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。

価格 在庫  
USD 214 あり
USD 342 あり
USD 403 あり
USD 1222 あり

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

高品質保証

文献中の引用(34)

カスタマーフィードバック(3)

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 NYLHbnBqS3m2b4TvfIlkKEG|c3H5 NXTre2R6PzJiaB?= M{Pp[mROW09? NHLMWVhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN NXPaWo1DOjR7MECyOlY>
DU145 MWHDfZRwfG:6aXOgRZN{[Xl? Ml\HO|IhcA>? M13vTGROW09? NHXFeWtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2= M3i1RlI1QTByMk[2
A2780 NEXw[lZEgXSxdH;4bYMhSXO|YYm= M3fDZVczKGh? MkW2SG1UVw>? MnP3R5l1d3SxeHnjbZR6KGGpYXnud5QhWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCJSUWwJI9nKDBwMECwOlM2KM7:TR?= MlnVNlQ6ODB{Nk[=
U87MG NGPpU2lEgXSxdH;4bYMhSXO|YYm= MV63NkBp NEjXbFZFVVOR M{XROWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY6QCEQvF2= M3fiNFI1QTByMk[2
A2780 MWrGeY5kfGmxbjDBd5NigQ>? MUGxJIg> NF2zUHBFVVOR MXzJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>? M2H5NFI1QTByMk[2
DU145 MlHBSpVv[3Srb36gRZN{[Xl? NULYUVR4OSCq NHvUWo1FVVOR M2ewNGlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBFXTF2NTDj[YxteyCqYYLic5JqdmdiTFvCNUBufXSjdHnvckB4cXSqIFXDOVAhd2ZiMD6wO|Mh|ryP M1vtXFI1QTByMk[2
A2780 M1nhfmZ2dmO2aX;uJGF{e2G7 NHv0ZmcyKGh? MmnzSG1UVw>? M13qdmlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP NX7jOJdxOjR7MECyOlY>
MCF7 NYPIUpFvTnWwY4Tpc44hSXO|YYm= NHTIR3YyKGh? MlTISG1UVw>? MnPDTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO MUeyOFkxODJ4Nh?=
U87MG NFu5XW5HfW6ldHnvckBCe3OjeR?= MYmxJIg> NVz1UIVVTE2VTx?= MYXJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO NXXv[pBvOjR7MECyOlY>
A2780 M1vUVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILEV3g4OiCq NIDtfmJFVVOR M{[3cWVEPTB;MD61NkDPxE1? MmiyNlQ6ODB{Nk[=
SKMES-1 MlfhR5l1d3SxeHnjJGF{e2G7 MVexJO69VQ>? MkL3O|IhcA>? MVHJcoR2[2W|IHPlcIwh\GWjdHi= NYTW[oh5OjZyMUOzNVg>
H596 NFrqR2tHfW6ldHnvckBCe3OjeR?= MXKxJO69VQ>? Mm\6TY1x[Wm{czDj[YxtKG2rZ4LheIlwdg>? MmHlNlYxOTN|MUi=
HCC2450 NF7lTIlHfW6ldHnvckBCe3OjeR?= NWXRbHpLOSEQvF2= NV;3XXdyUW2yYXnyd{Bk\WyuIHnueoF{cW:w NIC3XpAzPjBzM{OxPC=>
A549 MlTKSpVv[3Srb36gRZN{[Xl? Mm\VOVAxKG6P MmmzOFghcA>? NGrIR3JFVVOR NFr1NpdKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= MnjRNlU6Ozd{OUm=
A549 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXqyR|dvOSEQvF2= NV\YRlNyPzJiaB?= M{XOeGROW09? NE\DVXRKdmirYnn0d{Bk\WyuIHfyc5d1cA>? MlLGNlU6Ozd{OUm=
H522 NV3YWHJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXvb2YyKM7:TR?= MlHaO|IhcA>? MYPEUXNQ NIfTbJRKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NX3lRm1zOjV7M{eyPVk>
LNCaP NWLVflJsTnWwY4Tpc44hSXO|YYm= MnuyNUDPxE1? MlnmV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? M2e0elI2OzZyN{m5
LNCaP95 NWTkTYJXTnWwY4Tpc44hSXO|YYm= M2rnTVEh|ryP MYrTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? M17qTVI2OzZyN{m5
HCT-15 NIjG[FVCeG:2b4Ppd{BCe3OjeR?= NIjKNY4yOCEQvF2= MoqwOFghcA>? Mn\mSG1UVw>? M3PMXWlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xOUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MUSyOVE2OjJ2NR?=
HCT-116 NGS5RoNCeG:2b4Ppd{BCe3OjeR?= NF7HdGIyOCEQvF2= MlnkOFghcA>? M3e0ZWROW09? MWnJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? NHzLOJYzPTF3MkK0OS=>
NCI-H460 NWS2SGlySXCxdH;zbZMhSXO|YYm= NYfqTVl5OTBizszN M1jLVVQ5KGh? M1jR[2ROW09? M3m2e2lv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NYqyRpdTOjVzNUKyOFU>
SKOV-3 NIL6RZJCeG:2b4Ppd{BCe3OjeR?= NGXGcYsyOCEQvF2= MY[0PEBp NEfmUZlFVVOR MUXJcoR2[2W|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NYXxeHd2OjVzNUKyOFU>
BSY-1 NWfPZ|JqSXCxdH;zbZMhSXO|YYm= M4DKSlExKM7:TR?= NEnIN5E1QCCq NWPs[npOTE2VTx?= NYTw[IE{UW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= Mo\MNlUyPTJ{NEW=
MKN-1 M2XpOmFxd3Sxc3nzJGF{e2G7 NXuxTJBkOTBizszN MWq0PEBp NHfKVHNFVVOR M2XmUGlv\HWlZYOgZZBweHSxc3nzJIlvKE2NTj2xJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MnjqNlUyPTJ{NEW=
NCI-H522 MX7BdI91d3OrczDBd5NigQ>? M{j0[|ExKM7:TR?= MoeyOFghcA>? MVTEUXNQ M3KyeWlv\HWlZYOgZZBweHSxc3nz M2LDd|I2OTV{MkS1
OVCAR-3 MkjJRZBwfG:|aYOgRZN{[Xl? M2W2UFExKM7:TR?= MUC0PEBp NUj0TnM1TE2VTx?= MYLJcoR2[2W|IHHwc5B1d3Orcx?= M3TjbVI2OTV{MkS1
HBC-5 MnfTRZBwfG:|aYOgRZN{[Xl? NVjVSGNYOTBizszN MXe0PEBp MYfEUXNQ M4nSXWlv\HWlZYOgZZBweHSxc3nz M3ewflI2OTV{MkS1
RXF-631L NW\vXGJGSXCxdH;zbZMhSXO|YYm= MnTLNVAh|ryP MYm0PEBp M3;VeGROW09? NGHncppKdmS3Y3XzJIFxd3C2b4Ppdy=> MVOyOVE2OjJ2NR?=
MKN-45 M1G1NWFxd3Sxc3nzJGF{e2G7 MUWxNEDPxE1? NIPwU4g1QCCq NYrPR5pXTE2VTx?= MVjJcoR2[2W|IHHwc5B1d3Orcx?= MX:yOVE2OjJ2NR?=
BON-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HGXlUxOCCwTR?= M3nLUFExKGR? M4PTZWROW09? NYrJNGJ1UW6qaXLpeJMh[2WubDDndo94fGh? NX30TGdsOjVyMk[yPVI>
BON-1 NX24UVVKTnWwY4Tpc44hSXO|YYm= NXnFe2R2PTByIH7N NIrJ[|A1KGh? NYjWO|FFTE2VTx?= M4X3NGlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= MYWyOVAzPjJ7Mh?=
QGP-1 M1zG[2Z2dmO2aX;uJGF{e2G7 NFHtc3E2ODBibl2= MWe0JIg> M2O0[mROW09? NH7LeZhKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez MkPRNlUxOjZ{OUK=
Huh7 M4jRZmZ2dmO2aX;uJGF{e2G7 MX2xJO69VQ>? MXexJIg> NF61T5FFVVOR NHr5[I1KdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHNmejR5NB?= MonENlUxODR2MEO=
BNL M1rDU2Z2dmO2aX;uJGF{e2G7 NWPjXXRlOSEQvF2= MkW3NUBp NV20RXZnTE2VTx?= MUfJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Y> NYi1VpU6OjVyMES0NFM>
MDA-MB-175 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL6eXl5OSEQvF2= MlTpOUBl NWr4[|hOTE2VTx?= M1v6WWlEPTB:MTFOwG0> MXSyOFg4QTd7Nh?=
MDA-MB-134 NFrlS5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIr5cJcyKM7:TR?= NXrmTHNyPSCm MV\EUXNQ NV3nXoZMUUN3MEyxJO69VQ>? M1zxeVI1QDd7N{m2
HCC1500 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Xz[VEh|ryP NEXpeVA2KGR? NVrnWYZiTE2VTx?= NG\2cGdKSzVyPEGg{txO MXSyOFg4QTd7Nh?=
EFM-19 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{K0SlEh|ryP NGnDWGk2KGR? MnflSG1UVw>? MUTJR|UxRDFizszN NVixPYZmOjR6N{m3PVY>
ZR-75-30 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDqOIJUOSEQvF2= NH;RcFc2KGR? MmTYSG1UVw>? NV;oNnRDUUN3MEyxJO69VQ>? MlLvNlQ5Pzl5OU[=
MDA-MB-361 M2jGUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\Rc|h[OSEQvF2= M2Tjc|Uh\A>? MUXEUXNQ M{PwOWlEPTB:MTFOwG0> M37VZ|I1QDd7N{m2
T-47D M4PPW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWixJO69VQ>? M3nuXlUh\A>? Mm\4SG1UVw>? MXXJR|UxRDFizszN M2X1U|I1QDd7N{m2
SK-BR-3 NUDsZYI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLkOZJzOSEQvF2= NH7FfYg2KGR? M4nXR2ROW09? NH:5bmNKSzVyPEGg{txO MWqyOFg4QTd7Nh?=
UACC-732 NVPnVGhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDBNUDPxE1? NXLmbVllPSCm NIi1WY1FVVOR NFnUfY1KSzVyPEGg{txO M4PZNVI1QDd7N{m2
BT-474 MmqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxJO69VQ>? MY[1JIQ> MmHSSG1UVw>? M1qwdmlEPTB:MTFOwG0> MnrGNlQ5Pzl5OU[=
HCC202 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi1XGY2OSEQvF2= Mn:4OUBl NYq1bIhYTE2VTx?= MoniTWM2ODxzIN88US=> NHu3fGMzPDh5OUe5Oi=>
MCF7 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIOxXI4yKM7:TR?= MljMOUBl MmPISG1UVw>? NWTqeIR3UUN3MEyxJO69VQ>? NWL3NlRiOjR6N{m3PVY>
MDA-MB-415 M3vuTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuxJO69VQ>? NGLDSnQ2KGR? Mn\SSG1UVw>? M3vYbmlEPTB:MTFOwG0> NV72V45SOjR6N{m3PVY>
MDA-MB-453 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTWNUDPxE1? M{LHWFUh\A>? MYTEUXNQ NYnsdYJVUUN3MEyxJO69VQ>? M2\VUFI1QDd7N{m2
ZR-75-1 NGXYXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCxJO69VQ>? MknBOUBl MmP6SG1UVw>? MYPJR|UxRDFizszN MnXoNlQ5Pzl5OU[=
HCC38 M2HEe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3VRYJjOSEQvF2= NI\WTWY2KGR? NVTWPW9lTE2VTx?= MYfJR|UxRDFizszN MkDpNlQ5Pzl5OU[=
HCC1419 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHXRmNMOSEQvF2= NVf1Vms1PSCm MVzEUXNQ NGDnS|NKSzVyPEGg{txO M13wVlI1QDd7N{m2
UACC-812 NWfUe2dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\pSFEh|ryP NHPxcog2KGR? MUPEUXNQ NGTxTlRKSzVyPEGg{txO M1O0RlI1QDd7N{m2
HCC1187 M2n2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPLVJMyKM7:TR?= NFXKW4E2KGR? M1j3fmROW09? NFHSS5hKSzVyPEGg{txO MmrONlQ5Pzl5OU[=
KPL-1 MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrCRmk5OSEQvF2= M3KwbVUh\A>? NHHDSYFFVVOR NULFXoNFUUN3MEyxJO69VQ>? NHzM[G0zPDh5OUe5Oi=>
SUM-225 NVXPUldFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYOxJO69VQ>? M2izPFUh\A>? M4rrUmROW09? Mm[yTWM2ODxzIN88US=> MkO2NlQ5Pzl5OU[=
EFM-192A MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorkNUDPxE1? NYPTc41OPSCm MYfEUXNQ M2nCb2lEPTB:MTFOwG0> NVmwTWE2OjR6N{m3PVY>
JIMT-1 MkjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvvNUDPxE1? M1vON|Uh\A>? NYDVc3NJTE2VTx?= NHrJb49KSzVyPEGg{txO M13oWVI1QDd7N{m2
HCC1143 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3zNUDPxE1? MnHFOUBl MULEUXNQ NXPYVmVJUUN3MEyxJO69VQ>? NF3kfnIzPDh5OUe5Oi=>
HCC2218 M1Sxfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXqxJO69VQ>? MWi1JIQ> NHnjOoNFVVOR NYTBeW5iUUN3MEyxJO69VQ>? MXeyOFg4QTd7Nh?=
MDA-MB-468 NIn1V|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[xJO69VQ>? MWK1JIQ> NF\XUWlFVVOR Ml;aTWM2ODxzIN88US=> MnPBNlQ5Pzl5OU[=
BT-20 NYPpRZdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjDS5oyOSEQvF2= M{XURVUh\A>? NHLwOYVFVVOR MkC3TWM2ODxzIN88US=> MlnqNlQ5Pzl5OU[=
MDA-MB-435 NILsVGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDLNUDPxE1? MWm1JIQ> M36wR2ROW09? MkfwTWM2ODxzIN88US=> MnTiNlQ5Pzl5OU[=
BT-549 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;uNUDPxE1? M3uwXVUh\A>? MYTEUXNQ M3TEb2lEPTB:MTFOwG0> M1XoWFI1QDd7N{m2
HCC1806 NH3qb5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TsOlEh|ryP M{LMS|Uh\A>? NVewb3lETE2VTx?= MVzJR|UxRDFizszN NEXDbI0zPDh5OUe5Oi=>
HCC1937 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjmNUDPxE1? MYG1JIQ> NI\k[WFFVVOR NH[yTmVKSzVyPEGg{txO M4freFI1QDd7N{m2
Hs578T MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn0fYgyKM7:TR?= NXvGXmVqPSCm MkLhSG1UVw>? NH;XN3BKSzVyPEGg{txO NU\FW5ZyOjR6N{m3PVY>
LN18 Mmj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYCyNEDPxE1? NX:1WZFjPzJiaB?= NYj5UpI6TE2VTx?= MYDJR|UxRDVizszN MUmyOFc1OTB5NB?=
LN229 M1\lemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYeyNEDPxE1? NYfyb2k1PzJiaB?= NXewOYYxTE2VTx?= MkHzTWM2ODx3IN88US=> M2frXlI1PzRzMEe0
LNZ308 NFjCemFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS2OZEzOCEQvF2= MlzIO|IhcA>? MUXEUXNQ MoPjTWM2ODx3IN88US=> Mof1NlQ4PDFyN{S=
T98G MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fxbVIxKM7:TR?= M3;ZWFczKGh? MY\EUXNQ NUG4SFlFUUN3MEy1JO69VQ>? MUiyOFc1OTB5NB?=
U87 NX3rTHhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlf1NlAh|ryP NGP2cZQ4OiCq MUnEUXNQ MmnKTWM2ODx3IN88US=> NHH1[ZozPDd2MUC3OC=>
LN18 MnnhSpVv[3Srb36gRZN{[Xl? MnnIOUDPxE1? NWTmdIZ2OjRiaB?= MXTEUXNQ NFLVOI5KdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuW MlTTNlQ4PDFyN{S=
LNZ308 MlHGSpVv[3Srb36gRZN{[Xl? NVfE[GJiPSEQvF2= MXqyOEBp M1vFZmROW09? MU\Jcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV MYKyOFc1OTB5NB?=
Saos-2 NYDtV2RbTnWwY4Tpc44hSXO|YYm= NXnDfWY5PTBizszN MnjtOFghcA>? NVjSPWdTUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= NEH2c|gzPDd{N{[2NC=>
MG-63 MoK2SpVv[3Srb36gRZN{[Xl? NGjDVmM2OCEQvF2= NELaNFU1QCCq MVPJcohq[mm2czDj[YxtKGmwdnHzbY9v NFG2NZIzPDd{N{[2NC=>
SJSA-1 NIXyfXFHfW6ldHnvckBCe3OjeR?= NEPRWFY2OCEQvF2= NIjhO4c1QCCq NXfu[JRPUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MVKyOFczPzZ4MB?=
Saos-2 MoDHSpVv[3Srb36gRZN{[Xl? Mnz5OVAh|ryP MkDtOFghcA>? NWfKUI5FUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? NXvEPIdvOjR5Mke2OlA>
MG-63 NUD3doNKTnWwY4Tpc44hSXO|YYm= NGjKPXA2OCEQvF2= M2DOeFQ5KGh? NETmc5VKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v M3nFSlI1PzJ5Nk[w
SJSA-1 NF\adoFHfW6ldHnvckBCe3OjeR?= M3n1V|UxKM7:TR?= NYXHcVhRPDhiaB?= MVfJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NGSxUYozPDd{N{[2NC=>
Saos-2 MkDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXniSYtHPTBizszN MVu0PEBp M1vXb2lvcGmkaYTzJINmdGxidnnhZoltcXS7 MWiyOFczPzZ4MB?=
MG-63 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUS1NEDPxE1? NFLBVVc1QCCq MYfJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? MlPmNlQ4Ojd4NkC=
SJSA-1 M{Dhfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH62OVc2OCEQvF2= MUG0PEBp NF\sblBKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NIT5UIIzPDd{N{[2NC=>
FaDu MofmSpVv[3Srb36gRZN{[Xl? M3X6[|Uh|ryP M{KybVI1KGh? NH;nfHpFVVOR NET6UXVT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> NXzvdYxjOjR4M{GxOFc>
EMT6 M{fNOWZ2dmO2aX;uJGF{e2G7 MmPpOUDPxE1? MlG4NlQhcA>? M2K5NGROW09? NYLneWdKWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NUDDcGJJOjR4M{GxOFc>
HCT116 MWDGeY5kfGmxbjDBd5NigQ>? MofHOUDPxE1? MkTTNlQhcA>? MVHEUXNQ NVnpT5dUWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NYHqV3NFOjR4M{GxOFc>
U87 M{\wN2Z2dmO2aX;uJGF{e2G7 M4LiN|Uh|ryP MmnRNlQhcA>? M{jqdmROW09? MWPS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= MW[yOFY{OTF2Nx?=
GBM NYDhTpNtSXCxcITvd4l{KEG|c3H5 MYOy{txO M3;LXVQ5cA>? MW\EUXNQ NYrZUJdCcW6mdXPl[EBpcWeqZYKgcIV3\Wy|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>? NX\TNXU6OjR3MEC0PVI>
BON MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqxMVXPxE1? M4jk[|czcA>? M4XvOIRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MVSyOFQ1OzV{Mx?=
BON MlTXRZBweHSxc3nzJGF{e2G7 NI\me|MyNTYQvF2= NWG2ZVkzOjSq NVXyXW85cW6lcnXhd4V{KGGyb4D0c5Nqew>? MXGyOFQ1OzV{Mx?=
H1975 MlvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjFNE4{NTlwNt88US=> NH6xZZM4Omh? MYnEUXNQ NFTLeo5KSzVyPUGuN|g2|ryP MkTONlQ{Ozd6NE[=
H1975 NYm2SnFqSXCxcITvd4l{KEG|c3H5 NF:1O3Mz|ryP NYXGfnNrOjSq NUPaNIJFTE2VTx?= NIf4TFhqdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>? M3jKdFI1OzN5OES2
T-ALL MlvoRZBweHSxc3nzJGF{e2G7 MX7i[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV? NXrnXnFMOjRib4KgOFhp NY\KW|Z[TE2VTx?= MXzh[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= MYmyOFMyODd|Nh?=
BCR-ABL MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fkVlAvOjVvMUFOwG0> NETTemE1\A>? M2TmWJNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? NEfocHYzPDJ2NE[xNi=>
LC-1/SQSF NI\pZ4lHfW6ldHnvckBCe3OjeR?= MXqz{txO NIDlfpUzPGh? M2DC[2ROW09? NGW2Xmll\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw> MWKyN|k5ODB7Mx?=
Primary CLL cells MYTBdI9xfG:|aYOgRZN{[Xl? MV[xMVEx|ryP M2HBZ|Q5cA>? MXjpcoR2[2W|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz MVuyN|g2ODhyNx?=
Primary CLL cells MVHLbY5ie2ViQYPzZZk> Mk\0Nu69VQ>? M2jmeFMxdWmw M2TmZ4Rm[3KnYYPl[EBRUTONIHHjeIl3cXS7 MlPMNlM5PTB6MEe=
Primary CLL cells NFf1VXBEgXSxdH;4bYMhSXO|YYm= Mn7pNu69VQ>? MXmyOIg> M1HtO4lv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= NHq1[IIzOzh3MEiwOy=>
human NSCLC cell lines NXntNnBOSXCxcITvd4l{KEG|c3H5 NXzWZWxFOC5zMkWtOO69VQ>? Ml7jNlRp MnPCSG1UVw>? NI\p[VVKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> MXyyN|U3OjR5Mh?=
human HCC cell lines M33N[WNmdGxidnnhZoltcXS7IHHzd4F6 M1S2TVAvODB3LUJOwG0> NUXCdVVxPDiq M4LVOGlEPTB;Md88US=> MlTaNlM1QDl7OUm=
Huh7 M2LRSWtqdmG|ZTDBd5NigQ>? MlXVNe69VQ>? NXWzNHQ2PDiq MkLRd4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NELCZmozOzR6OUm5PS=>
SK-HEP1 NF;BUHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnmwNU0zOM7:TR?= M2OxS|czcA>? M2HOTWROW09? NUnmdIF4UUN3MP-8oFHPxE1? M3PKU|I{PDd7MUO2
786-0 NXe0UFA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXL4SFVmOS1{MN88US=> M1fJ[VczcA>? NVfjR2dqTE2VTx?= NEHRe5VKSzVy78{cNe69VQ>? MnrmNlM1PzlzM{[=
JVM2 MXzDfZRwfG:6aXPpeJkh[XO|YYm= NVvoSIRqOC5{LUKw{txO MlvVO|Jp MUPEUXNQ MmTGTWM2OD1yLkpOwG0> MkD0NlMzOzh4M{m=
EHEB NFXsb4dEgXSxdH;4bYNqfHliYYPzZZk> Ml22NE4zNTJyzszN Mni0O|Jp NX7ESlVLTE2VTx?= MorKTWM2OD1yLkhOwG0> Mli0NlMzOzh4M{m=
MEC2 NFfIXm1EgXSxdH;4bYNqfHliYYPzZZk> NX7U[mVTOC5{LUKw{txO MU[3Nog> MnPoSG1UVw>? MmDMTWM2OD1yLkhOwG0> MVGyN|I{QDZ|OR?=
primary B-CLL lymphocytes MVvBdI9xfG:|aYOgRZN{[Xl? NHzhbIJKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n NFPoR3MzPGh? NUn0cZVTTE2VTx?= MUnJR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz Mn3QNlMzOzh4M{m=
primary B-CLL lymphocytes MUXLbY5ie2ViQYPzZZk> M1;remlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? M4S2WVI1cA>? M1K1Z4lvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u NHzvdIMzOzJ|OE[zPS=>
human NSCLC M2jsW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL1NE42NTMQvF2= NELRPWg4Omh? NVnXeHIxUUN3ME2x{txO M1r5PVIzPzhzM{mz
human NSCLC NHLRToFMcW6jc3WgRZN{[Xl? M1r4S|HPxE1? M3rKe|I1cA>? NUn2SYlNcW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=> NUTLe4k1OjJ5OEGzPVM>
Y1 cell line NVz5[2NUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:wO2YxNjIQvF2vNe69VQ>? MWiyOIg> Mn3YSG1UVw>? NXzY[oJ6cW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= Ml3nNlI3QTJ7MES=
PIK3CA-mutant MCF7 MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? NI\4[GM4Omh? NWDaVINTT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= NX;TS|VEOjJ4NUO5Olc>
PIK3CA-mutant MCF7 NHz5O3RMcW6jc3WgRZN{[Xl? NUDGOHRbUUN3ME2xNVTDuTOwTR?= M2fjcFczcA>? MUjJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| NFrPb3ozOjZ3M{m2Oy=>
MCF7-myr-Akt M{DmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXzWZh6T0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= M{HPWFczcA>? MkfLS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? MknENlI3PTN7Nke=
colon cancer cell lines NELKR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWwMVEx|ryP NW[1dZV2PzKq Ml;aSG1UVw>? MoW2TWM2OD1zzszN NYDSeYJ{OjJ3NEO4OVc>
gastric cancer cell lines MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT5fG8zOC1zMN88US=> NVKy[Is5PzKq NWPnOpVmTE2VTx?= MVrJR|UxRTJvNd88US=> MX[yNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45 NIW0PXJCeG:ydH;zbZMhSXO|YYm= NH\rW|Uz|ryP M4fB[VQ5cA>? MVXzbIlnfCCrbjDHNkBxcGG|ZR?= MYiyNlU1Ozh3Nx?=
HT-29 and HCT-116 M2[2V2Nie3Cjc3WgZZN{[Xl? MnmwOe69VQ>? M2fXcFI1cA>? MnPRbY5lfWOnczDjZZNx[XOnIHHjeIl3cXS7 NXzCcFJMOjJ3NEO4OVc>
MM cell lines NIDHfppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHMOZkyOM7:TR?= NUHMbnFWOjSq NI\IVIRFVVOR NF:yWldKSzVyII\hdolmeyCjbX;u[{BlcW[oZYLlcpQh[2WubDDsbY5meyCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVv[2V? NVjPRmN{OjJ{MEe0PFU>
ARP-1 M1PsO2Fxd3C2b4Ppd{BCe3OjeR?= MoXwNVDPxE1? MWWyOIg> NEGzRpBFVVOR NGi3fVhqdmS3Y3XzJG1OKGOnbHygZZBweHSxc3nzJJRpem:3Z3igZ4F{eGG|ZTDhZ5RqfmG2aX;u NIfo[pQzOjJyN{S4OS=>
SNU-601 NUGxRo9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPOflQ4Omh? MVzEUXNQ Mkm4TWM2OD1yLkixOuKyOC5yNkROwG0> NV7XboFWOjJzNUm4NVQ>
SNU-1 NEC5ZmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LucVczcA>? NYr4PWN[TE2VTx?= M4nCcGlEPTB;MT6wPFLDuTBwMEK4{txO MmjVNlIyPTl6MUS=
SNU-668 NGfnOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\LO|Jp M1fHR2ROW09? M3TyNWlEPTB;MT61O|nDuTBwMEe0{txO MXSyNlE2QThzNB?=
AGS MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HJdlczcA>? MoLySG1UVw>? NHTkVJFKSzVyPUGuO|E1yrFyLkGxO:69VQ>? NYK0SmpuOjJzNUm4NVQ>
SNU-216 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXwe|Q4Omh? MlPwSG1UVw>? MXTJR|UxRTJwNkmyxtExNjB6Mt88US=> NGXSbpkzOjF3OUixOC=>
SNU-5 NUH3d|dFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTS[YU4Omh? M12wXGROW09? MVzJR|UxRTFwM{WxxtExNjB7Md88US=> M{TSNlIzOTV7OEG0
SNU-638 NXrBWodQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWe3Nog> MlLGSG1UVw>? M2P1WmlEPTB;Mj6yPFLDuTBwMEWz{txO MXOyNlE2QThzNB?=
SNU-16 Ml\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf4Tnk4Omh? MnjiSG1UVw>? M3LjemlEPTB;MT61O|PDuTBwMECx{txO MoX2NlIyPTl6MUS=
SNU-484 NHqyPXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWK3Nog> NWDkXHoyTE2VTx?= M3K4XmlEPTB;MT63NljDuTBwMES1{txO NV;rWFA5OjJzNUm4NVQ>
SNU-620 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfQbHB3PzKq NYrleWFLTE2VTx?= Ml\tTWM2OD1{LkmzPeKyOC5yMEJOwG0> MoK4NlIyPTl6MUS=
SNU-719 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnzU5ZPPzKq NXO1WIVqTE2VTx?= NXn0dY1jUUN3ME2zMlA{P8LzMD6wN|LPxE1? MVuyNlE2QThzNB?=
glioma cell lines NHTDU|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLBVY44Omh? MlvCTWM2OD1zLUNOwG0> NX7OV5JPOjJyNkWwPFA>
U87 MXXBdI9xfG:|aYOgRZN{[Xl? NVrMdmhXOs7:TR?= MlHyO|Jp NYPCc|FwcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> Mn2xNlIxPjVyOEC=

... 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)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related PI3K 阻害剤

  • GDC-0032

    GDC-0032は一種有効的で、次世代のβ亜型PI3K阻害剤で、PI3Kα/δ/γに作用する時のIC50値が0.29 nM/0.12 nM/0.97nMそれぞれ分かれます。GDC-0032はPI3Kα/δ/γに作用する選択性はPI3Kβに作用する選択性より10倍以上が高くなります。

    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阻害剤で、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、初めに命名されたPI3K阻害剂で、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。

最近チェックしたアイテム

Tags: BKM120 (NVP-BKM120, Buparlisib)を買う | BKM120 (NVP-BKM120, Buparlisib)供給者 | BKM120 (NVP-BKM120, Buparlisib)を購入する | BKM120 (NVP-BKM120, Buparlisib)費用 | BKM120 (NVP-BKM120, Buparlisib)生産者 | オーダーBKM120 (NVP-BKM120, Buparlisib) | BKM120 (NVP-BKM120, Buparlisib)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ