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 M4jqPGN6fG:2b4jpZ{BCe3OjeR?= MYi3NkBp NHjjb3RFVVOR NF3H[|hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN NYLtN5drOjR7MECyOlY>
DU145 NXPw[ZA5S3m2b4TvfIlkKEG|c3H5 MoLCO|IhcA>? MniySG1UVw>? MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1? NWi5R2l[OjR7MECyOlY>
A2780 MW\DfZRwfG:6aXOgRZN{[Xl? Mlj2O|IhcA>? M2K4bmROW09? MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N|Uh|ryP MYWyOFkxODJ4Nh?=
U87MG NXzGXod3S3m2b4TvfIlkKEG|c3H5 MX:3NkBp M2jMUmROW09? Mke2R5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlk5KM7:TR?= NXvhR25mOjR7MECyOlY>
A2780 NXvNelhXTnWwY4Tpc44hSXO|YYm= MX2xJIg> MVjEUXNQ MnzwTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkC1OUDPxE1? M{PDWlI1QTByMk[2
DU145 NXTsZZBZTnWwY4Tpc44hSXO|YYm= NUjqRpgzOSCq NXfa[oZwTE2VTx?= MX3Jcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>? MorNNlQ6ODB{Nk[=
A2780 Mlu5SpVv[3Srb36gRZN{[Xl? MYexJIg> MWrEUXNQ NY\rc5NYUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2= NVHndmpDOjR7MECyOlY>
MCF7 MXnGeY5kfGmxbjDBd5NigQ>? NGjnN2syKGh? NIX1fWZFVVOR NXqxdFkzUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh|ryP M1LjSlI1QTByMk[2
U87MG NVX2e|VpTnWwY4Tpc44hSXO|YYm= MUexJIg> NXP2SYRKTE2VTx?= M{[xOGlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1? MYmyOFkxODJ4Nh?=
A2780 M3nQXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\i[lczKGh? NGDOeYFFVVOR M3nuSWVEPTB;MD61NkDPxE1? M3X3WVI1QTByMk[2
SKMES-1 M4Toc2N6fG:2b4jpZ{BCe3OjeR?= NWjaUVVMOSEQvF2= NVfhNJJ{PzJiaB?= MYXJcoR2[2W|IHPlcIwh\GWjdHi= M{T5cFI3ODF|M{G4
H596 MoPYSpVv[3Srb36gRZN{[Xl? M{HLdVEh|ryP M1[1NmlueGGrcoOgZ4VtdCCvaXfyZZRqd25? NULFSlNMOjZyMUOzNVg>
HCC2450 NF\HZ4FHfW6ldHnvckBCe3OjeR?= NXrMeVN1OSEQvF2= NHS4Z4FKdXCjaYLzJINmdGxiaX72ZZNqd25? Mmr5NlYxOTN|MUi=
A549 NUO3UmpNTnWwY4Tpc44hSXO|YYm= MUS1NFAhdk1? MVi0PEBp M{\WTWROW09? NWm0WnhpUW6qaXLpeJMhSWu2IHHjeIl3[XSrb36= NUHzTYRZOjV7M{eyPVk>
A549 M2n0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvnV4kyKM7:TR?= MUC3NkBp MXHEUXNQ M3vIW2lvcGmkaYTzJINmdGxiZ4Lve5Rp NVXlZVJXOjV7M{eyPVk>
H522 M2HLSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYH4UVNXOSEQvF2= M3HVXFczKGh? NFe5cXdFVVOR MkPZTY5pcWKrdIOgZ4VtdCCpcn;3eIg> Mor4NlU6Ozd{OUm=
LNCaP M1\NT2Z2dmO2aX;uJGF{e2G7 M2DmOVEh|ryP MnrnV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? MlW4NlU{PjB5OUm=
LNCaP95 M4jqbGZ2dmO2aX;uJGF{e2G7 MlnxNUDPxE1? NWjUSJpUW3WycILld5NmeyCyLVHLWEBt\X[nbIO= M2\YdlI2OzZyN{m5
HCT-15 MX3BdI91d3OrczDBd5NigQ>? M2j3elExKM7:TR?= NIDDN481QCCq MVPEUXNQ MXzJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MoTnNlUyPTJ{NEW=
HCT-116 MVzBdI91d3OrczDBd5NigQ>? M3jFNlExKM7:TR?= NWDjcnJrPDhiaB?= Ml3USG1UVw>? MWTJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? NGT4bXozPTF3MkK0OS=>
NCI-H460 MYPBdI91d3OrczDBd5NigQ>? NWTYUGt2OTBizszN MXy0PEBp NXvCcY9rTE2VTx?= NYTBV5dQUW6mdXPld{BieG:ydH;zbZMhcW5iTlPJMWg1PjBiY3XscJMhcGG{Yn;1dolv\yCSSVuzR2EhcG:2c4DveEBufXSjdHnvci=> M3LaZ|I2OTV{MkS1
SKOV-3 MUjBdI91d3OrczDBd5NigQ>? NUm4S4VLOTBizszN NUny[HV6PDhiaB?= MYXEUXNQ M1\aVGlv\HWlZYOgZZBweHSxc3nzJIlvKFONT2[tN{Bk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w M1;CelI2OTV{MkS1
BSY-1 MWHBdI91d3OrczDBd5NigQ>? NXPGV3piOTBizszN NXLFNJVUPDhiaB?= M{H4cWROW09? M4[4b2lv\HWlZYOgZZBweHSxc3nzJIlvKEKVWT2xJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? M2ewRVI2OTV{MkS1
MKN-1 M1;EOGFxd3Sxc3nzJGF{e2G7 NXu5PY9lOTBizszN MV20PEBp MVPEUXNQ NGXzNm1KdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MlHINlUyPTJ{NEW=
NCI-H522 NYjM[W4zSXCxdH;zbZMhSXO|YYm= M1vDZVExKM7:TR?= NWrkfVgyPDhiaB?= M4DpOGROW09? MWPJcoR2[2W|IHHwc5B1d3Orcx?= NITXO4wzPTF3MkK0OS=>
OVCAR-3 MUjBdI91d3OrczDBd5NigQ>? NFzxTGcyOCEQvF2= NVXWPYdXPDhiaB?= MWnEUXNQ MYHJcoR2[2W|IHHwc5B1d3Orcx?= NIHlelgzPTF3MkK0OS=>
HBC-5 MkDCRZBwfG:|aYOgRZN{[Xl? MVGxNEDPxE1? NE\he4U1QCCq MkXDSG1UVw>? NIC0OmdKdmS3Y3XzJIFxd3C2b4Ppdy=> MVOyOVE2OjJ2NR?=
RXF-631L M4Ty[2Fxd3Sxc3nzJGF{e2G7 Ml;qNVAh|ryP MorNOFghcA>? MWTEUXNQ M{fLcWlv\HWlZYOgZZBweHSxc3nz M1\vblI2OTV{MkS1
MKN-45 MXHBdI91d3OrczDBd5NigQ>? M{DzOlExKM7:TR?= NXPiSYJoPDhiaB?= Mmj6SG1UVw>? NHW4fWhKdmS3Y3XzJIFxd3C2b4Ppdy=> NGTQd4UzPTF3MkK0OS=>
BON-1 M{nKO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX1OVAxKG6P NXjWRopHOTBiZB?= NYfFNZhlTE2VTx?= MX;Jcohq[mm2czDj[YxtKGe{b4f0bC=> NXrzbopUOjVyMk[yPVI>
BON-1 NX7zVGFqTnWwY4Tpc44hSXO|YYm= Mo\FOVAxKG6P NGnpWZQ1KGh? M4T5[mROW09? NIj1PHdKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez M2rtPFI2ODJ4Mkmy
QGP-1 NV;FSHo4TnWwY4Tpc44hSXO|YYm= NYniXnNKPTByIH7N NXixRWZqPCCq MYLEUXNQ NHfEe25KdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez M4fHblI2ODJ4Mkmy
Huh7 MVHGeY5kfGmxbjDBd5NigQ>? M1vsW|Eh|ryP NHTKZ3gyKGh? NGLyS2NFVVOR M2nqdGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgV4VzPDd2 NWXhUFVkOjVyMES0NFM>
BNL NHjIc3ZHfW6ldHnvckBCe3OjeR?= Mkj3NUDPxE1? M3rhOVEhcA>? NULuOWxETE2VTx?= NU\CNphRUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4 MYGyOVAxPDRyMx?=
MDA-MB-175 MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGG0cGEyKM7:TR?= MnjUOUBl MoDmSG1UVw>? NFTjRoRKSzVyPEGg{txO NFrHSVMzPDh5OUe5Oi=>
MDA-MB-134 M1fYWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHSx[ZAyKM7:TR?= MWK1JIQ> MoWwSG1UVw>? MmjnTWM2ODxzIN88US=> MVGyOFg4QTd7Nh?=
HCC1500 MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1K1[lEh|ryP M{O1cVUh\A>? NWjCe2dCTE2VTx?= NHLqR4tKSzVyPEGg{txO MXSyOFg4QTd7Nh?=
EFM-19 NWPsXVdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnJcYxbOSEQvF2= M{LTNFUh\A>? M3nte2ROW09? NXewfmJQUUN3MEyxJO69VQ>? M2TIcFI1QDd7N{m2
ZR-75-30 NXu5V5N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jGNlEh|ryP NVL3N3ZYPSCm MlvESG1UVw>? NH23SlNKSzVyPEGg{txO MYWyOFg4QTd7Nh?=
MDA-MB-361 NUfFO3ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnxVHhKOSEQvF2= NHuwOo82KGR? Mn76SG1UVw>? NXPJfGVCUUN3MEyxJO69VQ>? NXLnS3hMOjR6N{m3PVY>
T-47D MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHhdHozOSEQvF2= M1LTd|Uh\A>? M4npOWROW09? NEHGUVFKSzVyPEGg{txO M1H4SFI1QDd7N{m2
SK-BR-3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTRNlBDOSEQvF2= M4jESVUh\A>? NH7BOWxFVVOR NF\SW45KSzVyPEGg{txO MVqyOFg4QTd7Nh?=
UACC-732 NXLuPGdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHpWFUyKM7:TR?= NF3BO5E2KGR? NWnrSG51TE2VTx?= NEC4bnJKSzVyPEGg{txO MUCyOFg4QTd7Nh?=
BT-474 MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInyR4YyKM7:TR?= NH\oPG42KGR? MnfWSG1UVw>? NYfXTZhCUUN3MEyxJO69VQ>? MkjKNlQ5Pzl5OU[=
HCC202 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7sbIkyKM7:TR?= MXK1JIQ> NGrxcYJFVVOR NUfuZXZ7UUN3MEyxJO69VQ>? M1zjUFI1QDd7N{m2
MCF7 Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSxJO69VQ>? NWjUS3JuPSCm M2rBWGROW09? MlzPTWM2ODxzIN88US=> M1HvcVI1QDd7N{m2
MDA-MB-415 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\nNUDPxE1? NX3mUJE{PSCm MmWySG1UVw>? NHXPPI5KSzVyPEGg{txO NVfVTHlnOjR6N{m3PVY>
MDA-MB-453 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fRbFEh|ryP MXq1JIQ> MnzsSG1UVw>? NV\ycoJ[UUN3MEyxJO69VQ>? MlTONlQ5Pzl5OU[=
ZR-75-1 NYPleY43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHZUmVZOSEQvF2= Ml3sOUBl M4W3VmROW09? MY\JR|UxRDFizszN NV\uOVM4OjR6N{m3PVY>
HCC38 NE\re3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DxelEh|ryP NEG5eFk2KGR? NVzuNJE6TE2VTx?= Ml3ITWM2ODxzIN88US=> NGraepQzPDh5OUe5Oi=>
HCC1419 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2xJO69VQ>? NEfWcWI2KGR? NXfXfFBTTE2VTx?= MVjJR|UxRDFizszN MoCwNlQ5Pzl5OU[=
UACC-812 NG\3OXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWxJO69VQ>? MXi1JIQ> NFq2fWtFVVOR NYnHXJRqUUN3MEyxJO69VQ>? MYKyOFg4QTd7Nh?=
HCC1187 M2Dlfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvINUDPxE1? MYi1JIQ> MYTEUXNQ MXzJR|UxRDFizszN NEXjV4MzPDh5OUe5Oi=>
KPL-1 NIP1WIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXCcYtFOSEQvF2= MkDYOUBl MmLjSG1UVw>? MX;JR|UxRDFizszN NGXVWGozPDh5OUe5Oi=>
SUM-225 MnXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfoVY4yKM7:TR?= MnrFOUBl MX;EUXNQ MXfJR|UxRDFizszN M4LhVVI1QDd7N{m2
EFM-192A MnPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnoNUDPxE1? MlK5OUBl M2XYfmROW09? NGrGO29KSzVyPEGg{txO NYOzW2txOjR6N{m3PVY>
JIMT-1 NFzHSmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;zfJEyKM7:TR?= NXPMblhiPSCm MVPEUXNQ NXLz[ZBoUUN3MEyxJO69VQ>? NEezNIIzPDh5OUe5Oi=>
HCC1143 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PONlEh|ryP MXe1JIQ> M3f4c2ROW09? M{HlTmlEPTB:MTFOwG0> M3z0NVI1QDd7N{m2
HCC2218 NVvKOWp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K1V|Eh|ryP MXq1JIQ> NEjKfoNFVVOR MYXJR|UxRDFizszN MXOyOFg4QTd7Nh?=
MDA-MB-468 MlHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIX1PXoyKM7:TR?= NGTUdo82KGR? MWPEUXNQ NHm1SnVKSzVyPEGg{txO NF[1RmczPDh5OUe5Oi=>
BT-20 NGnQPJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nLZVEh|ryP NW\ZbI5RPSCm NI\rSlFFVVOR MYDJR|UxRDFizszN MmriNlQ5Pzl5OU[=
MDA-MB-435 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGxJO69VQ>? NUK3Ro5rPSCm NGrVcIRFVVOR MUDJR|UxRDFizszN MVqyOFg4QTd7Nh?=
BT-549 MlT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrTNFJuOSEQvF2= MkS4OUBl M1nBVGROW09? NEftZ2JKSzVyPEGg{txO MXWyOFg4QTd7Nh?=
HCC1806 NGLPXWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PwVVEh|ryP NITEbJI2KGR? NIHZepRFVVOR NELMOYhKSzVyPEGg{txO NIXOepgzPDh5OUe5Oi=>
HCC1937 NGnDU3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\hTVEh|ryP MVS1JIQ> M3fXXWROW09? MV7JR|UxRDFizszN M376VVI1QDd7N{m2
Hs578T MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml21NUDPxE1? MWS1JIQ> NFft[ZdFVVOR MXXJR|UxRDFizszN MUKyOFg4QTd7Nh?=
LN18 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3La[|IxKM7:TR?= NUHvVZF4PzJiaB?= MmfMSG1UVw>? NXf2eG8{UUN3MEy1JO69VQ>? MlnQNlQ4PDFyN{S=
LN229 M4TwTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXjO|F7OjBizszN NWH1N5VKPzJiaB?= MYTEUXNQ MoPPTWM2ODx3IN88US=> MY[yOFc1OTB5NB?=
LNZ308 M2DGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDZXYczOCEQvF2= NV3JSFFqPzJiaB?= Mlz2SG1UVw>? Mmn3TWM2ODx3IN88US=> MkfrNlQ4PDFyN{S=
T98G NVy2XYJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC2NmVoOjBizszN MVW3NkBp MoPYSG1UVw>? NGC3TFZKSzVyPEWg{txO MX2yOFc1OTB5NB?=
U87 M4nkS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOyNEDPxE1? MlL0O|IhcA>? NWjIUVlXTE2VTx?= NYLvbWQ2UUN3MEy1JO69VQ>? M{Tn[FI1PzRzMEe0
LN18 NFP1[oRHfW6ldHnvckBCe3OjeR?= NGrnUGg2KM7:TR?= NFLPb4EzPCCq NWPDfYVOTE2VTx?= MX;Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV MlPtNlQ4PDFyN{S=
LNZ308 Mlz4SpVv[3Srb36gRZN{[Xl? MnfUOUDPxE1? NXTpNlVJOjRiaB?= MWjEUXNQ NULGUGl4UW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= M{\zVlI1PzRzMEe0
Saos-2 NI\lXGtHfW6ldHnvckBCe3OjeR?= NXvZ[mZSPTBizszN NVTiWpplPDhiaB?= MW\Jcohq[mm2czDj[YxtKGmwdnHzbY9v M3TCeVI1PzJ5Nk[w
MG-63 NYPEPXFOTnWwY4Tpc44hSXO|YYm= MWK1NEDPxE1? MnLCOFghcA>? NYriNpllUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MYmyOFczPzZ4MB?=
SJSA-1 NV7DcnBjTnWwY4Tpc44hSXO|YYm= MnT4OVAh|ryP M3PlVVQ5KGh? MUfJcohq[mm2czDj[YxtKGmwdnHzbY9v Mn3vNlQ4Ojd4NkC=
Saos-2 M{PUXGZ2dmO2aX;uJGF{e2G7 MlHZOVAh|ryP NHe3PVg1QCCq MmD3TY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> Mm\6NlQ4Ojd4NkC=
MG-63 NWLrPXRCTnWwY4Tpc44hSXO|YYm= M2TobVUxKM7:TR?= NHjlc3I1QCCq M3PUN2lvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> MX[yOFczPzZ4MB?=
SJSA-1 MWLGeY5kfGmxbjDBd5NigQ>? NFvleFg2OCEQvF2= Mm\XOFghcA>? NEXzdFlKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v NVexWZdnOjR5Mke2OlA>
Saos-2 NHrwN5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlniOVAh|ryP MnWyOFghcA>? MX3Jcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? M2jpWFI1PzJ5Nk[w
MG-63 NUjWNXVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX61NEDPxE1? M16xb|Q5KGh? MmLZTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? MV6yOFczPzZ4MB?=
SJSA-1 NG\t[G5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnUd41uPTBizszN M4O1Z|Q5KGh? NFvMcIRKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MWmyOFczPzZ4MB?=
FaDu M4\CfmZ2dmO2aX;uJGF{e2G7 MoK5OUDPxE1? MVGyOEBp NXfLdXVpTE2VTx?= NET4[WVT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> NYXH[XROOjR4M{GxOFc>
EMT6 Mke0SpVv[3Srb36gRZN{[Xl? M{jGW|Uh|ryP MmT5NlQhcA>? MWDEUXNQ MWDS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= MWKyOFY{OTF2Nx?=
HCT116 MX\GeY5kfGmxbjDBd5NigQ>? Ml2xOUDPxE1? M13RWFI1KGh? NVruRmttTE2VTx?= NYPLS5A5WmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> Mk\3NlQ3OzFzNEe=
U87 MYfGeY5kfGmxbjDBd5NigQ>? NF;DZ2U2KM7:TR?= NYLyTXZSOjRiaB?= MYPEUXNQ M2nYdHJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u MkT1NlQ3OzFzNEe=
GBM NEH4bIRCeG:ydH;zbZMhSXO|YYm= M{T0RlLPxE1? NF:2NpI1QGh? MWrEUXNQ NEXTfJhqdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6 NV24dFhmOjR3MEC0PVI>
BON NGnFTGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfmNU02|ryP MVq3Nog> NHGwUJFl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MoDDNlQ1PDN3MkO=
BON Mnr0RZBweHSxc3nzJGF{e2G7 M2Ww[VEuPc7:TR?= M373eVI1cA>? NHnTTlNqdmO{ZXHz[ZMh[XCxcITvd4l{ MkfpNlQ1PDN3MkO=
H1975 M1TH[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3S4OVAvOy17LkdOwG0> NGfjU|I4Omh? MXPEUXNQ M{KyS2lEPTB;MT6zPFXPxE1? NIrhN5ozPDN|N{i0Oi=>
H1975 NHrlfIJCeG:ydH;zbZMhSXO|YYm= NFPsNJIz|ryP MmLyNlRp MofVSG1UVw>? M2joNolv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6 M2XGT|I1OzN5OES2
T-ALL MnfXRZBweHSxc3nzJGF{e2G7 M3;3SYJmfHenZX6gNU41KGGwZDC1MlMhdU1iYYSgNlRpKGGwZDCwMlkh[W6mIEWuOUBuVSCjdDC0PIghcW5iZHnm[oVz\W62IHPlcIwhdGmwZR?= M33BelI1KG:{IES4bC=> MV7EUXNQ NVHibXJ7[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM> NYm5[5F4OjR|MUC3N|Y>
BCR-ABL NVX1NmxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGwMlI2NTFyzszN Ml\GOIQ> Mm\Zd4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>? MnP6NlQzPDR4MUK=
LC-1/SQSF M3LMVmZ2dmO2aX;uJGF{e2G7 NUDKeGJMO87:TR?= M2rTNVI1cA>? MX7EUXNQ NX3odHhx\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt MnflNlM6QDByOUO=
Primary CLL cells NWnoR4pVSXCxcITvd4l{KEG|c3H5 NYL4RVM4OS1zMN88US=> MUe0PIg> M2S0UIlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> NX7ufXE6OjN6NUC4NFc>
Primary CLL cells NITJNpdMcW6jc3WgRZN{[Xl? MmXjNu69VQ>? MX6zNI1qdg>? NVnxdIY4\GWlcnXhd4VlKFCLM1ugZYN1cX[rdIm= M3rwblI{QDVyOEC3
Primary CLL cells M3HUXGN6fG:2b4jpZ{BCe3OjeR?= NIfJWGQz|ryP M1\hSFI1cA>? M{\k[Ilv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= M3rrZVI{QDVyOEC3
human NSCLC cell lines NHq4fnNCeG:ydH;zbZMhSXO|YYm= MX6wMlEzPS12zszN NVS0fpVxOjSq M3jDeGROW09? MmLRTWM2OHNicnHu[4V{KG[{b32gNE41NTMQvF2= MlHxNlM2PjJ2N{K=
human HCC cell lines MknzR4VtdCC4aXHibYxqfHliYYPzZZk> NGLTe48xNjByNT2x{txO NEnKWIw1QGh? NEf3U5FKSzVyPUJOwG0> M{\ZTlI{PDh7OUm5
Huh7 NEnwdJNMcW6jc3WgRZN{[Xl? NFnvOVUy|ryP NWHwV3FJPDiq NHuzZWZ{cWewaf-shYNidnSueTDy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NWTPRZh2OjN2OEm5PVk>
SK-HEP1 NH;uVodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4njW|EuOjEQvF2= MoHOO|Jp MoT6SG1UVw>? MknWTWM2OO,:nEJOwG0> NF\rToszOzR5OUGzOi=>
786-0 NWP1OVR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjJXpUyNTJyzszN MmLLO|Jp NGXXUXhFVVOR MmqxTWM2OO,:nEJOwG0> NIPKPIUzOzR5OUGzOi=>
JVM2 NY\EfZNQS3m2b4TvfIlkcXS7IHHzd4F6 NYHERoduOC5{LUKw{txO Ml23O|Jp MoLFSG1UVw>? MnrGTWM2OD1yLkpOwG0> MU[yN|I{QDZ|OR?=
EHEB NWfyUFBVS3m2b4TvfIlkcXS7IHHzd4F6 M2DsbVAvOi1{MN88US=> M3XKVFczcA>? MkmzSG1UVw>? M3\ifmlEPTB;MD63{txO MnvUNlMzOzh4M{m=
MEC2 NGrHSolEgXSxdH;4bYNqfHliYYPzZZk> NFjsUo0xNjJvMkFOwG0> NW[3b2RsPzKq M1HucWROW09? NF\jUotKSzVyPUCuO:69VQ>? NXztT|VKOjN{M{i2N|k>
primary B-CLL lymphocytes NHvV[pdCeG:ydH;zbZMhSXO|YYm= NFnzO3dKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n NGrwfY4zPGh? MkP3SG1UVw>? NHrUNpNKSzVy78{cN:69VSCob4KgZYxtKHCjdHnlcpR{ Mom2NlMzOzh4M{m=
primary B-CLL lymphocytes NYXh[VFvU2mwYYPlJGF{e2G7 NHTmS25KSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n M3SwVlI1cA>? NFThR3dqdmirYnn0d{BxPzCVNlugKkA1TS2EUEGg[ZhxemW|c3nvci=> NUfWV2wzOjN{M{i2N|k>
human NSCLC MkDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\aTpNKOC53LUNOwG0> NWmzRYxrPzKq M{fBZ2lEPTB;Md88US=> Mk\ONlI4QDF|OUO=
human NSCLC NEexUGlMcW6jc3WgRZN{[Xl? M3XsbVHPxE1? M4rjc|I1cA>? M2rmb4lvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= MUSyNlc5OTN7Mx?=
Y1 cell line NFTsWYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELSS24xNjIQvF2vNe69VQ>? NYLwbnJNOjSq M3mySWROW09? MWLpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>? M2LXUlIzPjl{OUC0
PIK3CA-mutant MCF7 NWnwcXppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTKS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? MljoO|Jp NWTjNIsyT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= NF;CU|UzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 M{DTemtqdmG|ZTDBd5NigQ>? MnjaTWM2OD1zMUVCtVNvVQ>? MVS3Nog> M4rUZWlEPTB;MUG0xtE{dk1iaX6gdoVlfWOrbnegRYt1KHCqb4PwbI9zgWyjdHnvckBt\X[nbIO= MW[yNlY2Ozl4Nx?=
MCF7-myr-Akt MoPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvkS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? M1nRfVczcA>? NIn5VYtIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= MXiyNlY2Ozl4Nx?=
colon cancer cell lines NV73[ZpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTPNE0yOM7:TR?= NEjidZI4Omh? MV;EUXNQ M37pRmlEPTB;Md88US=> M3zVSVIzPTR|OEW3
gastric cancer cell lines NHjEWZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nsdFAuOTEQvF2= NFTyb2w4Omh? M1zUd2ROW09? MWXJR|UxRTJvNd88US=> NX6xXYR2OjJ3NEO4OVc>
HCT-116/HT-29/MKN-45 MU\BdI9xfG:|aYOgRZN{[Xl? NHfQTI8z|ryP MnvCOFhp MlW2d4hq\nRiaX6gS|IheGijc3W= Ml\oNlI2PDN6NUe=
HT-29 and HCT-116 MlnyR4F{eGG|ZTDhd5NigQ>? NV\xcFNVPc7:TR?= M1;HfFI1cA>? M1zVWIlv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= M3HYV|IzPTR|OEW3
MM cell lines NEHNVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj5NVDPxE1? NIXuVXUzPGh? M4LwU2ROW09? Mn;ETWM2OCC4YYLp[ZMh[W2xbneg[Iln\mW{ZX70JINmdGxibHnu[ZMhcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcoNm Ml;tNlIzODd2OEW=
ARP-1 NF\le2ZCeG:ydH;zbZMhSXO|YYm= MlvUNVDPxE1? Mm\PNlRp MmTvSG1UVw>? MYXpcoR2[2W|IF3NJINmdGxiYYDvdJRwe2m|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w NGfQXoozOjJyN{S4OS=>
SNU-601 NXPFflkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIraeGg4Omh? NWLjPXdHTE2VTx?= M4SwPGlEPTB;MD64NVbDuTBwME[z{txO M{\UflIzOTV7OEG0
SNU-1 M2TmSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYW3Nog> NE\BNodFVVOR MnexTWM2OD1zLkC4NuKyOC5yMklOwG0> M1LqbVIzOTV7OEG0
SNU-668 NUfId|hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\HRVczcA>? M4rSSWROW09? M2LTNmlEPTB;MT61O|nDuTBwMEe0{txO NXPVU2U3OjJzNUm4NVQ>
AGS MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe3Nog> NXXSNpJ2TE2VTx?= MXnJR|UxRTFwN{G0xtExNjFzN988US=> M1zUbFIzOTV7OEG0
SNU-216 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTzS41rPzKq MkX3SG1UVw>? NILae2RKSzVyPUKuOlkzyrFyLkC4Nu69VQ>? NYnjZmdiOjJzNUm4NVQ>
SNU-5 NVfaTIgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPjO|Jp NF3v[ZZFVVOR M4T0WWlEPTB;MT6zOVHDuTBwMEmx{txO M3H6WFIzOTV7OEG0
SNU-638 M{\ieGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXO3Nog> NFP6ZVVFVVOR MULJR|UxRTJwMkiyxtExNjB3M988US=> NXT1SpZbOjJzNUm4NVQ>
SNU-16 M2DLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3iwVlczcA>? MlTaSG1UVw>? NETQU4NKSzVyPUGuOVc{yrFyLkCwNe69VQ>? MmDaNlIyPTl6MUS=
SNU-484 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HFbVczcA>? M2i3UmROW09? MlrWTWM2OD1zLkeyPOKyOC5yNEZOwG0> NWX6bHU2OjJzNUm4NVQ>
SNU-620 NUnCNnhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjtO|Jp Mkf1SG1UVw>? M1fNSWlEPTB;Mj65N|nDuTBwMECx{txO NWHRbYZMOjJzNUm4NVQ>
SNU-719 NULaeZlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnXWXhiPzKq NVHIeZd[TE2VTx?= MVzJR|UxRTNwMEO3xtExNjB|Mt88US=> NXezTZZ6OjJzNUm4NVQ>
glioma cell lines MnfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnBO|Jp NF\a[WpKSzVyPUGtNu69VQ>? Ml3VNlIxPjVyOEC=
U87 M2ixe2Fxd3C2b4Ppd{BCe3OjeR?= NUP6Zph3Os7:TR?= MlP6O|Jp MmXubY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= NFnPeHczOjB4NUC4NC=>

... 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 (37)

技術サポート&よくある質問(FAQ)

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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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