2OD1zLUNOwG0> MYCyNlA3PTB6MB?=
U87 NGfrUotCeG:ydH;zbZMhSXO|YYm= MYKy{txO MUC3Nog> MnrSbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= M2[2cVIzODZ3MEiw

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 82 mg/mL (199.8 mM)
Ethanol 2 mg/mL (4.87 mM)
Water <1 mg/mL
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

文献中の引用 (34)

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    Pilaralisib (XL147)は一種の選択性的で、可逆なI型PI3K阻害剤で、無細胞試験でPI3Kα/δ/γに作用する時のIC50値が39 nM/36 nM/23 nMそれぞれに分かれて、PI3Kβに低い作用をしています。臨床1/2期。

  • GNE-317

    GNE-317は一種の有効な大脳浸透性のPI3K阻害剤です。

  • PI-3065

    PI-3065は一種の選択性p110δ阻害剤で、IC50値が15 nMです。PI-3065は選択性について、他のPI3K家族メンバーより70倍以上が高くなります。

  • LY294002

    LY294002は初めての周知されたPI3Kα/δ/βを抑制する小分子で、無細胞試験でIC50値が0.5 μM/0.57 μM/0.97 μM に分かれることですが、溶液にの状態はWortmanninにの状態よりもっと安定になりって、自食体の形成も遮断できます。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA)は一種の選択性的なPI3K阻害剤で、HeLa細胞の中にVps34とPI3Kγに作用する時のIC50値が25μMと60μMに分かれることですが、I型PI3Kを永久性的に抑制しても、III型PI3Kを抑制することが一時になって、自食体の形成を遮断できます。

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101)は1種のセレクティブp110δ阻害剤です。無細胞試験で、IC50値は2.5 nMです。CAL-101 (Idelalisib, GS-1101)はp110δに表現する選択性はp110α/β/γに表現する選択性 より40-300倍が高くなって、C2β、hVPS34、DNA-PK とmTORに表現する選択性より400-4000倍が高くなります。

  • Wortmannin

    Wortmanninは一種の初めての命名されたPI3K阻害剤で、無細胞試験でこのIC50値が3 nMですが、PI3K家族に作用する選択性は低くて、自食体の形成を抑制し、無細胞試験でDNA-PK/ATMを有効に抑制する時のIC50値が16 nMと150 nMに分かれます。

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235,Dactolisib)は一種の二重ATP競争性PI3KとmTOR阻害剤で、無細胞試験でp110α/γ/δ/β/mTOR(p70S6K)を抑制する時のIC50値は 4 nM /5 nM /7 nM /75 nM /6 nMそれぞれ分かれます。BEZ235 (NVP-BEZ235,Dactolisib)はT3TopBP1-ER 細胞の中でATRを抑制して、IC50 値が21 nMになって、Akt とPDK1に作用することが弱くなります。臨床2期。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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