Buparlisib (BKM120, NVP-BKM120)

目录号:S2247

Buparlisib (BKM120, NVP-BKM120) Chemical Structure

Molecular Weight(MW): 410.39

Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34,mTOR,DNAPK 的作用效果下降,而对 PI4Kβ几乎没有活性。Phase 2。

规格 价格 库存 购买数量  
In DMSO RMB 2227.95 现货
RMB 1400.12 现货
RMB 2607.65 现货
RMB 7928.28 现货
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产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34,mTOR,DNAPK 的作用效果下降,而对 PI4Kβ几乎没有活性。Phase 2。
特性 BKM120是可用于口服的生物有效的PI3K抑制剂。
靶点
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
Vps34 [1]
(Cell-free assay)
52 nM 116 nM 166 nM 262 nM 2.4 μM
体外研究

BKM120作用于解除PI3K调节的细胞系,包括A2780, U87MG, MCF7和DU145时,具有抗增殖活性,GI50为0.1-0.7 nM。[1] BKM120诱导多发性骨髓瘤细胞(ARP1, ARK, MM.1S, MM1.R和U266)凋亡,导致G1期细胞增多,S期细胞减少。BKM120诱导CD138+原代MM 细胞凋亡,且作用于CD138−基质细胞时毒性较低。BKM120可引起BimS的上调和XIAP的下调。[2]BKM120作用于人类胃癌细胞系,降低mTOR下游信号,具有抗增殖活性。BKM120作用于KRAS突变的胃癌细胞系,可以增强p-ERK或 p-STAT3。BKM120 和STAT3阻断剂联用, 作用于含突变KRAS的细胞,诱导凋亡,具有协同效应,但是作用于KRAS野生型细胞没有这种效果。[3]BKM120主要通过Aurora B激酶调节有丝分裂崩坏。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 NH71N|hEgXSxdH;4bYMhSXO|YYm= MmPKO|IhcA>? MXTEUXNQ NYrqbppwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=> M1PUNVI1QTByMk[2
DU145 MlHGR5l1d3SxeHnjJGF{e2G7 NWjvd|JLPzJiaB?= NYe5d|ZvTE2VTx?= NIDxXWNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2= MlrKNlQ6ODB{Nk[=
A2780 MXHDfZRwfG:6aXOgRZN{[Xl? NWrac29QPzJiaB?= NVPzZplmTE2VTx?= NX24eJV2S3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjN3IN88US=> NYL5dXhbOjR7MECyOlY>
U87MG M1yyXWN6fG:2b4jpZ{BCe3OjeR?= M1rUd|czKGh? MVHEUXNQ NX:zb|NtS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjl6IN88US=> MmTHNlQ6ODB{Nk[=
A2780 Mn:1SpVv[3Srb36gRZN{[Xl? NH;3UlkyKGh? M4nRdWROW09? M{fFS2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6wOVUh|ryP MXmyOFkxODJ4Nh?=
DU145 MnLISpVv[3Srb36gRZN{[Xl? Mm\BNUBp M2HuOWROW09? Mkn3TY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? MUSyOFkxODJ4Nh?=
A2780 M360[GZ2dmO2aX;uJGF{e2G7 Ml\XNUBp MYjEUXNQ M17SdmlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP M3PNXlI1QTByMk[2
MCF7 NFHVPINHfW6ldHnvckBCe3OjeR?= MljSNUBp Mnr4SG1UVw>? MYHJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCHNUS1T{BufXSjboStcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMTFOwG0> NHSwU3QzPDlyMEK2Oi=>
U87MG NGG2b5lHfW6ldHnvckBCe3OjeR?= MV2xJIg> MWPEUXNQ NV;vRpdPUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJHU5P02JIHPlcIx{KHerdHigSWM2OCCxZjCwMlE{KM7:TR?= NWO0[pBmOjR7MECyOlY>
A2780 NFj1NVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW1e4JYPzJiaB?= MV3EUXNQ NFjsXJVGSzVyPUCuOVIh|ryP M{PKOlI1QTByMk[2
SKMES-1 MYnDfZRwfG:6aXOgRZN{[Xl? M4f5OVEh|ryP M{jOPVczKGh? MorpTY5lfWOnczDj[YxtKGSnYYTo M3GzSlI3ODF|M{G4
H596 MlTYSpVv[3Srb36gRZN{[Xl? NHPqZo4yKM7:TR?= NHn3XZBKdXCjaYLzJINmdGxibXnndoF1cW:w MnjYNlYxOTN|MUi=
HCC2450 Mk\KSpVv[3Srb36gRZN{[Xl? M{f5WVEh|ryP MXvJcZBicXK|IHPlcIwhcW64YYPpc44> MV:yOlAyOzNzOB?=
A549 MYHGeY5kfGmxbjDBd5NigQ>? NWe5fG5LPTByIH7N MoW4OFghcA>? MXrEUXNQ M2HISmlvcGmkaYTzJGFsfCCjY4TpeoF1cW:w NYTjUIhrOjV7M{eyPVk>
A549 M1rOVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmxJO69VQ>? Ml7sO|IhcA>? NV;abW5bTE2VTx?= NF\iZ21KdmirYnn0d{Bk\WyuIHfyc5d1cA>? NIHpc3AzPTl|N{K5PS=>
H522 NHjLRXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzJbZJWOSEQvF2= NIjv[5k4OiCq MVLEUXNQ Mm\zTY5pcWKrdIOgZ4VtdCCpcn;3eIg> NV\YTXZNOjV7M{eyPVk>
LNCaP NHHaWmVHfW6ldHnvckBCe3OjeR?= M1zZXVEh|ryP M4PFNXN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| NFu4PVkzPTN4MEe5PS=>
LNCaP95 NYCx[pNsTnWwY4Tpc44hSXO|YYm= Mn7UNUDPxE1? NV\HPYYzW3WycILld5NmeyCyLVHLWEBt\X[nbIO= NV7FN5A2OjV|NkC3PVk>
HCT-15 NVXQXYRJSXCxdH;zbZMhSXO|YYm= MXWxNEDPxE1? MXG0PEBp NXK5XWozTE2VTx?= NWLjXGZTUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVE2KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NGLNS4EzPTF3MkK0OS=>
HCT-116 M4LuWmFxd3Sxc3nzJGF{e2G7 M3Pt[VExKM7:TR?= M{P0TVQ5KGh? NIG5dGZFVVOR NXuzdVNEUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVEyPiClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u MlnCNlUyPTJ{NEW=
NCI-H460 NHG3[GdCeG:2b4Ppd{BCe3OjeR?= MV[xNEDPxE1? M{\aNFQ5KGh? NEe3RYRFVVOR MYfJcoR2[2W|IHHwc5B1d3OrczDpckBPS0lvSES2NEBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NX;UfW55OjVzNUKyOFU>
SKOV-3 MWTBdI91d3OrczDBd5NigQ>? NH;LS|IyOCEQvF2= M4nBPFQ5KGh? NEHuN5JFVVOR M2HQXmlv\HWlZYOgZZBweHSxc3nzJIlvKFONT2[tN{Bk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NETvcJgzPTF3MkK0OS=>
BSY-1 MoTtRZBwfG:|aYOgRZN{[Xl? Mn7ENVAh|ryP Mn36OFghcA>? NIT2TpdFVVOR MUPJcoR2[2W|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v MnvHNlUyPTJ{NEW=
MKN-1 Mn;YRZBwfG:|aYOgRZN{[Xl? NHPWSXgyOCEQvF2= NGDMOXE1QCCq MknZSG1UVw>? NV\lSXV6UW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NGTPc5YzPTF3MkK0OS=>
NCI-H522 NXnzTG5VSXCxdH;zbZMhSXO|YYm= M3;RT|ExKM7:TR?= MnnuOFghcA>? MlXFSG1UVw>? NH\oeXlKdmS3Y3XzJIFxd3C2b4Ppdy=> NU\lNZRnOjVzNUKyOFU>
OVCAR-3 Ml6zRZBwfG:|aYOgRZN{[Xl? MV:xNEDPxE1? MmqxOFghcA>? NIG1fYlFVVOR NVnUXolKUW6mdXPld{BieG:ydH;zbZM> M37pOVI2OTV{MkS1
HBC-5 NUXTdGlZSXCxdH;zbZMhSXO|YYm= NULLZ3hLOTBizszN MYW0PEBp NULrUFBoTE2VTx?= M4jVbWlv\HWlZYOgZZBweHSxc3nz NVfhTG9LOjVzNUKyOFU>
RXF-631L MmD0RZBwfG:|aYOgRZN{[Xl? M4TlUFExKM7:TR?= NXu4R2w1PDhiaB?= NEGySZhFVVOR M{fsb2lv\HWlZYOgZZBweHSxc3nz NHfpVZkzPTF3MkK0OS=>
MKN-45 NUXVNodESXCxdH;zbZMhSXO|YYm= MmfhNVAh|ryP NHHQNpU1QCCq NYjkd2c{TE2VTx?= MnTBTY5lfWOnczDhdI9xfG:|aYO= Mkf4NlUyPTJ{NEW=
BON-1 MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\LOVAxKG6P NUH4XpV{OTBiZB?= NVvMcWRHTE2VTx?= MX;Jcohq[mm2czDj[YxtKGe{b4f0bC=> NVXRNodKOjVyMk[yPVI>
BON-1 MU\GeY5kfGmxbjDBd5NigQ>? MlL0OVAxKG6P NUHmNIF3PCCq MYfEUXNQ NYCxTnhZUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> NEXMOYYzPTB{NkK5Ni=>
QGP-1 M1i1OGZ2dmO2aX;uJGF{e2G7 NYfvSZhQPTByIH7N NXXt[I5RPCCq M33ZN2ROW09? NWXLO|lyUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> MnXkNlUxOjZ{OUK=
Huh7 NVSwbmJKTnWwY4Tpc44hSXO|YYm= Mnq2NUDPxE1? NYrVVnJsOSCq NHLQXJdFVVOR MoXvTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR? MYmyOVAxPDRyMx?=
BNL MXXGeY5kfGmxbjDBd5NigQ>? M2O5RlEh|ryP M3fzXFEhcA>? MmPWSG1UVw>? NHqz[XNKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZ? M1;VbFI2ODB2NECz
MDA-MB-175 NGizcHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q1S|Eh|ryP MnrZOUBl MlrTSG1UVw>? M3;VOWlEPTB:MTFOwG0> Mo\JNlQ5Pzl5OU[=
MDA-MB-134 NYXRd3FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH5WVg2OSEQvF2= NXqxUmd5PSCm MoDQSG1UVw>? MmPmTWM2ODxzIN88US=> M{XHTFI1QDd7N{m2
HCC1500 NGC3WZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fHe|Eh|ryP M3[0dlUh\A>? NUnvWYVKTE2VTx?= NUXhWGVlUUN3MEyxJO69VQ>? MlizNlQ5Pzl5OU[=
EFM-19 M4jmUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrpNUDPxE1? MXi1JIQ> NF\jSoJFVVOR NVzPR4R6UUN3MEyxJO69VQ>? Ml34NlQ5Pzl5OU[=
ZR-75-30 NWfzZmRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTSNUDPxE1? NGmwR|g2KGR? MVnEUXNQ Mly0TWM2ODxzIN88US=> NXzuUldqOjR6N{m3PVY>
MDA-MB-361 NWG3[lRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXmNUDPxE1? NVHLcXBDPSCm NWDvXWlLTE2VTx?= MYrJR|UxRDFizszN MVyyOFg4QTd7Nh?=
T-47D NWrofGdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTqTZN2OSEQvF2= M1P5cVUh\A>? MkHwSG1UVw>? MYTJR|UxRDFizszN MViyOFg4QTd7Nh?=
SK-BR-3 MmXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O1b|Eh|ryP MWC1JIQ> NIHpflhFVVOR Mki3TWM2ODxzIN88US=> NXu1e3hbOjR6N{m3PVY>
UACC-732 MlLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojoNUDPxE1? NHTROIo2KGR? MYnEUXNQ NEnxc3JKSzVyPEGg{txO NWPvfYUyOjR6N{m3PVY>
BT-474 NH7oZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOxJO69VQ>? M33T[lUh\A>? MVHEUXNQ NWLzdG9YUUN3MEyxJO69VQ>? MoXYNlQ5Pzl5OU[=
HCC202 M1\yfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Kz[|Eh|ryP NV:0Z4ZNPSCm NWHYOWZtTE2VTx?= NGDJeZZKSzVyPEGg{txO NXW5S2NCOjR6N{m3PVY>
MCF7 NYPKVod{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLkN3EyKM7:TR?= MkP3OUBl NVPPWZk2TE2VTx?= M3HKfmlEPTB:MTFOwG0> MWSyOFg4QTd7Nh?=
MDA-MB-415 NVHlUmxsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7nNUDPxE1? NV;SU4hpPSCm MmDESG1UVw>? NEfQOmtKSzVyPEGg{txO Ml\6NlQ5Pzl5OU[=
MDA-MB-453 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVSxJO69VQ>? MmqxOUBl MkC3SG1UVw>? Mnm3TWM2ODxzIN88US=> MnyxNlQ5Pzl5OU[=
ZR-75-1 M17QO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP2NFY4OSEQvF2= NVnh[4prPSCm NXjqcpBoTE2VTx?= NHjaWFNKSzVyPEGg{txO M2DmSFI1QDd7N{m2
HCC38 NXzvPVlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXsNUDPxE1? NGr5XmI2KGR? NVPKN|FPTE2VTx?= MofCTWM2ODxzIN88US=> MlPDNlQ5Pzl5OU[=
HCC1419 NGHQU|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C5N|Eh|ryP NYDsXXlQPSCm MWDEUXNQ M2PIWWlEPTB:MTFOwG0> M4\2blI1QDd7N{m2
UACC-812 M3TZPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWGyXJBUOSEQvF2= NYnNZ2lCPSCm NFnkRmlFVVOR M13VVWlEPTB:MTFOwG0> Mn3rNlQ5Pzl5OU[=
HCC1187 M1jBZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWro[HFSOSEQvF2= MXy1JIQ> MlzaSG1UVw>? MWLJR|UxRDFizszN MlrONlQ5Pzl5OU[=
KPL-1 MkjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrLW2kyKM7:TR?= NE\UfZQ2KGR? NWXJe296TE2VTx?= MXzJR|UxRDFizszN MYmyOFg4QTd7Nh?=
SUM-225 NH\CdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfCZmkyKM7:TR?= NW\0fllqPSCm NGfsZ2ZFVVOR NE\6fZpKSzVyPEGg{txO NUixOJg5OjR6N{m3PVY>
EFM-192A NX\LV3R2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV2yZVkzOSEQvF2= M{e1RlUh\A>? NYnJfGdFTE2VTx?= NUHTTllLUUN3MEyxJO69VQ>? NYr2WI9wOjR6N{m3PVY>
JIMT-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjZcGc5OSEQvF2= NWHXVXE6PSCm Mn;NSG1UVw>? M4LjXWlEPTB:MTFOwG0> NEHSO5ozPDh5OUe5Oi=>
HCC1143 NFHlO|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vwfFEh|ryP MVe1JIQ> NHntU49FVVOR MlS2TWM2ODxzIN88US=> NVPseG1EOjR6N{m3PVY>
HCC2218 NYTh[o9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z2bFEh|ryP M2fH[|Uh\A>? NFnnTW5FVVOR NXrSSYZDUUN3MEyxJO69VQ>? M{jkSlI1QDd7N{m2
MDA-MB-468 NHHoWo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO4NUDPxE1? NWTaSnliPSCm M3nmcWROW09? NES4XoxKSzVyPEGg{txO M1\ZWFI1QDd7N{m2
BT-20 NHnrUWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTHZYpiOSEQvF2= M{jRbFUh\A>? M3KybWROW09? MkK5TWM2ODxzIN88US=> NGPaRnIzPDh5OUe5Oi=>
MDA-MB-435 MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;aclEh|ryP NYPaTVNYPSCm M2O1OGROW09? NXXnRYh2UUN3MEyxJO69VQ>? NVHJR|hvOjR6N{m3PVY>
BT-549 NYXz[IE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH4S2pkOSEQvF2= NHfkPGo2KGR? MlPHSG1UVw>? NYL0R|BCUUN3MEyxJO69VQ>? M2TCWlI1QDd7N{m2
HCC1806 NGTINXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DwcVEh|ryP NVXadZdtPSCm MV\EUXNQ NHnsNVNKSzVyPEGg{txO NYHMU2lEOjR6N{m3PVY>
HCC1937 NFLXfmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOxJO69VQ>? M37W[FUh\A>? M{HQOmROW09? MXLJR|UxRDFizszN NWPBWmFuOjR6N{m3PVY>
Hs578T NVfDXXl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHP2cWEyKM7:TR?= NXfPfmZ3PSCm NVjuWI11TE2VTx?= Mnj4TWM2ODxzIN88US=> M3vPUVI1QDd7N{m2
LN18 NFrVPIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfhUGNSOjBizszN M2LtcFczKGh? M{jpUGROW09? MlOzTWM2ODx3IN88US=> M3vrUFI1PzRzMEe0
LN229 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELvbmgzOCEQvF2= MojkO|IhcA>? MljaSG1UVw>? MlTBTWM2ODx3IN88US=> NHfMRWEzPDd2MUC3OC=>
LNZ308 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nXeVIxKM7:TR?= NEPDN204OiCq MlXqSG1UVw>? MX7JR|UxRDVizszN NGLr[XAzPDd2MUC3OC=>
T98G M1fScWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7JclAzOCEQvF2= MUm3NkBp MmrCSG1UVw>? MoLKTWM2ODx3IN88US=> NV22N4JHOjR5NEGwO|Q>
U87 MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrid|AzOCEQvF2= MXu3NkBp Ml;qSG1UVw>? M1jtUmlEPTB:NTFOwG0> M2LBZ|I1PzRzMEe0
LN18 NVrzUpdbTnWwY4Tpc44hSXO|YYm= NE\6bWY2KM7:TR?= NH73S5czPCCq M2SwfGROW09? Mn;lTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MVqyOFc1OTB5NB?=
LNZ308 NVjrcFNpTnWwY4Tpc44hSXO|YYm= NFP6V3Y2KM7:TR?= NGKxb2YzPCCq M1e4d2ROW09? M3;lNWlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? M{\s[lI1PzRzMEe0
Saos-2 MXHGeY5kfGmxbjDBd5NigQ>? NEX2Z|I2OCEQvF2= M3nue|Q5KGh? MULJcohq[mm2czDj[YxtKGmwdnHzbY9v MlXyNlQ4Ojd4NkC=
MG-63 NXr3UFV3TnWwY4Tpc44hSXO|YYm= M4n1XFUxKM7:TR?= NWCzV2l5PDhiaB?= M4jP[mlvcGmkaYTzJINmdGxiaX72ZZNqd25? MYGyOFczPzZ4MB?=
SJSA-1 MXPGeY5kfGmxbjDBd5NigQ>? MoO5OVAh|ryP NHn0WFI1QCCq MXHJcohq[mm2czDj[YxtKGmwdnHzbY9v M1XnO|I1PzJ5Nk[w
Saos-2 M4f2VmZ2dmO2aX;uJGF{e2G7 NEH1cG42OCEQvF2= NES0bWQ1QCCq M3Hn[WlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> M4nmSFI1PzJ5Nk[w
MG-63 NXrUdYdiTnWwY4Tpc44hSXO|YYm= NG\1Xpg2OCEQvF2= MYS0PEBp M2LhZmlvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> NUT1WlIxOjR5Mke2OlA>
SJSA-1 MoW0SpVv[3Srb36gRZN{[Xl? NG\VVHY2OCEQvF2= M1iySVQ5KGh? MVHJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u MVGyOFczPzZ4MB?=
Saos-2 MlvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPTRVU2OCEQvF2= M2HVcFQ5KGh? M1nNWmlvcGmkaYTzJINmdGxidnnhZoltcXS7 M3zuelI1PzJ5Nk[w
MG-63 NIrH[Y1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLDfYpOPTBizszN NHXS[Zg1QCCq MV7Jcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? MWCyOFczPzZ4MB?=
SJSA-1 NX[4Z|NyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PNTFUxKM7:TR?= NY\yVI9RPDhiaB?= M4DOUGlvcGmkaYTzJINmdGxidnnhZoltcXS7 MYKyOFczPzZ4MB?=
FaDu MWHGeY5kfGmxbjDBd5NigQ>? MUO1JO69VQ>? MofqNlQhcA>? MnewSG1UVw>? NVj4cXVVWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NVfRT3p[OjR4M{GxOFc>
EMT6 MYDGeY5kfGmxbjDBd5NigQ>? MU[1JO69VQ>? MV6yOEBp MlPZSG1UVw>? MU\S[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= MViyOFY{OTF2Nx?=
HCT116 MUfGeY5kfGmxbjDBd5NigQ>? NFHzUmg2KM7:TR?= MX[yOEBp Mo\tSG1UVw>? NUmyZlJOWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MYiyOFY{OTF2Nx?=
U87 NY\ER4M3TnWwY4Tpc44hSXO|YYm= Ml7nOUDPxE1? MUeyOEBp NWnPdVZrTE2VTx?= NVT0PHNVWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NWrPXnd4OjR4M{GxOFc>
GBM MYDBdI9xfG:|aYOgRZN{[Xl? NV3XeWFTOs7:TR?= NFqyXYE1QGh? MonOSG1UVw>? MVXpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5 NHn1Um4zPDVyMES5Ni=>
BON NXjJTnBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXqxMVXPxE1? MVe3Nog> NFS0TZFl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NGC2UJkzPDR2M{WyNy=>
BON NFLaNo9CeG:ydH;zbZMhSXO|YYm= NIqxN|YyNTYQvF2= MmTTNlRp MVLpcoNz\WG|ZYOgZZBweHSxc3nz MY[yOFQ1OzV{Mx?=
H1975 M3;adWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;IN4dYOC5|LUmuOu69VQ>? NWjEN4xwPzKq MXLEUXNQ Ml3uTWM2OD1zLkO4Oe69VQ>? MVyyOFM{Pzh2Nh?=
H1975 NU\Se|hESXCxcITvd4l{KEG|c3H5 NWnFXJJtOs7:TR?= MX6yOIg> M2LTN2ROW09? MmPybY5kemWjc3XzJIFxd3C2b4Ppd{Bz[XSnIIPp[45q\mmlYX70cJk> MXGyOFM{Pzh2Nh?=
T-ALL M2Dy[WFxd3C2b4Ppd{BCe3OjeR?= MknPZoV1f2WnbjCxMlQh[W6mIEWuN{BuVSCjdDCyOIgh[W6mIECuPUBidmRiNT61JI1OKGG2IES4bEBqdiCmaX\m[ZJmdnRiY3XscEBtcW6n MknKNlQhd3JiNEjo MXfEUXNQ NIflfG1i\m[nY4TzJJRp\SCSSUPLJJBifGi5YYmgbY4hXC2DTFygZ4VtdCCuaX7ldy=> NVTZfHJXOjR|MUC3N|Y>
BCR-ABL NX\KNm4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfKdZpDOC5{NT2xNO69VQ>? MlvWOIQ> NGKxW2l{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w NXH5[JdKOjR{NES2NVI>
LC-1/SQSF MmLYSpVv[3Srb36gRZN{[Xl? NUSyfm1QO87:TR?= MUWyOIg> MUPEUXNQ NVnkUmxj\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt MoPpNlM6QDByOUO=
Primary CLL cells M1vNUWFxd3C2b4Ppd{BCe3OjeR?= Mor1NU0yOM7:TR?= MnHwOFhp MlLPbY5lfWOnczDhdI9xfG:|aYOgbY4hS0yOIHPlcIx{KGmwZHXw[Y5l\W62IH;mJJBzd2ewb4P0bYMhdWG{a3Xydy=> NIXoT|UzOzh3MEiwOy=>
Primary CLL cells M1W0TWtqdmG|ZTDBd5NigQ>? MUey{txO NGPNZZU{OG2rbh?= MWDk[YNz\WG|ZXSgVGk{UyCjY4Tpeol1gQ>? NWDBW4p[OjN6NUC4NFc>
Primary CLL cells M3rwSWN6fG:2b4jpZ{BCe3OjeR?= NY\SRmh[Os7:TR?= M3v3[|I1cA>? MU\pcoR2[2W|IHPlcIwh[3m2b4TvfIlkcXS7 MXuyN|g2ODhyNx?=
human NSCLC cell lines M4e2WGFxd3C2b4Ppd{BCe3OjeR?= M36xU|AvOTJ3LUVOwG0> NHnwZoYzPGh? M4C5WWROW09? NFX6PVlKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> M3jIN|I{PTZ{NEey
human HCC cell lines M{HTNWNmdGxidnnhZoltcXS7IHHzd4F6 NFrMZowxNjByNT2x{txO NVHTe2VnPDiq NVjXbYlnUUN3ME2x{txO NHPOXoEzOzR6OUm5PS=>
Huh7 NGPnS3FMcW6jc3WgRZN{[Xl? MYCx{txO MnHPOFhp M2HOXpNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NUflfJJnOjN2OEm5PVk>
SK-HEP1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqxMVIx|ryP NHGwPWo4Omh? MknoSG1UVw>? MmX6TWM2OO,:nEJOwG0> M1TWN|I{PDd7MUO2
786-0 M1faRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjzNU0zOM7:TR?= NVLWfVN5PzKq M{HUbmROW09? MWTJR|Ux97zeMd88US=> MlvmNlM1PzlzM{[=
JVM2 MlvjR5l1d3SxeHnjbZR6KGG|c3H5 M4TQXVAvOi1{MN88US=> MVi3Nog> MmDFSG1UVw>? NVj6WXZbUUN3ME2wMlnPxE1? MVuyN|I{QDZ|OR?=
EHEB NFjoSI5EgXSxdH;4bYNqfHliYYPzZZk> NVOyPJdkOC5{LUKw{txO M4fM[lczcA>? M4j4VGROW09? NWjNS29UUUN3ME2wMlfPxE1? NFvHdoYzOzJ|OE[zPS=>
MEC2 MkTIR5l1d3SxeHnjbZR6KGG|c3H5 NFTGRpIxNjJvMkFOwG0> NVnCeos{PzKq NWHu[VdWTE2VTx?= Mlu4TWM2OD1yLkhOwG0> NIHBc4MzOzJ|OE[zPS=>
primary B-CLL lymphocytes MV3BdI9xfG:|aYOgRZN{[Xl? MmeyTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? NIrUPW8zPGh? M4LVU2ROW09? NUHBdJJnUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>? M3jZ[VI{OjN6NkO5
primary B-CLL lymphocytes NXn4NI15U2mwYYPlJGF{e2G7 Mkn3TWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MmPMNlRp NV2xV2RocW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> NHL1R2MzOzJ|OE[zPS=>
human NSCLC M1P1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnmxNE42NTMQvF2= NGLhXos4Omh? NXO1T4J2UUN3ME2x{txO NIfDfHMzOjd6MUO5Ny=>
human NSCLC NVjJXY5lU2mwYYPlJGF{e2G7 Mk\yNe69VQ>? M3ewTVI1cA>? MYjpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 MY[yNlc5OTN7Mx?=
Y1 cell line NUDVZoJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPOXXFKOC5zzszNM|HPxE1? MmXNNlRp NGW1VotFVVOR NFT6RodqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?= M{DEOlIzPjl{OUC0
PIK3CA-mutant MCF7 MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjjXVZiT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= NF\sZWE4Omh? NVn1fHBWT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= NEDy[ZkzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 NFHubZBMcW6jc3WgRZN{[Xl? NX;3O5dJUUN3ME2xNVTDuTOwTR?= M3HOXlczcA>? NUXFe2JrUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=> NVfiRZBmOjJ4NUO5Olc>
MCF7-myr-Akt MkK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nQS2dKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P MV:3Nog> Mlv1S2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? MXGyNlY2Ozl4Nx?=
colon cancer cell lines NHTVSHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjJbZMxNTFyzszN MlKyO|Jp NGm3NJNFVVOR NUTGbpBqUUN3ME2x{txO MojmNlI2PDN6NUe=
gastric cancer cell lines MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnEUYgxNTFyzszN MkDGO|Jp M4XnWWROW09? NVfiSHhKUUN3ME2yMVXPxE1? MVWyNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45 NEHhRWZCeG:ydH;zbZMhSXO|YYm= M{\hZ|LPxE1? NXjkRVI{PDiq M{TCcpNpcW[2IHnuJGczKHCqYYPl NXHBNo1mOjJ3NEO4OVc>
HT-29 and HCT-116 M1\IcWNie3Cjc3WgZZN{[Xl? NVj6c2FrPc7:TR?= NX7DU4FMOjSq MYjpcoR2[2W|IHPhd5Bie2ViYXP0bZZqfHl? NUn0[IxiOjJ3NEO4OVc>
MM cell lines NVP6d5FIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M125[VEx|ryP M3f3XVI1cA>? M{e2R2ROW09? NUL0R41oUUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn MkmyNlIzODd2OEW=
ARP-1 MlPVRZBweHSxc3nzJGF{e2G7 NF;xV20yOM7:TR?= NYr2fmRIOjSq MYLEUXNQ M1vaSolv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36= MYeyNlIxPzR6NR?=
SNU-601 Mny2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LQSFczcA>? NELWdIpFVVOR MkjzTWM2OD1yLkixOuKyOC5yNkROwG0> M3P5[FIzOTV7OEG0
SNU-1 MkfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHFdJI4Omh? M{PyWmROW09? NVn5fHBqUUN3ME2xMlA5OsLzMD6wNljPxE1? NXThVIZUOjJzNUm4NVQ>
SNU-668 MnjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLtfFE4Omh? M2nES2ROW09? NUDr[Hh[UUN3ME2xMlU4QcLzMD6wO|TPxE1? NHnoZYkzOjF3OUixOC=>
AGS NYSxRVBIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUW3Nog> MUPEUXNQ NX;TOYw5UUN3ME2xMlcyPMLzMD6xNVfPxE1? NEnUTm4zOjF3OUixOC=>
SNU-216 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1W5O|czcA>? Ml7nSG1UVw>? NXjDUG05UUN3ME2yMlY6OsLzMD6wPFLPxE1? M3f3eVIzOTV7OEG0
SNU-5 NHTkZ3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV63Nog> MXLEUXNQ NXvDPHl[UUN3ME2xMlM2OcLzMD6wPVHPxE1? NWS4OGp6OjJzNUm4NVQ>
SNU-638 NE\SUXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:3Nog> NV31elVJTE2VTx?= M4D6N2lEPTB;Mj6yPFLDuTBwMEWz{txO NXTXdI9OOjJzNUm4NVQ>
SNU-16 NYSzSplkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDNO|Jp MVjEUXNQ NITsc|VKSzVyPUGuOVc{yrFyLkCwNe69VQ>? Ml;QNlIyPTl6MUS=
SNU-484 MkPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjlO|Jp NWXVZ2xuTE2VTx?= NUfLd3d[UUN3ME2xMlczQMLzMD6wOFXPxE1? NHLpcIYzOjF3OUixOC=>
SNU-620 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fkR|czcA>? M1uzW2ROW09? Ml\ZTWM2OD1{LkmzPeKyOC5yMEJOwG0> NHOxbWwzOjF3OUixOC=>
SNU-719 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLlO|Jp M{LiRmROW09? MknpTWM2OD1|LkCzO:KyOC5yM{NOwG0> M4CzU|IzOTV7OEG0
glioma cell lines NYO3ZlN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPHSohsPzKq NXW3PXhLUUN3ME2xMVLPxE1? NWHmc4xmOjJyNkWwPFA>
U87 NGj0WY5CeG:ydH;zbZMhSXO|YYm= MoHxNu69VQ>? NFT3bog4Omh? NVPzdpU3cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> NWHzbmN4OjJyNkWwPFA>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT (T308) / p-AKT (S473) / AKT; 

PubMed: 27283525     


Left western blots showing levels of pAkt (T308), pAkt (S473) and total Akt in U87 cells exposed to buparlisib for 72 h. Right densitometric assessment of western blots, showing relative changes in phosphorylation.

p-FOXO3a (S253) / FOXO3a; 

PubMed: 28036259     


Cells were treated with 0.5 μM BKM120 for 24 h and cell lysates were immunoblotted with the indicated antibodies. Actin was used as the loading control.

Nuclear NF-κB p65 / NF-κB p65; 

PubMed: 26673665     


Western blots show BKM120 downregulating pAKT, nuclear NF-κB p65 and total NF-κB p65 in MDR and their parental cells. β-actin was used as a loading control for pAKT, AKT and total NF-κB p65. Lamin B was used as a loading control for nuclear NF-κB p65. 

p-ERK / ERK / LC3; 

PubMed: 27572309     


The indicated cell lines were exposed to different concentrations of BKM120 as indicated for 8 h A. or with 2 μM BKM120 for the indicated times B. The cells were then harvested for preparation of whole-cell protein lysates and subsequent Western blot analysis to detect the given proteins.

p-STAT3 / STAT3 / p-ERK / ERK / p-S6; 

PubMed: 29928341     


Western blot analysis of H460 and H2126 cell lysates using specific antibodies to phosphorylated or total proteins of STAT3, ERK1/2, AKT, S6 or GAPDH (loading control). The cells were treated with increasing concentrations of BKM120 for 24 h.

p-MET / MET; 

PubMed: 29928341     


The expression of phosphorylated or total forms of MET protein was analyzed by western blotting. 

27283525 28036259 26673665 27572309 29928341
Immunofluorescence
FOXO3a; 

PubMed: 28036259     


Cells were cultured on coverslips to approximately 60% confluency and then treated with 1 μM BKM120 for an additional 24 h. Immunofluorescence staining was performed using an anti-FOXO3a antibody and the nuclei were stained with DAPI. Scale bar, 20 μm.

28036259
Growth inhibition assay
Cell viability; 

PubMed: 26673665     


Dose-response curves were used to calculate the IC50 of BKM120 for MCs of MCF-7/A02 cells (upper) and CALDOX cells (lower).

26673665
体内研究 BKM120按30, 60, 或100 mg/kg剂量作用于A2780移植瘤,完全抑制pAKTser473。BKM120按 30和 60 mg/kg剂量作用于U87MG神经胶质瘤模型,显示抗癌活性。[1]BKM120每天按5μM/kg剂量处理具有持久生命力的ARP1 SCID鼠模型,导致肿瘤体积和K链水平明显降低。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[2]
- 合并

PI3K 生化实验(ATP 消耗实验):

BKM120溶于DMSO中,按每孔1.25 µL直接加到黑色384孔板上。开始反应, 25 µL 10nM PI3K和5 µg/mL 1-α-磷酸肌醇(PI)加到实验 buffer (10 mM Tris pH 为7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT,及0.05% CHAPS),然后加到每孔中,随后在实验buffer中加入25 µL 2 µM ATP。反应进行直到50% ATP被消耗,然后加入25 µL KinaseGlo溶液终止反应。终止的反应温育5分钟,然后通过荧光测定残留的ATP。
细胞实验:[1]
- 合并
  • Cell lines: A2780细 胞
  • Concentrations: 0-6.6 μM
  • Incubation Time: 3天
  • Method: A2780细胞培养在含10% FBS,L-谷氨酸,丙酮酸钠和抗生素的DMEM培养基上。细胞按每孔103个细胞的密度接种在相同培养基上,温育3到5小时。稀释溶于20 mM DMSO中的BKM120。2 µL稀释的BKM120溶液加到细胞培养基上, (浓度为0-6.6 µM)。等体积(100 µL)溶液加到96孔板中,在37oC下温育3天。使用Trilux读取荧光值而测定抑制细胞增殖的效果
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带U87MG 和A2780移植瘤的雌性裸鼠
  • Formulation: 15% Captisol
  • Dosages: ~60 mg/kg
  • Administration: 每天口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 82 mg/mL (199.8 mM)
Ethanol 2 mg/mL (4.87 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+30% PEG 300+ddH2O
15mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 410.39
化学式

C18H21F3N6O2

CAS号 944396-07-0
储存条件 粉状
溶于溶剂
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02614508 Terminated Drug: Buparlisib|Drug: Ibrutinib|Biological: Ofatumumab Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma Emory University|Novartis January 2016 Phase 1
NCT01613677 Withdrawn Drug: BKM120 Treatment for Metastatic or Locally Advanced Cervical Cancer Novartis Pharmaceuticals|Novartis November 2015 Phase 2
NCT01953445 Withdrawn Drug: paclitaxel|Drug: BKM120 Breast Neoplasms Washington University School of Medicine August 2014 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID