Alpelisib (BYL719)

For research use only. Not for use in humans.

Catalog No.S2814

54 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 54 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 M3rlRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW0NE4yNTFyMDFOwG0> NGftTI44OiCq MkfrTWM2OD1zLkGwJO69VQ>? M3;BcVI2PTVyNUS5
SNU-1076 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXCNE4yNTFyMDFOwG0> MXy3NkBp Mm\uTWM2OD14LkiyJO69VQ>? M2HyRVI2PTVyNUS5
SNU-1066 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMlEuOTByIN88US=> NUDXbYVUPzJiaB?= NHnnV2dKSzVyPUGuNVMh|ryP M4HWb|I2PTVyNUS5
FaDu M2PqUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\p[lIxNjFvMUCwJO69VQ>? NUXYe|VEPzJiaB?= M2nZUWlEPTB;MUmuOlYh|ryP MXeyOVU2ODV2OR?=
SNU1041 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LBelAvOS1zMECg{txO MX[3NkBp M{DFWmlEPTB;MkCuOlUh|ryP M1PXN|I2PTVyNUS5
SCC25 NYTIeGVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX6zfGVnOC5zLUGwNEDPxE1? Mn;LO|IhcA>? MlrRTWM2OD12OT6zNEDPxE1? NUmz[JFxOjV3NUC1OFk>
BON-1 MVTGeY5kfGmxbjDBd5NigQ>? NVT5UIF5OS9zMDFOwG0> M3PpN|QhcA>? MUnpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? NXjDcm1rOjVyMk[yPVI>
QGP-1 MlvrSpVv[3Srb36gRZN{[Xl? NGn0cmQyNzFyIN88US=> MkHvOEBp M1KxSYlvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| MWiyOVAzPjJ7Mh?=
MG-63 M{nVemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjWTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= M320Z|I1QTZzN{mw
HOS MkPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLrTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= NVnqUHVtOjR7NkG3PVA>
MOS-J NUnkTHlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXBTWM2OD1zMDFOwG3wxIxiSVO5NF0{PiEQvF2= MWGyOFk3OTd7MB?=
POS-1 NXfGcZpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRThizszN89yNKEmFOUC9N|Yh|ryP M2W1d|I1QTZzN{mw
92.1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Hzb|UxOC1{MECwJI5O NXr3T|hNPSCm M4PxTIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MnnzNlQ2PjN3NEC=
Mel270 NY\Bd5JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlO4OVAxNTJyMECgcm0> NF3lWGo2KGR? Mn;4bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NX;oeYtDOjR3NkO1OFA>
Omm1.3 M1j5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrwR45OPTByLUKwNFAhdk1? NWLqbJFmPSCm NFOz[|JqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M4TK[VI1PTZ|NUSw
Omm1 M4LObmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknDOVAxNTJyMECgcm0> M2fobVUh\A>? MXHpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MW[yOFU3OzV2MB?=
C918 Mm\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm1NFAuOjByMDDuUS=> MWq1JIQ> NE\XSY1qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MljzNlQ2PjN3NEC=
Mel290 NILacFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEKwdpQ2ODBvMkCwNEBvVQ>? NET1Tmk2KGR? M2TkSIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M3vINFI1PTZ|NUSw
OPM2 M4HiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnWUHYxNjVvMj61JO69VQ>? Ml\0OFghcA>? NE\TPXFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M17SeVI1PDB3MUKx
OPM1 MnTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mni2NE42NTJwNTFOwG0> NXTWbGVIPDhiaB?= MUTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHHPOXYzPDRyNUGyNS=>
U266 MkTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXm[4xZOC53LUKuOUDPxE1? Mn[5OFghcA>? NEi0dmFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MViyOFQxPTF{MR?=
MM1R MkTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj3OmxxOC53LUKuOUDPxE1? NIrqb4M1QCCq MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWGyOFQxPTF{MR?=
MM1S M4fOTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fvW|AvPS1{LkWg{txO MXm0PEBp NVTDcHRPcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NU\4[FNOOjR2MEWxNlE>
H929 M2fvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoraNE42NTJwNTFOwG0> NF3m[3c1QCCq NIXVV3FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUOyOFQxPTF{MR?=
RPMI NUDIbXFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MViwMlUuOi53IN88US=> M2XjNlQ5KGh? M4XZU4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M332bFI1PDB3MUKx
SKBR3 M2nObmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuzN{DPxE1? MoHWOUBl NXPZNHJFcW6qaXLpeJMhOzYxvJWgZ4VtdCCpcn;3eIg> MmDINlM6OTh5OUe=
MDA453 NV7ufVdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jwdlM{KM7:TR?= M33qRVUh\A>? M2\l[4lvcGmkaYTzJFM597zHIHPlcIwh\3Kxd4To NWj0d2REOjN7MUi3PVc>
EFM192A MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HqT|M{KM7:TR?= M1y5dVUh\A>? NV\0NmRGcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> M2jTZ|I{QTF6N{m3
AU565 NXHZWIJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[zN{DPxE1? MkizOUBl NVv2b3dHcW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg> NXG1OW5POjN7MUi3PVc>
MDA361 NH\tclBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUSzN{DPxE1? Mn3IOUBl NIDNSYtqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> MnHDNlM6OTh5OUe=
BT474 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOzN{DPxE1? Mn7tOUBl Mkn0bY5pcWKrdIOgNVbwxIViY3XscEBoem:5dHi= NUnOeHY{OjN7MUi3PVc>
HCC202 NUflfHQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;nOm0{OyEQvF2= MV[1JIQ> NWjsUJRFcW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> NUjleYVJOjN7MUi3PVc>
KPL4 NH:zU3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz0OYQ{OyEQvF2= MknVOUBl MlLMbY5pcWKrdIOgOVjwxIViY3XscEBoem:5dHi= M4fn[FI{QTF6N{m3
NCL-N87 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLKN|Mh|ryP MUK1JIQ> MWHpcohq[mm2czCzNg+9jSClZXzsJIdzd3e2aB?= M1nZRVI{QTF6N{m3
UACC812 M1nzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLIN|Mh|ryP MXq1JIQ> NG\ycWFqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> MlXBNlM6OTh5OUe=
HCC2218 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf2N|Mh|ryP MXG1JIQ> M3H4UYlvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To NEDQbYIzOzlzOEe5Oy=>
HCC1569 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXezN{DPxE1? NWDIcYViPSCm MlvEbY5pcWKrdIOgOg+9jSClZXzsJIdzd3e2aB?= M{jOVVI{QTF6N{m3
OE19 NXTY[ZJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOzN{DPxE1? MUO1JIQ> M4H3S4lvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To NG\LSHEzOzlzOEe5Oy=>
OE33 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\ReXM{OyEQvF2= NIW1eoc2KGR? Ml;VbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= M2XmeVI{QTF6N{m3
JIMT1 NVLnXmJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLvN|Mh|ryP MlTBOUBl M4HyXolvcGmkaYTzJFnwxIViY3XscEBoem:5dHi= MWGyN|kyQDd7Nx?=
HCC1954 NIrhNoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jVSlM{KM7:TR?= M1ywSFUh\A>? MUPpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= MUmyN|kyQDd7Nx?=
NUGC4 NEeyenRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHzR3M{OyEQvF2= NHPLWms2KGR? Mo\5bY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= NUfSflFKOjN7MUi3PVc>
ZR-75-30 NIPobY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXG1OFdTOzNizszN NHjiTlE2KGR? NV[5[VJqcW6qaXLpeJMhNTF378{FJINmdGxiZ4Lve5Rp MWWyN|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):
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
NCT03207529 Recruiting Drug: Alpelisib|Drug: Enzalutamide 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|Estrogen Receptor Negative|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Progesterone Receptor Negative|Progesterone Receptor Positive|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)|Novartis|Astellas Pharma Global Development Inc. June 7 2019 Phase 1
NCT02620839 Recruiting Drug: Alpelisib|Drug: Cisplatin Solid Tumors Pamela Munster|University of California San Francisco December 1 2016 Phase 1
NCT02734615 Recruiting Drug: LSZ102|Drug: LEE011|Drug: BYL719 Advanced or Metastatic ER+ Breast Cancer Novartis Pharmaceuticals|Novartis June 14 2016 Phase 1
NCT02550743 Terminated Drug: BYL719|Drug: Capecitabine|Radiation: Radiation Rectal Cancer howard safran|Brown University|Lifespan|Novartis Pharmaceuticals Corporation (Financial supporter) June 3 2016 Phase 1
NCT02437318 Active not recruiting Drug: Fulvestrant|Drug: Alpelisib|Drug: Alpelisib placebo Breast Cancer Novartis Pharmaceuticals|Novartis July 23 2015 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID