Alpelisib (BYL719)

For research use only.

Catalog No.S2814

101 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.

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Selleck's Alpelisib (BYL719) has been cited by 101 publications

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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 Mn3NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMlEuOTByIN88US=> M1PNVVczKGh? M4XKV2lEPTB;MT6xNEDPxE1? NViwSYcxOjV3NUC1OFk>
SNU-1076 M1zwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDUbpIxNjFvMUCwJO69VQ>? MYi3NkBp MVfJR|UxRTZwOEKg{txO NF7zNZUzPTV3MEW0PS=>
SNU-1066 NX7mc4pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYT5UZhROC5zLUGwNEDPxE1? NWniUVJiPzJiaB?= MXPJR|UxRTFwMUOg{txO NH\kW4MzPTV3MEW0PS=>
FaDu M1y1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\tNE4yNTFyMDFOwG0> M{jtTVczKGh? M1;3N2lEPTB;MUmuOlYh|ryP MXqyOVU2ODV2OR?=
SNU1041 M{nSNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTwNE4yNTFyMDFOwG0> NEfENlY4OiCq Ml31TWM2OD1{MD62OUDPxE1? NXrRXmluOjV3NUC1OFk>
SCC25 MnLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVSwMlEuOTByIN88US=> MXi3NkBp MlrnTWM2OD12OT6zNEDPxE1? NEf4bnczPTV3MEW0PS=>
BON-1 NG[wWpNHfW6ldHnvckBCe3OjeR?= MVexM|ExKM7:TR?= MYO0JIg> Ml;NbY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? M3vQdlI2ODJ4Mkmy
QGP-1 NVHOV5UzTnWwY4Tpc44hSXO|YYm= NWT5OIwxOS9zMDFOwG0> M2PkVVQhcA>? NHHqR5pqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NGfTR5AzPTB{NkK5Ni=>
MG-63 NFPWSXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYj1dodwUUN3ME22JO69Ve,:jDDJR|kxRTJ2IN88US=> MnnYNlQ6PjF5OUC=
HOS MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF3IN88Ug+9lCCLQ{mwQVQzKM7:TR?= NFfBSJEzPDl4MUe5NC=>
MOS-J NH;1R5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= MnPMNlQ6PjF5OUC=
POS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\aSpBNUUN3ME24JO69Ve,:jDDJR|kxRTN4IN88US=> NWLxPXhEOjR7NkG3PVA>
92.1 Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO1NFAuOjByMDDuUS=> M1;T[|Uh\A>? MmC2bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NYfYVJZIOjR3NkO1OFA>
Mel270 NUnCZYNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nJb|UxOC1{MECwJI5O NH\zOWI2KGR? NHPRNVdqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NFfJS3czPDV4M{W0NC=>
Omm1.3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHmwVmc2ODBvMkCwNEBvVQ>? M{TqNFUh\A>? M{jMN4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NVXhTW5NOjR3NkO1OFA>
Omm1 MkDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TVeFUxOC1{MECwJI5O Mn35OUBl MX3pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MmmzNlQ2PjN3NEC=
C918 Mn[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWW1NFAuOjByMDDuUS=> M3fI[FUh\A>? NGnEVG9qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NFnnUYszPDV4M{W0NC=>
Mel290 M4SzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC1NFAuOjByMDDuUS=> MYK1JIQ> NYeyXIlncW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NULhNG5KOjR3NkO1OFA>
OPM2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PVbVAvPS1{LkWg{txO M2TKe|Q5KGh? M3\IT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWS1b2d6OjR2MEWxNlE>
OPM1 NVTiR|hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\mRXMxNjVvMj61JO69VQ>? NHfM[JI1QCCq NYDiXWh1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1XzPFI1PDB3MUKx
U266 NF3ySG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFv6UHUxNjVvMj61JO69VQ>? MoDMOFghcA>? NE\RRmhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWfCbnh6OjR2MEWxNlE>
MM1R MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInqWWwxNjVvMj61JO69VQ>? NE\JTYE1QCCq M33lWolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYP3TnhYOjR2MEWxNlE>
MM1S NGjYe3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[wMlUuOi53IN88US=> Mme1OFghcA>? M4LkVIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVLGNplbOjR2MEWxNlE>
H929 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2wMlUuOi53IN88US=> NVzxfXF3PDhiaB?= NHTsVoNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIO3e48zPDRyNUGyNS=>
RPMI NFX4eoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUiwMlUuOi53IN88US=> NXPKZppJPDhiaB?= MV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGG1WZczPDRyNUGyNS=>
SKBR3 M1XjNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWzN{DPxE1? Ml\pOUBl MUTpcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= MXKyN|kyQDd7Nx?=
MDA453 MlT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHvN40{OyEQvF2= NVLFe2xzPSCm NFThRndqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> NV\Re4YxOjN7MUi3PVc>
EFM192A NHvwd45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XsT|M{KM7:TR?= NILsVWE2KGR? MmjibY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= NH\6[YgzOzlzOEe5Oy=>
AU565 NGTqOplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1OwT|M{KM7:TR?= MlTCOUBl NVSxOphPcW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg> NVj1NlVEOjN7MUi3PVc>
MDA361 M2HFT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvsOotpOzNizszN NGj6c2s2KGR? NXXwRnN{cW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> M{TRNlI{QTF6N{m3
BT474 M2rwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPheVQ{OyEQvF2= NE\tSXQ2KGR? NIrzdGtqdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> NH6wTVIzOzlzOEe5Oy=>
HCC202 M{izc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G4U|M{KM7:TR?= MXe1JIQ> MXvpcohq[mm2czCyNQ+9jSClZXzsJIdzd3e2aB?= M3HTVFI{QTF6N{m3
KPL4 M4r4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzxN|Mh|ryP NW\T[mRUPSCm NWn2XWJWcW6qaXLpeJMhPTkxvJWgZ4VtdCCpcn;3eIg> NYL0c2NmOjN7MUi3PVc>
NCL-N87 M1nkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO3bGw{OyEQvF2= Mk\EOUBl NXyyOHYzcW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> M4T3R|I{QTF6N{m3
UACC812 MnHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqzN{DPxE1? M4ribFUh\A>? M4X1[olvcGmkaYTzJFI497zHIHPlcIwh\3Kxd4To NFT2OGczOzlzOEe5Oy=>
HCC2218 M{jWU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XzflM{KM7:TR?= MlvnOUBl NGDlRmNqdmirYnn0d{AyPe,:hTDj[YxtKGe{b4f0bC=> NVvVPYhJOjN7MUi3PVc>
HCC1569 MmjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuzN{DPxE1? NHjR[pA2KGR? NHTNcpRqdmirYnn0d{A297zHIHPlcIwh\3Kxd4To NYHwZmUzOjN7MUi3PVc>
OE19 M1WwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLmPHduOzNizszN NFK0NJo2KGR? MmHLbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= Mn\UNlM6OTh5OUe=
OE33 NYrrfZFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\x[|c{OyEQvF2= NXryT2dWPSCm MVrpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= Ml3QNlM6OTh5OUe=
JIMT1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHac4xHOzNizszN M2T4b|Uh\A>? NEnrWWpqdmirYnn0d{A697zHIHPlcIwh\3Kxd4To NU[4bpN7OjN7MUi3PVc>
HCC1954 Mm\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKzN{DPxE1? MnXPOUBl MWTpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= M{nUUlI{QTF6N{m3
NUGC4 M3LOeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUKzR3BNOzNizszN NH7uRok2KGR? MWnpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= NGniOJkzOzlzOEe5Oy=>
ZR-75-30 NX;IPIM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7Jco9IOzNizszN NIn0N5M2KGR? MkfRbY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To MXWyN|kyQDd7Nx?=

... 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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04524000 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis October 1 2020 Phase 2
NCT04526470 Not yet recruiting Drug: Alpelisib + Paclitaxel Solid Tumor|Stomach Cancer Seoul National University Bundang Hospital September 1 2020 Phase 1|Phase 2
NCT04300790 Not yet recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis June 30 2020 Phase 2
NCT04251533 Recruiting Drug: alpelisib|Drug: placebo|Drug: nab-paclitaxel Triple Negative Breast Neoplasms Novartis Pharmaceuticals|Novartis June 8 2020 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID