Alpelisib (BYL719)

For research use only.

Catalog No.S2814

127 publications

Alpelisib (BYL719) Chemical Structure

CAS No. 1217486-61-7

Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

Selleck's Alpelisib (BYL719) has been cited by 127 publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.
Targets
PI3Kα [1]
(Cell-free assay)
5 nM
In vitro

BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Detroit562 Ml20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuwMlEuOTByIN88US=> NETPRmE4OiCq NHvjRXdKSzVyPUGuNVAh|ryP NYGzdmNmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVA2PDlpPkK1OVUxPTR7PD;hQi=>
SNU-1076 NXL6NJQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Ll[lAvOS1zMECg{txO Mnf2O|IhcA>? MkHPTWM2OD14LkiyJO69VQ>? NWjEWnh{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVA2PDlpPkK1OVUxPTR7PD;hQi=>
SNU-1066 NF\HVnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTMNE4yNTFyMDFOwG0> MYm3NkBp MVjJR|UxRTFwMUOg{txO MljUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
FaDu NUPNdVFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSwMlEuOTByIN88US=> M2n6TVczKGh? NX:5U4NqUUN3ME2xPU43PiEQvF2= NFPkSVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW1NFU1QSd-MkW1OVA2PDl:L3G+
SNU1041 NVXDcGxJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInlc3ExNjFvMUCwJO69VQ>? MWC3NkBp MkH4TWM2OD1{MD62OUDPxE1? NVO2TZJTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVA2PDlpPkK1OVUxPTR7PD;hQi=>
SCC25 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV75[FRxOC5zLUGwNEDPxE1? MnjNO|IhcA>? M{TVbWlEPTB;NEmuN|Ah|ryP M3XEW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWwOVQ6Lz5{NUW1NFU1QTxxYU6=
BON-1 NVr6SGZyTnWwY4Tpc44hSXO|YYm= MXSxM|ExKM7:TR?= NF\T[Gg1KGh? NUPhPGFjcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= M4fJd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK2NlkzLz5{NUCyOlI6OjxxYU6=
QGP-1 MmXiSpVv[3Srb36gRZN{[Xl? NIjXOJkyNzFyIN88US=> M{jqdVQhcA>? NWPJPGlXcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= NVjPSIVvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlYzQTJpPkK1NFI3Ojl{PD;hQi=>
MG-63 NUnWeG1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PlW2lEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= NFPxPXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NVc6OCd-MkS5OlE4QTB:L3G+
HOS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLQTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= M4jjXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OU[xO|kxLz5{NEm2NVc6ODxxYU6=
MOS-J NUDnPXB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7hTWM2OD1zMDFOwG3wxIxiSVO5NF0{PiEQvF2= M4LyflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OU[xO|kxLz5{NEm2NVc6ODxxYU6=
POS-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnmPWU2UUN3ME24JO69Ve,:jDDJR|kxRTN4IN88US=> Mke1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkG3PVAoRjJ2OU[xO|kxRC:jPh?=
92.1 MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrPSnA2ODBvMkCwNEBvVQ>? NVHOZplTPSCm M3r5RolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NWnRZXJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OlM2PDBpPkK0OVY{PTRyPD;hQi=>
Mel270 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vlbVUxOC1{MECwJI5O MXe1JIQ> NWe4O3UxcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M1;yd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NU[zOVQxLz5{NEW2N|U1ODxxYU6=
Omm1.3 MkD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XGelUxOC1{MECwJI5O MoPPOUBl MlHNbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4M{W0NEc,OjR3NkO1OFA9N2F-
Omm1 M1LiOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:zOVAxNTJyMECgcm0> M3Poe|Uh\A>? M1;pXYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4M{W0NEc,OjR3NkO1OFA9N2F-
C918 NX3xN4txT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK1NFAuOjByMDDuUS=> NVrJfVhNPSCm M2rHUolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M3jIdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NU[zOVQxLz5{NEW2N|U1ODxxYU6=
Mel290 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvNRpN[PTByLUKwNFAhdk1? MWS1JIQ> NUnyUWxCcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? Mm[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NkO1OFAoRjJ2NU[zOVQxRC:jPh?=
OPM2 NV3OTnB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XRO|AvPS1{LkWg{txO M4eyNVQ5KGh? M3;YTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NW\leVJCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFUyOjFpPkK0OFA2OTJzPD;hQi=>
OPM1 NWrl[41QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W2XVAvPS1{LkWg{txO NXPaU4FMPDhiaB?= NH7aOItqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUGyNUc,OjR2MEWxNlE9N2F-
U266 NVjpT4dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjqepFGOC53LUKuOUDPxE1? Moe4OFghcA>? NVXkPGlqcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYP5PXRsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFUyOjFpPkK0OFA2OTJzPD;hQi=>
MM1R NEPmO3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPUXoI5OC53LUKuOUDPxE1? MnLwOFghcA>? NVPPO5FpcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUGyNUc,OjR2MEWxNlE9N2F-
MM1S NIflWW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGwMlUuOi53IN88US=> NXTo[WZ2PDhiaB?= MkjvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2LH[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1NVIyLz5{NESwOVEzOTxxYU6=
H929 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXicYkxOC53LUKuOUDPxE1? MX[0PEBp M{jwOYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MEWxNlEoRjJ2NEC1NVIyRC:jPh?=
RPMI Ml;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuwMlUuOi53IN88US=> M4nHeVQ5KGh? NUe1SIZpcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIPUOlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESwOVEzOSd-MkS0NFUyOjF:L3G+
SKBR3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\aZXhLOzNizszN NWDmPI56PSCm M1\wTolvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To M3nWUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
MDA453 NWDrTVNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWKzN{DPxE1? MVO1JIQ> NGmxV4NqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> NX3vb5Y2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
EFM192A MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWraNXVtOzNizszN MmPjOUBl NXL6RYUycW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> NXzzUHNlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
AU565 NGDYeHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rZflM{KM7:TR?= MnH6OUBl NFnoeYtqdmirYnn0d{AzPu,:hTDj[YxtKGe{b4f0bC=> M{mzZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
MDA361 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fUdlM{KM7:TR?= MkLkOUBl NVvTZZFucW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> Mmm3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ|OUG4O|k4RC:jPh?=
BT474 MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T6ZVM{KM7:TR?= M1zCW|Uh\A>? NGnVTmlqdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
HCC202 M3viT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWezN{DPxE1? NVf1c4JLPSCm MV7pcohq[mm2czCyNQ+9jSClZXzsJIdzd3e2aB?= MlSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ|OUG4O|k4RC:jPh?=
KPL4 NGixUVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXy0dJh6OzNizszN NWrOdI9WPSCm MV;pcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= NYLaOGV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
NCL-N87 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXizN{DPxE1? NUPDRYdzPSCm M4\DV4lvcGmkaYTzJFMy97zHIHPlcIwh\3Kxd4To NUfBVXB3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
UACC812 M37jPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOzN{DPxE1? NXjBZ4czPSCm M4rlSYlvcGmkaYTzJFI497zHIHPlcIwh\3Kxd4To MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
HCC2218 M3f6TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfON|Mh|ryP NIHOZZA2KGR? NGHJVG5qdmirYnn0d{AyPe,:hTDj[YxtKGe{b4f0bC=> M1HnSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
HCC1569 M4nzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmzN{DPxE1? MmLWOUBl M1fSbolvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= NWrZ[2FtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
OE19 M2jicmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7LfFVGOzNizszN M4raUFUh\A>? NUPueI9ucW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> M17teVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
OE33 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISzR3Y{OyEQvF2= MUi1JIQ> M4\0Z4lvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To M363WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
JIMT1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;2fVM{OyEQvF2= MYq1JIQ> M4DDUYlvcGmkaYTzJFnwxIViY3XscEBoem:5dHi= NF7EVlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mxPFc6Pyd-MkO5NVg4QTd:L3G+
HCC1954 Mk\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv3d5E4OzNizszN Mn;UOUBl MYrpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= NYPXeYJxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
NUGC4 MoTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfSV4g{OyEQvF2= Ml;wOUBl MmHXbY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= M36zUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUG4O|k4Lz5{M{mxPFc6PzxxYU6=
ZR-75-30 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnYV4c{OyEQvF2= MXK1JIQ> NYiydGlTcW6qaXLpeJMhNTF378{FJINmdGxiZ4Lve5Rp NVnrOZk6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
Rat1 MYfQNVEx[WyyaHGgbY5pcWKrdHnvckBie3OjeR?= NWGybFh2UUN3MDC9JFAvODd2IN88US=> NX\PWmZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOlQyQDlpPkK2NVY1OTh7PD;hQi=>
Rat1 NF6xNnVRUTONYXzwbIEhcW6qaXLpeIlwdiCjc4PhfS=> NYfYfYg6UUN3MDC9JFAvODd2IN88US=> NVnt[5dGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNFY2ODRpPkK2NlA3PTB2PD;hQi=>
Rat1 MVXQNVEx[WyyaHGgbY5pcWKrdHnvckBie3OjeR?= MX7JR|UxKD1iMD6wO|Qh|ryP NGXzRXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyOlA{PCd-MkO3NlYxOzR:L3G+
Rat1 M{LLdnAyOTCmZXz0ZUBqdmirYnn0bY9vKGG|c3H5 MXzJR|UxKD1iMT6yJO69VQ>? NVXtWFE1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOlQyQDlpPkK2NVY1OTh7PD;hQi=>
Rat1 MXjQTVNM\2GvbXGgbY5pcWKrdHnvckBie3OjeR?= NX:4NJVxUUN3MDC9JFEvOiEQvF2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1 MWDQNVEx\GWudHGgbY5pcWKrdHnvckBie3OjeR?= NXX0W3l6UUN3MDC9JFEvOiEQvF2= NXG3Z3BFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NlYxOzRpPkKzO|I3ODN2PD;hQi=>
Rat1 MYnQNVEx[mW2YTDpcohq[mm2aX;uJIF{e2G7 M4XMfWlEPTBiPTCyMlIh|ryP NFLUZ|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG2OFE5QSd-Mk[xOlQyQDl:L3G+
Rat1 MUDQTVNM[mW2YTDpcohq[mm2aX;uJIF{e2G7 MV3JR|UxKD1iMj6yJO69VQ>? M37BPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkC2OVA1Lz5{NkKwOlUxPDxxYU6=
Rat1 MnrEVFEyOGGucHjhJIlvcGmkaYTpc44h[XO|YYm= M4C2XWlEPTBiPTCyMlIh|ryP NEjFdG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyOlA{PCd-MkO3NlYxOzR:L3G+

... 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
In vivo BYL719(>270 mg/d) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC in human. BYL719(270mg/d) shows first signs of clinical efficacy include 1 confirmed partial response in a patient with ER+ breast cancer, and significant PET responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17 evaluated patients. [1]

Protocol

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.33 mM)
Ethanol 2 mg/mL (4.53 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
4.4 mg/mL

* 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.

Chemical Information

Molecular Weight 441.47
Formula

C19H22F3N5O2S

CAS No. 1217486-61-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

Tags: buy Alpelisib (BYL719) | Alpelisib (BYL719) supplier | purchase Alpelisib (BYL719) | Alpelisib (BYL719) cost | Alpelisib (BYL719) manufacturer | order Alpelisib (BYL719) | Alpelisib (BYL719) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID