Alpelisib (BYL719)

For research use only.

Catalog No.S2814

70 publications

Alpelisib (BYL719) Chemical Structure

Molecular Weight(MW): 441.47

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 70 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 NYHOdlRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT2[GF1OC5zLUGwNEDPxE1? NWfWfXA6PzJiaB?= MY\JR|UxRTFwMUCg{txO MUSyOVU2ODV2OR?=
SNU-1076 M4TMN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULHcXRpOC5zLUGwNEDPxE1? Mk\pO|IhcA>? NUjPZYFwUUN3ME22MlgzKM7:TR?= NIrQd|MzPTV3MEW0PS=>
SNU-1066 NUXjSW9OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOwMlEuOTByIN88US=> NYq2blRDPzJiaB?= MWrJR|UxRTFwMUOg{txO NVvhW|QyOjV3NUC1OFk>
FaDu MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PJNFAvOS1zMECg{txO MWi3NkBp MYXJR|UxRTF7Lk[2JO69VQ>? NWHTPGViOjV3NUC1OFk>
SNU1041 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW2NE4yNTFyMDFOwG0> NFe3eHA4OiCq NEfFfmJKSzVyPUKwMlY2KM7:TR?= MUmyOVU2ODV2OR?=
SCC25 NGr4PIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjsVGoxNjFvMUCwJO69VQ>? MlPXO|IhcA>? Ml3rTWM2OD12OT6zNEDPxE1? NU\kdmxkOjV3NUC1OFk>
BON-1 NHfVVY1HfW6ldHnvckBCe3OjeR?= NFzDPIYyNzFyIN88US=> MVS0JIg> M2\GOIlvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| MYSyOVAzPjJ7Mh?=
QGP-1 MonESpVv[3Srb36gRZN{[Xl? NV3XUJJPOS9zMDFOwG0> MV20JIg> NYjGeVFFcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= MoDENlUxOjZ{OUK=
MG-63 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTZizszN89yNKEmFOUC9NlQh|ryP MkDnNlQ6PjF5OUC=
HOS MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLCTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= NYKxUlhXOjR7NkG3PVA>
MOS-J M2rCVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zXWWlEPTB;MUCg{txO97zOIFnDPVA:OzZizszN MlrmNlQ6PjF5OUC=
POS-1 M3faeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRThizszN89yNKEmFOUC9N|Yh|ryP M4nITVI1QTZzN{mw
92.1 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LGVFUxOC1{MECwJI5O MV[1JIQ> MVTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MWiyOFU3OzV2MB?=
Mel270 M{LWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;PToM2ODBvMkCwNEBvVQ>? MV:1JIQ> NXS5S2d{cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NVnkOWFFOjR3NkO1OFA>
Omm1.3 MmDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjD[og2ODBvMkCwNEBvVQ>? NGfmOJI2KGR? NUD1O2ZzcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NFXzTY0zPDV4M{W0NC=>
Omm1 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzjOVAxNTJyMECgcm0> MmDKOUBl M4\RWYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NGrINpUzPDV4M{W0NC=>
C918 NUD2WXdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnf5OVAxNTJyMECgcm0> MlHVOUBl NV7XTGRFcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M2\VWlI1PTZ|NUSw
Mel290 MlzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;IOVAxNTJyMECgcm0> Mn\1OUBl NHnYNJZqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MnG0NlQ2PjN3NEC=
OPM2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPKNE42NTJwNTFOwG0> M{npO|Q5KGh? MlTEbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2\pflI1PDB3MUKx
OPM1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL6VVA1OC53LUKuOUDPxE1? NImwZpY1QCCq MkLhbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEXST3kzPDRyNUGyNS=>
U266 NVTzbGxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPCN5VYOC53LUKuOUDPxE1? MoLCOFghcA>? NInkfGhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF;FTmczPDRyNUGyNS=>
MM1R NEDPWW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[wMlUuOi53IN88US=> MkfQOFghcA>? M2jEeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYqyOFQxPTF{MR?=
MM1S MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfnV|cxNjVvMj61JO69VQ>? MonQOFghcA>? MnXObY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2\5d|I1PDB3MUKx
H929 NWXnOXB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTuZ4o4OC53LUKuOUDPxE1? MUS0PEBp NWi1bHZ2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Ml72NlQ1ODVzMkG=
RPMI NYHsfoNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPnPXAxNjVvMj61JO69VQ>? MVW0PEBp NELCS29qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1LsWFI1PDB3MUKx
SKBR3 NYKy[VNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLUNZQ{OyEQvF2= MV61JIQ> NILkXVJqdmirYnn0d{A{Pe,:hTDj[YxtKGe{b4f0bC=> MUmyN|kyQDd7Nx?=
MDA453 M3v1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLIN|Mh|ryP NF\ySG02KGR? NWP0eJRqcW6qaXLpeJMhOzkxvJWgZ4VtdCCpcn;3eIg> MXWyN|kyQDd7Nx?=
EFM192A M3fWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXWyNHcyOzNizszN NF[weG82KGR? NWDDR|RxcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> NILveHMzOzlzOEe5Oy=>
AU565 NXvHW3Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPQeJM{OyEQvF2= NUe2Wmp7PSCm M1HUSolvcGmkaYTzJFI397zHIHPlcIwh\3Kxd4To MYKyN|kyQDd7Nx?=
MDA361 NG\wdZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXnN|Mh|ryP MWO1JIQ> NHXIendqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> MlvONlM6OTh5OUe=
BT474 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSzN{DPxE1? MoTLOUBl MlTSbY5pcWKrdIOgNVbwxIViY3XscEBoem:5dHi= NWrOOFhWOjN7MUi3PVc>
HCC202 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TUOFM{KM7:TR?= M3TTfVUh\A>? NYfJUZljcW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> M1XNR|I{QTF6N{m3
KPL4 MkHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjrN|Mh|ryP NHjQOpc2KGR? M3z6fIlvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To NILINokzOzlzOEe5Oy=>
NCL-N87 MlXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKzN{DPxE1? MnjkOUBl M3npPIlvcGmkaYTzJFMy97zHIHPlcIwh\3Kxd4To NH7XeFczOzlzOEe5Oy=>
UACC812 M3z1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnYN|Mh|ryP MY[1JIQ> NY\uTHp1cW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> M4f6ZlI{QTF6N{m3
HCC2218 NHTRVm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH2N|Mh|ryP MX21JIQ> NWTn[ZdScW6qaXLpeJMhOTYxvJWgZ4VtdCCpcn;3eIg> NFz2XIYzOzlzOEe5Oy=>
HCC1569 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWzN{DPxE1? MWi1JIQ> NVzpR|VxcW6qaXLpeJMhPe,:hTDj[YxtKGe{b4f0bC=> MV[yN|kyQDd7Nx?=
OE19 MnLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnJdIVnOzNizszN NXi0WI52PSCm NW\Dc2I5cW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> NUfMS3gyOjN7MUi3PVc>
OE33 M33NXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPr[5E{OyEQvF2= NXeyRY1DPSCm NXy3V45TcW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> MmTlNlM6OTh5OUe=
JIMT1 NHHZSGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LHRlM{KM7:TR?= NV3lO2l5PSCm MUfpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq M3j2[|I{QTF6N{m3
HCC1954 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXKzN{DPxE1? NGnYdXI2KGR? MlfRbY5pcWKrdIOgNlnwxIViY3XscEBoem:5dHi= M32xPFI{QTF6N{m3
NUGC4 M3jDe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HwelM{KM7:TR?= MnPoOUBl MWXpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= MYiyN|kyQDd7Nx?=
ZR-75-30 MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWzN{DPxE1? M4TPO|Uh\A>? NXriNY55cW6qaXLpeJMhNTF378{FJINmdGxiZ4Lve5Rp NIi5OnUzOzlzOEe5Oy=>

... 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):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 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(N)=O)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
NCT04300790 Not yet recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis June 30 2020 Phase 2
NCT04251533 Not yet recruiting Drug: alpelisib|Drug: placebo|Drug: nab-paclitaxel Triple Negative Breast Neoplasms Novartis Pharmaceuticals|Novartis April 22 2020 Phase 3
NCT03207529 Recruiting Drug: Alpelisib|Drug: Enzalutamide Advanced Breast Carcinoma|Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Androgen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|PTEN Positive|Recurrent Breast Carcinoma|Refractory Breast Carcinoma|Triple-Negative Breast Carcinoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) June 7 2019 Phase 1
NCT02620839 Terminated Drug: Alpelisib|Drug: Cisplatin Solid Tumors Pamela Munster|University of California San Francisco December 1 2016 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID