Alpelisib (BYL719)

For research use only. Not for use in humans.

目录号：S2814 中文名称：阿培利司

Alpelisib (BYL719) Chemical Structure

CAS No. 1217486-61-7

Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 4864.29 现货
RMB 3034.22 现货
RMB 4650.12 现货
RMB 7115.91 现货
RMB 10401.3 现货
RMB 13677.3 现货
RMB 21867.3 现货
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客户使用Selleck生产的Alpelisib (BYL719)发表文献127篇：

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。
靶点
PI3Kα [1]
(Cell-free assay)
5 nM
体外研究

BYL719抑制含有PIK3CA突变体的乳腺癌细胞系的增殖，与PI3K/Akt通路各种下游信号组分的抑制相关。[1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Detroit562 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT1NE4yNTFyMDFOwG0> MVq3NkBp NHzONmtKSzVyPUGuNVAh|ryP MorzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
SNU-1076 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLhNE4yNTFyMDFOwG0> NE\QSYQ4OiCq MXPJR|UxRTZwOEKg{txO MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3MEW0PUc,OjV3NUC1OFk9N2F-
SNU-1066 M4GyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfoNE4yNTFyMDFOwG0> MWW3NkBp M17XUWlEPTB;MT6xN{DPxE1? NIrYT3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW1NFU1QSd-MkW1OVA2PDl:L3G+
FaDu NE\MPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX6xU2FWOC5zLUGwNEDPxE1? MV[3NkBp MnX3TWM2OD1zOT62OkDPxE1? M1PVZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWwOVQ6Lz5{NUW1NFU1QTxxYU6=
SNU1041 NW\FSYxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvJWGdXOC5zLUGwNEDPxE1? MnnHO|IhcA>? NWT4dW4{UUN3ME2yNE43PSEQvF2= M1v4dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWwOVQ6Lz5{NUW1NFU1QTxxYU6=
SCC25 MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn1UIwxNjFvMUCwJO69VQ>? NX[xeWJCPzJiaB?= MUTJR|UxRTR7LkOwJO69VQ>? MmLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
BON-1 MlXXSpVv[3Srb36gRZN{[Xl? NWfCTFJ4OS9zMDFOwG0> NFPTV5k1KGh? M2HGfolvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| MlO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMk[yPVIoRjJ3MEK2NlkzRC:jPh?=
QGP-1 MYjGeY5kfGmxbjDBd5NigQ>? NULtd41bOS9zMDFOwG0> Mkf3OEBp M{D5S4lvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| NFfTS|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyOlI6Oid-MkWwNlYzQTJ:L3G+
MG-63 NGT4NXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPuTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= MojSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkG3PVAoRjJ2OU[xO|kxRC:jPh?=
HOS NVHYS4dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjKSYs6UUN3ME2xOUDPxE4xvJygTWM6OD12MjFOwG0> NYDHeGo4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OlE4QTBpPkK0PVYyPzlyPD;hQi=>
MOS-J NV7xTHRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf6TJB4UUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> NXX1S5VvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OlE4QTBpPkK0PVYyPzlyPD;hQi=>
POS-1 M4[0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljvTWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl4MUe5NEc,OjR7NkG3PVA9N2F-
92.1 NHz2U2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlKwOVAxNTJyMECgcm0> MlrkOUBl NXrHfop2cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NEfieWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW2N|U1OCd-MkS1OlM2PDB:L3G+
Mel270 NETq[I1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXhZZQ2ODBvMkCwNEBvVQ>? NWPib|V4PSCm MY\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NUnrV4poRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OlM2PDBpPkK0OVY{PTRyPD;hQi=>
Omm1.3 NEL6W2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjyRYc2ODBvMkCwNEBvVQ>? NXXKT|VxPSCm MVjpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NFzmR2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW2N|U1OCd-MkS1OlM2PDB:L3G+
Omm1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILnSGQ2ODBvMkCwNEBvVQ>? MkfuOUBl NVu3WnB1cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NInySHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW2N|U1OCd-MkS1OlM2PDB:L3G+
C918 NF;aZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjXOWZZPTByLUKwNFAhdk1? MWq1JIQ> MoXYbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4M{W0NEc,OjR3NkO1OFA9N2F-
Mel290 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTjeFY2ODBvMkCwNEBvVQ>? NXnySJc2PSCm NEDQPJhqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4M{W0NEc,OjR3NkO1OFA9N2F-
OPM2 MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjJbFcxNjVvMj61JO69VQ>? MXm0PEBp NUjEU2NtcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3jvVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1NVIyLz5{NESwOVEzOTxxYU6=
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U266 NH\obVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnt[JdGOC53LUKuOUDPxE1? M1i2ZlQ5KGh? MnPsbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUGyNUc,OjR2MEWxNlE9N2F-
MM1R MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmwMlUuOi53IN88US=> MkO5OFghcA>? M{XSbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWCxR3RtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFUyOjFpPkK0OFA2OTJzPD;hQi=>
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SKBR3 NYW4c2RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXOzN{DPxE1? NHfFT|A2KGR? MnnubY5pcWKrdIOgN|XwxIViY3XscEBoem:5dHi= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
MDA453 NUP3Z5VGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvaN|Mh|ryP NFvQeJg2KGR? MYnpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= Ml36QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ|OUG4O|k4RC:jPh?=
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MDA361 NUfnRllvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrnN|Mh|ryP NV\ZOYJWPSCm NH\VVYFqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> NWHVN45qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
BT474 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmzN{DPxE1? MknMOUBl NF33PYVqdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> M{DaOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
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NCL-N87 NXL1T4R7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfKN|Mh|ryP NUi3PFFLPSCm NVXnNY1OcW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
UACC812 NIG0PI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjCN|Mh|ryP NIXpdpI2KGR? MWTpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NFTzeZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mxPFc6Pyd-MkO5NVg4QTd:L3G+
HCC2218 MoTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[xTlM{KM7:TR?= NF\CPGk2KGR? M{DWdYlvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To M1TjXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
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NUGC4 MmXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:zN{DPxE1? NYTKVGRPPSCm MVnpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
ZR-75-30 M2PpVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\3O5NvOzNizszN NVrZU3B[PSCm MWHpcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi= MkTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ|OUG4O|k4RC:jPh?=
Rat1 NUn5PVhIWDFzMHHsdIhiKGmwaHnibZRqd25iYYPzZZk> NV3Yb5JWUUN3MDC9JFAvODd2IN88US=> M4XwZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MU[0NVg6Lz5{NkG2OFE5QTxxYU6=
Rat1 MUHQTVNM[WyyaHGgbY5pcWKrdHnvckBie3OjeR?= M{X4RWlEPTBiPTCwMlA4PCEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1 NXexVGRjWDFzMHHsdIhiKGmwaHnibZRqd25iYYPzZZk> MmDkTWM2OCB;IECuNFc1KM7:TR?= MnryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mk[wN|QoRjJ|N{K2NFM1RC:jPh?=
Rat1 M2f4WXAyOTCmZXz0ZUBqdmirYnn0bY9vKGG|c3H5 MmOxTWM2OCB;IEGuNkDPxE1? MkPTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzNkSxPFkoRjJ4MU[0NVg6RC:jPh?=
Rat1 MUXQTVNM\2GvbXGgbY5pcWKrdHnvckBie3OjeR?= MXzJR|UxKD1iMT6yJO69VQ>? MmTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{ME[1NFQoRjJ4MkC2OVA1RC:jPh?=
Rat1 NF;tc4FROTFyZHXseIEhcW6qaXLpeIlwdiCjc4PhfS=> MojUTWM2OCB;IEGuNkDPxE1? M{LzPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{K2NFM1Lz5{M{eyOlA{PDxxYU6=
Rat1 NXfMNoVyWDFzMHLleIEhcW6qaXLpeIlwdiCjc4PhfS=> M3X1emlEPTBiPTCyMlIh|ryP NUn3fJRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOlQyQDlpPkK2NVY1OTh7PD;hQi=>
Rat1 NGPleItRUTONYnX0ZUBqdmirYnn0bY9vKGG|c3H5 NYnx[4dpUUN3MDC9JFIvOiEQvF2= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1 M{HTe3AyOTCjbIDoZUBqdmirYnn0bY9vKGG|c3H5 NGDIUVVKSzVyIE2gNk4zKM7:TR?= MluzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mk[wN|QoRjJ|N{K2NFM1RC:jPh?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-AKT(S473) / p-AKT(T308); 

PubMed: 25544637     


PIK3CA hot-spot mutant cell lines were treated with 1 µM BYL719 for the indicated period of time. Lysates were immunoblotted to detect the indicated proteins.

p100β / p110α / p85 / p-ERBB3(Y1289); 

PubMed: 25544637     


BT474 cells were treated with 1 µM BYL719 alone for different durations of time and lysates were immunoprecipitated with ERBB3 antibody. Precipitates were analyzed by western blot with the indicated antibodies.

p-HER2 / IGF-1R; 

PubMed: 25544637     


Cells were treated with 1 μM BYL719 for 24 hr and lysates were immunoblotted to detect the indicated proteins.

pS6 (Ser235-236); 

PubMed: 27048245     


Immunoblots of lysates from parental and resistant cells treated for 24 hours as indicated.

PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD; 

PubMed: 27604488     


T47D cells cultured to resistance in the presence of BYL719. Both parental (T47D) and resistant (T47DR) cells were treated with BYL719 at 1μM, and cell lysates were prepared at 0, 4, 24 hours for immunoblotting for the indicated proteins.

25544637 27048245 27604488
Growth inhibition assay
Cell viability; 

PubMed: 27602501     


The effect of BYL719 on cellular viability was evaluated in HCT116 (A) and SW480 (B) CRC cells. Briefly, cells were grown, treated with increasing concentrations of BYL719 (5, 10 and 20 μM) and cellular viability determined by MTS assay 72h after treatments. Controls included cells that remained untreated (media ctrl) and vehicle-treated controls (DMSO). Data represent means ± SEM of at least triplicate experiments normalized to controls. All conditions were compared with DMSO. Ctrl, control; DMSO, dimethyl sulfoxide. **, p< 0.01; ***, p< 0.001; ****, p< 0.0001.

27602501
Immunofluorescence
LC3; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 5 days with DMSO, 500 nM BKM120 or 500 nM BYL719. Cells were treated with DMSO or 1 μM Lapatinib for the final 18 h. GFP-LC3 localization was captured by fluorescent microscopy.

26637440
体内研究 BYL719(>270 mg/d)在PIK3CA突变体异种移植啮齿动物模型中表现出统计学显著的剂量依赖性抗肿瘤效能。BYL719具有低清除率，半衰期为8.5小时，并且它的作用在30mg/d 和450mg/d之间剂量成比例的增加，在人的Cmax 和AUC中显示出低的个体差异。BYL719(270mg/d)首次表现出临床疗效的迹象，包括在ER+乳腺癌患者中证实的部分响应，以及17个患者中8个实现了显著的PET响应(PMR)和/或肿瘤治愈。[1]

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)

溶解度 (25°C)

体外 DMSO 88 mg/mL (199.33 mM)
Ethanol 2 mg/mL (4.53 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+40%PEG300+5%Tween80+50%ddH2O
 4.4 mg/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 441.47
化学式

C19H22F3N5O2S
CAS号 1217486-61-7
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

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、SDS / 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、SDS / 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
NCT04997902 Not yet recruiting Drug: Tipifarnib|Drug: Alpelisib HNSCC Kura Oncology Inc. October 2021 Phase 1|Phase 2
NCT05022342 Not yet recruiting Other: alpelisib plus fulvestrant Breast Cancer Novartis Pharmaceuticals|Novartis September 15 2021 --
NCT04980833 Not yet recruiting Drug: Alpelisib PIK3CA-related Overgrowth Spectrum (PROS) Novartis Pharmaceuticals|Novartis September 30 2021 Phase 2
NCT04589650 Recruiting Drug: Alpelisib|Drug: Placebo PIK3CA-related Overgrowth Spectrum (PROS) Novartis Pharmaceuticals|Novartis April 19 2021 Phase 2
NCT04762979 Recruiting Drug: Alpelisib|Drug: Fulvestrant|Drug: Aromatase inhibitor Hormone Receptor Positive Breast Carcinoma|HER2-negative Breast Cancer|PIK3CA Mutant Metastatic Breast Cancer Amanda Parkes|Novartis|University of Wisconsin Madison|Big Ten Cancer Research Consortium February 12 2021 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。

  • * 必填项
Selleck产品目录册

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

  • 泛PI3K抑制剂

    LY294002 : Pan-PI3Kα/δ/β inhibitor, IC50=0.5 μM/0.57 μM/0.97 μM.

  • 活性最高的PI3K抑制剂

    BEZ235 (NVP-BEZ235, Dactolisib) : p110α/γ/δ/β, IC50=4 nM/5 nM/7 nM/75 nM.

  • FDA批准的PI3K抑制剂

    CAL-101 (Idelalisib, GS-1101) : Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.

  • 最新的PI3K抑制剂

    VS-5584 (SB2343) New : Potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

相关PI3K产品

  • Taselisib (GDC 0032) New

    Taselisib (GDC 0032, RG7604) 是一种有效，下一代的β亚型PI3K抑制剂，作用于PI3Kα/δ/γ， IC50分别为0.29 nM/0.12 nM/0.97nM，比作用于PI3Kβ选择性高10倍以上。

  • Pilaralisib (XL147) New

    Pilaralisib (XL147)是一种选择性的可逆I型PI3K抑制剂，作用于PI3Kα/δ/γ，在无细胞试验中IC50为 39 nM/36 nM/23 nM，对PI3Kβ作用较低。Phase 1/2。

  • LY294002

    LY294002 (SF 1101, NSC 697286) 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。

    Features:LY294002是选择性的, 可渗透细胞的特定PI3K抑制剂，可作用于酶的ATP结合位点，且抑制自体吞噬的螯合作用。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA, NSC 66389) 是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。3-Methyladenine (3-MA)可成功应用于抑制线粒体自噬。现配现用（加热助溶）。

  • Idelalisib (CAL-101, GS-1101)

    Idelalisib (CAL-101, GS-1101) 是选择性p110δ抑制剂，在无细胞试验中IC50为 2.5 nM；对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍，对p110δ的选择性是对 C2β，hVPS34，DNA-PK 和 mTOR的400到4000倍。Idelalisib 还可诱导自噬。

    Features:Calistoga 暗示 CAL-101治疗血液恶性肿瘤可能有更广泛的应用价值。

  • Wortmannin (KY 12420)

    Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609)是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。

  • Dactolisib (BEZ235)

    Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。

  • Buparlisib (BKM120)

    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/γ的IC50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。Buparlisib 可诱导凋亡。Phase 2。

    Features:BKM120是可用于口服的生物有效的PI3K抑制剂。

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941, RG7321) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Pictilisib (GDC-0941) 可诱导自噬和凋亡。Phase 2。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID