BKM120 (NVP-BKM120, Buparlisib)

BKM120 (NVP-BKM120, Buparlisib)は1種のセレクティブPI3K抑制剤で、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抑制剤で、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 NEPkVnpEgXSxdH;4bYMhSXO|YYm= MkPmO|IhcA>? MW\EUXNQ MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKEV3NEXLJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMECxOVgh|ryP NXj3NZh3OjR7MECyOlY>
DU145 M2nHZmN6fG:2b4jpZ{BCe3OjeR?= M4jvSlczKGh? Mn3JSG1UVw>? MnvmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCOS1KxJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMEC0N|Uh|ryP M4\DSlI1QTByMk[2
A2780 MmXOR5l1d3SxeHnjJGF{e2G7 M2[xfFczKGh? NGPo[mxFVVOR MmixR5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlM2KM7:TR?= NWL2S3BLOjR7MECyOlY>
U87MG NHTSdW5EgXSxdH;4bYMhSXO|YYm= M3K2bVczKGh? M2\qXWROW09? Ml:wR5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlk5KM7:TR?= NFnPco4zPDlyMEK2Oi=>
A2780 NYjNfpBpTnWwY4Tpc44hSXO|YYm= NFfhPIIyKGh? NETiTlVFVVOR NGfrWINKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNFU2KM7:TR?= MnHHNlQ6ODB{Nk[=
DU145 Mm\HSpVv[3Srb36gRZN{[Xl? MniyNUBp NEjUTI1FVVOR NHnQTG5KdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hTFVzNEWgZ4VtdHNiaHHyZo9zcW6pIFzLRlEhdXW2YYTpc44hf2m2aDDFR|UxKG:oIECuNFc{KM7:TR?= NGHCU2IzPDlyMEK2Oi=>
A2780 NEXTe|hHfW6ldHnvckBCe3OjeR?= NYnSfFR[OSCq MmjESG1UVw>? NY\5[GJ1UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2= MXyyOFkxODJ4Nh?=
MCF7 MkfJSpVv[3Srb36gRZN{[Xl? M{H3cFEhcA>? NXfFT2NJTE2VTx?= MkXNTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO NV7W[ZlYOjR7MECyOlY>
U87MG NX[1T4dwTnWwY4Tpc44hSXO|YYm= NHvFdpcyKGh? NVLSempOTE2VTx?= NGLmcplKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR|UxKG:oIECuNVMh|ryP NGXucZUzPDlyMEK2Oi=>
A2780 NECxZ5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq1O|IhcA>? MlnKSG1UVw>? MoHNSWM2OD1yLkWyJO69VQ>? MVmyOFkxODJ4Nh?=
SKMES-1 MnzQR5l1d3SxeHnjJGF{e2G7 NETuNG0yKM7:TR?= NYTSSZVpPzJiaB?= NI\nWmRKdmS3Y3XzJINmdGxiZHXheIg> M1PMVlI3ODF|M{G4
H596 MlnTSpVv[3Srb36gRZN{[Xl? M3rrVFEh|ryP MlrqTY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>? M{n1O|I3ODF|M{G4
HCC2450 M3[ye2Z2dmO2aX;uJGF{e2G7 MlTDNUDPxE1? NWm5NHRWUW2yYXnyd{Bk\WyuIHnueoF{cW:w M2\YXVI3ODF|M{G4
A549 NVPYfYZGTnWwY4Tpc44hSXO|YYm= MX21NFAhdk1? MV20PEBp MlvLSG1UVw>? NI\ReZFKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= MYGyOVk{PzJ7OR?=
A549 Ml3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PSWlEh|ryP M3u5PVczKGh? MXXEUXNQ M2LSRWlvcGmkaYTzJINmdGxiZ4Lve5Rp MmnSNlU6Ozd{OUm=
H522 M{DKV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF60[mkyKM7:TR?= NXfJV5VKPzJiaB?= M4rk[2ROW09? NIfNb|BKdmirYnn0d{Bk\WyuIHfyc5d1cA>? M1L0NFI2QTN5Mkm5
LNCaP M3nNVWZ2dmO2aX;uJGF{e2G7 Ml;rNUDPxE1? NITnWpVUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?= NFPibHkzPTN4MEe5PS=>
LNCaP95 NYn3OW5oTnWwY4Tpc44hSXO|YYm= MnjWNUDPxE1? MkW3V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? NUPQZYhVOjV|NkC3PVk>
HCT-15 NEfZSHRCeG:2b4Ppd{BCe3OjeR?= NV:xWm1ROTBizszN MnqwOFghcA>? NEDlflhFVVOR MXrJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MlLLNlUyPTJ{NEW=
HCT-116 M1nudWFxd3Sxc3nzJGF{e2G7 M3\PdlExKM7:TR?= M1TC[FQ5KGh? Mk\MSG1UVw>? M2PNN2lv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= M3fH[FI2OTV{MkS1
NCI-H460 MVjBdI91d3OrczDBd5NigQ>? Mn7BNVAh|ryP M2HkV|Q5KGh? NUntOphRTE2VTx?= M4WwTGlv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NVjBO2N{OjVzNUKyOFU>
SKOV-3 M2TUeGFxd3Sxc3nzJGF{e2G7 MV2xNEDPxE1? Mn31OFghcA>? M1K0WmROW09? MUHJcoR2[2W|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? M2\xXlI2OTV{MkS1
BSY-1 NUPt[HF4SXCxdH;zbZMhSXO|YYm= MYqxNEDPxE1? M2LTblQ5KGh? MYjEUXNQ Mnm2TY5lfWOnczDhdI9xfG:|aYOgbY4hSlO\LUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MnztNlUyPTJ{NEW=
MKN-1 M{GxR2Fxd3Sxc3nzJGF{e2G7 NULiS2ZxOTBizszN NWHWO2d1PDhiaB?= Mn7ISG1UVw>? MofGTY5lfWOnczDhdI9xfG:|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MWCyOVE2OjJ2NR?=
NCI-H522 MkXURZBwfG:|aYOgRZN{[Xl? MUGxNEDPxE1? MoH3OFghcA>? MmrwSG1UVw>? MlzaTY5lfWOnczDhdI9xfG:|aYO= MkTFNlUyPTJ{NEW=
OVCAR-3 NV3ZTodVSXCxdH;zbZMhSXO|YYm= NW\4XI5jOTBizszN MWS0PEBp NWfRWGx1TE2VTx?= NFPzTY9KdmS3Y3XzJIFxd3C2b4Ppdy=> MVOyOVE2OjJ2NR?=
HBC-5 MWXBdI91d3OrczDBd5NigQ>? MWCxNEDPxE1? M{Hr[lQ5KGh? NFrDUndFVVOR NFfwOWtKdmS3Y3XzJIFxd3C2b4Ppdy=> NXvTN2psOjVzNUKyOFU>
RXF-631L MVfBdI91d3OrczDBd5NigQ>? MWOxNEDPxE1? NGXtOmg1QCCq MoTXSG1UVw>? MlewTY5lfWOnczDhdI9xfG:|aYO= NFzqOJgzPTF3MkK0OS=>
MKN-45 NX\IT3oxSXCxdH;zbZMhSXO|YYm= NIDZc3kyOCEQvF2= NV\6W4x{PDhiaB?= MnXKSG1UVw>? NYTIXVY6UW6mdXPld{BieG:ydH;zbZM> NXu0UVQ{OjVzNUKyOFU>
BON-1 NWPwW5d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XWRVUxOCCwTR?= MlfNNVAh\A>? NXPBSFV{TE2VTx?= M3fi[mlvcGmkaYTzJINmdGxiZ4Lve5Rp M3;CTVI2ODJ4Mkmy
BON-1 NH60Z3pHfW6ldHnvckBCe3OjeR?= M3PHPVUxOCCwTR?= NHzOfZg1KGh? NIfxWIhFVVOR NG\OblBKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez NFLRSGEzPTB{NkK5Ni=>
QGP-1 NUTzZ5dYTnWwY4Tpc44hSXO|YYm= MX21NFAhdk1? NFKy[mE1KGh? MnnYSG1UVw>? M3nDXmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= M3TBUFI2ODJ4Mkmy
Huh7 M3TUVWZ2dmO2aX;uJGF{e2G7 MWSxJO69VQ>? NUDIUW5IOSCq NHjYXVZFVVOR MUnJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGPldlQ4PA>? NYLnXnVIOjVyMES0NFM>
BNL M3nLXmZ2dmO2aX;uJGF{e2G7 MYqxJO69VQ>? NXW4Wo1wOSCq NFmybZVFVVOR MU\Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Y> MlGyNlUxODR2MEO=
MDA-MB-175 NGj2S|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmxJO69VQ>? MoHMOUBl M2\pUmROW09? NGrhTGRKSzVyPEGg{txO MkXrNlQ5Pzl5OU[=
MDA-MB-134 M{nIUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV75W4RIOSEQvF2= MofQOUBl MW\EUXNQ MX\JR|UxRDFizszN MWOyOFg4QTd7Nh?=
HCC1500 NVL5N3Z{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXuxJO69VQ>? Mkf4OUBl NX3XSYZWTE2VTx?= Ml7NTWM2ODxzIN88US=> NGjpenEzPDh5OUe5Oi=>
EFM-19 NV\kVYQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvIcXMyKM7:TR?= MnLVOUBl NXnQVWhuTE2VTx?= Ml3LTWM2ODxzIN88US=> MoTmNlQ5Pzl5OU[=
ZR-75-30 NHfiN|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\FNUDPxE1? NYnqeXlXPSCm M2LZUmROW09? MVPJR|UxRDFizszN NVHSSYZmOjR6N{m3PVY>
MDA-MB-361 M{Lqdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLFNUDPxE1? MWm1JIQ> MX\EUXNQ M2ixV2lEPTB:MTFOwG0> M17GXlI1QDd7N{m2
T-47D MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXYTHIyOSEQvF2= NWHjfoRVPSCm M{XOTGROW09? MXfJR|UxRDFizszN MorTNlQ5Pzl5OU[=
SK-BR-3 M13Dd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4OxfFEh|ryP MW[1JIQ> MmjuSG1UVw>? NV7X[4hFUUN3MEyxJO69VQ>? M3;vNlI1QDd7N{m2
UACC-732 NXLMeoFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4n5V|Eh|ryP NIrBfGQ2KGR? NVizO|dCTE2VTx?= MXHJR|UxRDFizszN NVT0PYFjOjR6N{m3PVY>
BT-474 NVfEU5N6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmxJO69VQ>? M3rGeFUh\A>? NGTVbYRFVVOR M2\lPGlEPTB:MTFOwG0> NHnvcI8zPDh5OUe5Oi=>
HCC202 NUjTdIxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLUfoQyKM7:TR?= Mmm1OUBl M1[xXGROW09? NHfhdFNKSzVyPEGg{txO NEHxSGIzPDh5OUe5Oi=>
MCF7 NWfyNFB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV2xJO69VQ>? NYKyTZR{PSCm M{jIfGROW09? M1n3bWlEPTB:MTFOwG0> NGjOTo0zPDh5OUe5Oi=>
MDA-MB-415 M335cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTmW3IyKM7:TR?= NWjJNlRMPSCm NWTVV|ZQTE2VTx?= NX7RfYk1UUN3MEyxJO69VQ>? MnnMNlQ5Pzl5OU[=
MDA-MB-453 MljOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWThbFUxOSEQvF2= M1Xx[lUh\A>? MnHPSG1UVw>? NV\BeGljUUN3MEyxJO69VQ>? MWOyOFg4QTd7Nh?=
ZR-75-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2xJO69VQ>? M1XncFUh\A>? MVjEUXNQ NWD2TZY4UUN3MEyxJO69VQ>? NIHMe5MzPDh5OUe5Oi=>
HCC38 NEHjfFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPlNUDPxE1? M{m5XFUh\A>? M1;LZmROW09? NFXidIRKSzVyPEGg{txO MWOyOFg4QTd7Nh?=
HCC1419 NUTobYZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLuNUDPxE1? NUP0PZNjPSCm M1\hNWROW09? NH\QXm9KSzVyPEGg{txO MYSyOFg4QTd7Nh?=
UACC-812 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\T[VEh|ryP NEDodJc2KGR? M2nFSGROW09? M3fxemlEPTB:MTFOwG0> MVuyOFg4QTd7Nh?=
HCC1187 M3P2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xJO69VQ>? NVnx[ZVJPSCm MVnEUXNQ MmrCTWM2ODxzIN88US=> NYnoS|VsOjR6N{m3PVY>
KPL-1 MlvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHKUZEyKM7:TR?= NWrOdXZ6PSCm MULEUXNQ M{XYZWlEPTB:MTFOwG0> MVuyOFg4QTd7Nh?=
SUM-225 NVLrU|hVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;TNUDPxE1? NYn0cWVIPSCm M3PHfmROW09? NHjXeWtKSzVyPEGg{txO NYPOWmMyOjR6N{m3PVY>
EFM-192A MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjQNUDPxE1? MlHPOUBl NH;IbVhFVVOR M4HwbWlEPTB:MTFOwG0> MXyyOFg4QTd7Nh?=
JIMT-1 NXH6Vlh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoD5NUDPxE1? MUe1JIQ> NWC2eJZ3TE2VTx?= M{LIW2lEPTB:MTFOwG0> NXjWZnNQOjR6N{m3PVY>
HCC1143 M4LWO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6xJO69VQ>? NYLaR5pkPSCm M3zxb2ROW09? M13GdWlEPTB:MTFOwG0> NGr0cGwzPDh5OUe5Oi=>
HCC2218 MoS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XZ[FEh|ryP NYfoPIJ1PSCm MoqwSG1UVw>? MX;JR|UxRDFizszN NGjYNVUzPDh5OUe5Oi=>
MDA-MB-468 MlfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rZZ|Eh|ryP NHfiT5o2KGR? NHyzW2hFVVOR NV\UdXBIUUN3MEyxJO69VQ>? NWnmfWR7OjR6N{m3PVY>
BT-20 Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mom5NUDPxE1? NVjwNWF6PSCm Ml;rSG1UVw>? Moi1TWM2ODxzIN88US=> NXTx[FdDOjR6N{m3PVY>
MDA-MB-435 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\yNUDPxE1? NFf6bGo2KGR? M4rNVGROW09? MlS2TWM2ODxzIN88US=> MUiyOFg4QTd7Nh?=
BT-549 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG4NUDPxE1? NUnLUokxPSCm MYnEUXNQ MXjJR|UxRDFizszN NIfI[oEzPDh5OUe5Oi=>
HCC1806 NUTnZoFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknPNUDPxE1? MUm1JIQ> M{ezNWROW09? MlzJTWM2ODxzIN88US=> NH65N|kzPDh5OUe5Oi=>
HCC1937 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mne1NUDPxE1? M4m2dlUh\A>? MnznSG1UVw>? MlPQTWM2ODxzIN88US=> NWjrbnhyOjR6N{m3PVY>
Hs578T MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi0fYEyKM7:TR?= MYq1JIQ> MlLRSG1UVw>? NFuzS5BKSzVyPEGg{txO M4PWNVI1QDd7N{m2
LN18 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2GxNVIxKM7:TR?= NV;mO2p7PzJiaB?= MUjEUXNQ M4fwbmlEPTB:NTFOwG0> NU\VTIhrOjR5NEGwO|Q>
LN229 NHLRRnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGxeZUzOCEQvF2= NUXDPYhsPzJiaB?= NICyXY5FVVOR NYXne21WUUN3MEy1JO69VQ>? NUfYdm1FOjR5NEGwO|Q>
LNZ308 NH;Q[2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvicVIzOCEQvF2= MnrQO|IhcA>? NWDFOoxLTE2VTx?= M4jtOmlEPTB:NTFOwG0> NEHWWI0zPDd2MUC3OC=>
T98G MlLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGyNEDPxE1? M3;SeFczKGh? NGXPWmZFVVOR NUXMbmFCUUN3MEy1JO69VQ>? MlP6NlQ4PDFyN{S=
U87 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXyyNEDPxE1? M1zLPVczKGh? MWLEUXNQ MXfJR|UxRDVizszN MV[yOFc1OTB5NB?=
LN18 MnzmSpVv[3Srb36gRZN{[Xl? NWjVR5M4PSEQvF2= M3;qXVI1KGh? Mn3vSG1UVw>? Ml\BTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MViyOFc1OTB5NB?=
LNZ308 NYPFTI5UTnWwY4Tpc44hSXO|YYm= MYO1JO69VQ>? MkXvNlQhcA>? MVfEUXNQ MmDKTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MlLTNlQ4PDFyN{S=
Saos-2 M{jpUWZ2dmO2aX;uJGF{e2G7 M3vvNVUxKM7:TR?= NXP2VW9kPDhiaB?= M2ThdWlvcGmkaYTzJINmdGxiaX72ZZNqd25? M1Sxd|I1PzJ5Nk[w
MG-63 NVr2XHFETnWwY4Tpc44hSXO|YYm= NYnMN45rPTBizszN M1vz[lQ5KGh? NF7EcVJKdmirYnn0d{Bk\WyuIHnueoF{cW:w MUeyOFczPzZ4MB?=
SJSA-1 M1XE[WZ2dmO2aX;uJGF{e2G7 MXq1NEDPxE1? NHfsbVc1QCCq NVvXUVhKUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= Mli1NlQ4Ojd4NkC=
Saos-2 NEjZeIhHfW6ldHnvckBCe3OjeR?= M2TQc|UxKM7:TR?= NIPRRmQ1QCCq M1vTV2lvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> NUnuUYhtOjR5Mke2OlA>
MG-63 NUDiZ2dlTnWwY4Tpc44hSXO|YYm= NGLOUFY2OCEQvF2= MUi0PEBp NYLPT5plUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? MV[yOFczPzZ4MB?=
SJSA-1 NWTFe5VVTnWwY4Tpc44hSXO|YYm= NYiyZoNmPTBizszN NHS5d3o1QCCq MlO2TY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> NH3l[4UzPDd{N{[2NC=>
Saos-2 MkLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f5S|UxKM7:TR?= Ml3xOFghcA>? Ml\2TY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? MWSyOFczPzZ4MB?=
MG-63 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX61NEDPxE1? M3zyUFQ5KGh? NHLVcVlKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= Ml3qNlQ4Ojd4NkC=
SJSA-1 MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3zelE2OCEQvF2= NXXERWFbPDhiaB?= M1PB[mlvcGmkaYTzJINmdGxidnnhZoltcXS7 M3TMV|I1PzJ5Nk[w
FaDu MUTGeY5kfGmxbjDBd5NigQ>? NV\3dplrPSEQvF2= MkXLNlQhcA>? MknySG1UVw>? MWnS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= M2rXbVI1PjNzMUS3
EMT6 NUXw[lBRTnWwY4Tpc44hSXO|YYm= MlHyOUDPxE1? M3\YclI1KGh? NWDL[GpPTE2VTx?= NGjS[VdT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> M2HXNlI1PjNzMUS3
HCT116 MmfxSpVv[3Srb36gRZN{[Xl? NITDN3M2KM7:TR?= M4jJ[lI1KGh? NWLBUmx3TE2VTx?= Mmr0VoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= NXTPb|dVOjR4M{GxOFc>
U87 M{K1dGZ2dmO2aX;uJGF{e2G7 MUS1JO69VQ>? MXKyOEBp MUXEUXNQ NIi2OGVT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> NH;Qd4czPDZ|MUG0Oy=>
GBM NXn5UWs6SXCxcITvd4l{KEG|c3H5 M3;wVVLPxE1? M1ziZ|Q5cA>? NHrybmlFVVOR MnfIbY5lfWOnZDDobYdp\XJibHX2[Yx{KG:oIHHwc5B1d3OrczygZY5lKGSnY4LlZZNm\CClZXzsJJZq[WKrbHn0fS=> NIe2O4UzPDVyMES5Ni=>
BON M{K5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TBXVEuPc7:TR?= NH73T3Y4Omh? MkC2[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NW\RdHhTOjR2NEO1NlM>
BON NEXRW2lCeG:ydH;zbZMhSXO|YYm= NULuO4xsOS13zszN NGLxc|AzPGh? M1rQU4lv[3KnYYPld{BieG:ydH;zbZM> M2T4c|I1PDR|NUKz
H1975 M{\UXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;jNE4{NTlwNt88US=> NGjwRVg4Omh? NWK4cI9GTE2VTx?= MY\JR|UxRTFwM{i1{txO MXOyOFM{Pzh2Nh?=
H1975 M33rWGFxd3C2b4Ppd{BCe3OjeR?= M{TNWlLPxE1? MlrJNlRp NFLld49FVVOR MV7pcoNz\WG|ZYOgZZBweHSxc3nzJJJifGVic3nncolncWOjboTsfS=> MmDONlQ{Ozd6NE[=
T-ALL NGfWPXpCeG:ydH;zbZMhSXO|YYm= NVr5cFhm[mW2d3XlckAyNjRiYX7kJFUvOyCvTTDheEAzPGhiYX7kJFAvQSCjbnSgOU42KG2PIHH0JFQ5cCCrbjDkbYZn\XKnboSgZ4VtdCCuaX7l MlvUNlQhd3JiNEjo MoTtSG1UVw>? MWLh[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= NF7hNGkzPDNzMEezOi=>
BCR-ABL MlziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfhSJoxNjJ3LUGw{txO MUG0[C=> NFPW[Jd{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w Mn3aNlQzPDR4MUK=
LC-1/SQSF M3\CUmZ2dmO2aX;uJGF{e2G7 M1KxdVPPxE1? NW[0U5lGOjSq M{DyOmROW09? MX3k[YNz\WG|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy= M{nhO|I{QThyMEmz
Primary CLL cells NH;EbZdCeG:ydH;zbZMhSXO|YYm= MYKxMVEx|ryP NGft[nE1QGh? M1O5[Ilv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> NIfwRlAzOzh3MEiwOy=>
Primary CLL cells NUTwZWxoU2mwYYPlJGF{e2G7 Mk[4Nu69VQ>? NV\zT2ZpOzCvaX6= NH3ETHBl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= M3XOPVI{QDVyOEC3
Primary CLL cells NXHVSnl1S3m2b4TvfIlkKEG|c3H5 MUKy{txO NXr5N4lkOjSq NVrCPZdJcW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=> M3z1PVI{QDVyOEC3
human NSCLC cell lines NY[wRmx7SXCxcITvd4l{KEG|c3H5 NFy1NHoxNjF{NT20{txO MWKyOIg> M4nFVGROW09? M1fheWlEPTC|IILhcodmeyCocn;tJFAvPC1{zszN M1PzUFI{PTZ{NEey
human HCC cell lines M33Fb2NmdGxidnnhZoltcXS7IHHzd4F6 MlvjNE4xODVvMd88US=> NGDXN|M1QGh? MmX0TWM2OD1zzszN M4HrXVI{PDh7OUm5
Huh7 NWezb29QU2mwYYPlJGF{e2G7 NIm4dVAy|ryP NWPJUmZYPDiq M33EOpNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> Mk\SNlM1QDl7OUm=
SK-HEP1 M4njfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP2NU0zOM7:TR?= M4DWRlczcA>? Mlm4SG1UVw>? NFvRTZhKSzVy78{cNe69VQ>? MnHiNlM1PzlzM{[=
786-0 NUjjOW8{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO3NU0zOM7:TR?= NVOxOIQzPzKq M3;WTGROW09? MX3JR|Ux97zeMd88US=> NXy4VY9bOjN2N{mxN|Y>
JVM2 MWjDfZRwfG:6aXPpeJkh[XO|YYm= NY\BTIo6OC5{LUKw{txO MnfmO|Jp M1;sU2ROW09? NWnQfpdtUUN3ME2wMlnPxE1? M4nuOlI{OjN6NkO5
EHEB M2DIWmN6fG:2b4jpZ4l1gSCjc4PhfS=> MnLINE4zNTJyzszN NVfIS|VVPzKq NIrWNIVFVVOR MoXOTWM2OD1yLkhOwG0> NIfhbY8zOzJ|OE[zPS=>
MEC2 NWG2eoM2S3m2b4TvfIlkcXS7IHHzd4F6 NInQO3YxNjJvMkFOwG0> MV[3Nog> M2jDbGROW09? NGfMO4pKSzVyPUCuO:69VQ>? MXqyN|I{QDZ|OR?=
primary B-CLL lymphocytes MXPBdI9xfG:|aYOgRZN{[Xl? NFfDSnFKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n Mom3NlRp M3jWVmROW09? M{D0[mlEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM> Ml;MNlMzOzh4M{m=
primary B-CLL lymphocytes NXziPGpxU2mwYYPlJGF{e2G7 MoPPTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? NEHaUZYzPGh? M1zsRYlvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u NVmzV5o1OjN{M{i2N|k>
human NSCLC M2rCdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnNZppCOC53LUNOwG0> NVvDbIRxPzKq Mmm4TWM2OD1zzszN NHvyfnYzOjd6MUO5Ny=>
human NSCLC MWDLbY5ie2ViQYPzZZk> NEjSd|Ey|ryP Mny0NlRp NULiRVIycW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=> NGHGNI4zOjd6MUO5Ny=>
Y1 cell line NVrxXph5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHOdIwxNjIQvF2vNe69VQ>? NWW4[Gx4OjSq MorHSG1UVw>? NHvGT3RqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?= MUiyNlY6OjlyNB?=
PIK3CA-mutant MCF7 NX;QZopRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrJS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? MUS3Nog> NUXsUm83T0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= MoPqNlI3PTN7Nke=
PIK3CA-mutant MCF7 NHrwNItMcW6jc3WgRZN{[Xl? MoS1TWM2OD1zMUVCtVNvVQ>? NUTJT2J1PzKq MYHJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| NIrOUoszOjZ3M{m2Oy=>
MCF7-myr-Akt Ml\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLtS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? MnnXO|Jp MWLHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? MUiyNlY2Ozl4Nx?=
colon cancer cell lines M4\SXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHabFExNTFyzszN MXK3Nog> NFvFfZBFVVOR M1P0TGlEPTB;Md88US=> NUHmTnByOjJ3NEO4OVc>
gastric cancer cell lines NX24[GNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDCNE0yOM7:TR?= MUS3Nog> M4jlcWROW09? NVj1cWtRUUN3ME2yMVXPxE1? NYDybnk1OjJ3NEO4OVc>
HCT-116/HT-29/MKN-45 NFrLcpVCeG:ydH;zbZMhSXO|YYm= MkfYNu69VQ>? Ml;hOFhp Mofhd4hq\nRiaX6gS|IheGijc3W= MWCyNlU1Ozh3Nx?=
HT-29 and HCT-116 NXHSTXYyS2G|cHHz[UBie3OjeR?= NHfvPJg2|ryP NUXEcXp[OjSq NF75OmpqdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm= NVXpelFKOjJ3NEO4OVc>
MM cell lines NYXnbXFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPVNVDPxE1? NXTOcXRnOjSq NHGxd3lFVVOR M1vY[GlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? NInqfGMzOjJyN{S4OS=>
ARP-1 NF\mZZBCeG:ydH;zbZMhSXO|YYm= M4XXRVEx|ryP NUG3d4lZOjSq NID2UFRFVVOR MV;pcoR2[2W|IF3NJINmdGxiYYDvdJRwe2m|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w NXq2O4JxOjJ{MEe0PFU>
SNU-601 NFTDPHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHPO|Jp M3HsRmROW09? MYnJR|UxRTBwOEG2xtExNjB4M988US=> MnjHNlIyPTl6MUS=
SNU-1 NIPK[mFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7Ec5M4Omh? NGG1XYNFVVOR MV\JR|UxRTFwMEiyxtExNjB{ON88US=> M16y[|IzOTV7OEG0
SNU-668 NIjQOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rOd|czcA>? MXLEUXNQ MVHJR|UxRTFwNUe5xtExNjB5NN88US=> NIi0b|UzOjF3OUixOC=>
AGS MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn5fWY4Omh? M3TabGROW09? MnzmTWM2OD1zLkexOOKyOC5zMUhOwG0> MWSyNlE2QThzNB?=
SNU-216 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljXO|Jp NEfz[WVFVVOR NI\3RW5KSzVyPUKuOlkzyrFyLkC4Nu69VQ>? MmTxNlIyPTl6MUS=
SNU-5 NUHMToNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfFTIs4Omh? M3rW[GROW09? M3PyU2lEPTB;MT6zOVHDuTBwMEmx{txO MUCyNlE2QThzNB?=
SNU-638 NUPwNItLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfQO|Jp NFz4[ppFVVOR NXnudo5IUUN3ME2yMlI5OsLzMD6wOVPPxE1? M4LLRlIzOTV7OEG0
SNU-16 NFXyTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDDfGlFPzKq NWTmVohZTE2VTx?= MWjJR|UxRTFwNUezxtExNjByMd88US=> M4O0PFIzOTV7OEG0
SNU-484 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfMRmRNPzKq MYrEUXNQ M1e3UGlEPTB;MT63NljDuTBwMES1{txO MXyyNlE2QThzNB?=
SNU-620 NXr0VYdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XncVczcA>? NX[zZ4xETE2VTx?= M{H2XWlEPTB;Mj65N|nDuTBwMECx{txO NHTkc2YzOjF3OUixOC=>
SNU-719 NILURo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PBelczcA>? M4Xa[WROW09? NVv0OGZ7UUN3ME2zMlA{P8LzMD6wN|LPxE1? Mm[5NlIyPTl6MUS=
glioma cell lines M4naUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPub5JyPzKq M{TUVGlEPTB;MT2y{txO M1HBblIzODZ3MEiw
U87 NGrJTIlCeG:ydH;zbZMhSXO|YYm= MnzCNu69VQ>? NVzVPGFSPzKq Mln3bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= MlrtNlIxPjVyOEC=

... 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)

技術サポート&よくある質問(FAQ)

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    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147)

    Pilaralisib (XL147)は一種の選択性的で、可逆なI型PI3K抑制剤で、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抑制剤です。

  • PI-3065

    PI-3065は一種の選択性p110δ抑制剤で、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は初めの合成で、PI3Kα/δ/βを抑制することが分かった小分子です。無細胞試験で、IC50値は0.5 μM/0.57 μM/0.97 μMそれぞれに分かれます。尚、溶液にの状況はワートマニン(Wortmannin)にの状況よりもっと安定になって、自食胞の形成も遮断できます。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA)は1種の選択性PI3K抑制剤で、HeLa細胞の中で、Vps34とPI3Kγに作用する時のIC50値は25μMと60μMです。3-Methyladenine (3-MA)はI型PI3Kを永遠に抑制しますが、III型PI3Kを一時に抑制して、自食体の形成も遮断します。

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101)は1種のセレクティブp110δ抑制剤です。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、初めに命名されたPI3K抑制剂で、無細胞試験でIC50値が3 nMになって、PI3K家族に作用する選択性が弱くて、自食体の形成も抑制して、DNA-PK/ATMも有効に抑制して、無細胞試験で、このIC50値が16 nMと150 nMになります。

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235,Dactolisib)は一種の二重ATP競争性PI3KとmTOR抑制剤で、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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