Alpelisib (BYL719)

For research use only.

Catalog No.S2814

80 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 80 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 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fNeVAvOS1zMECg{txO NFPjR4Y4OiCq MnPKTWM2OD1zLkGwJO69VQ>? NUS4O3lqOjV3NUC1OFk>
SNU-1076 NEXGbZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljUNE4yNTFyMDFOwG0> M4\iZlczKGh? NGrt[|dKSzVyPU[uPFIh|ryP MYqyOVU2ODV2OR?=
SNU-1066 NX21c3B7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSwMlEuOTByIN88US=> M1;OOlczKGh? M1rtd2lEPTB;MT6xN{DPxE1? NYHwSHdtOjV3NUC1OFk>
FaDu M{e3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLSNE4yNTFyMDFOwG0> NWrRSWpXPzJiaB?= M{S4fmlEPTB;MUmuOlYh|ryP NHfWe24zPTV3MEW0PS=>
SNU1041 M{X6RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnezNE4yNTFyMDFOwG0> M3K1eFczKGh? Mlv2TWM2OD1{MD62OUDPxE1? NFzQVnIzPTV3MEW0PS=>
SCC25 NGi5OHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LzVVAvOS1zMECg{txO NXPB[VJlPzJiaB?= MmXCTWM2OD12OT6zNEDPxE1? MnLaNlU2PTB3NEm=
BON-1 NFvkbYhHfW6ldHnvckBCe3OjeR?= MmHRNU8yOCEQvF2= MXu0JIg> Mn7wbY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? NYXWTGRTOjVyMk[yPVI>
QGP-1 Ml7ISpVv[3Srb36gRZN{[Xl? M3TOblEwOTBizszN NG[wR2E1KGh? M2jHRolvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| MYqyOVAzPjJ7Mh?=
MG-63 NYDQUldDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELvV5dKSzVyPU[g{txO97zOIFnDPVA:OjRizszN NUHHVo9ROjR7NkG3PVA>
HOS MoTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rwfGlEPTB;MUWg{txO97zOIFnDPVA:PDJizszN MWCyOFk3OTd7MB?=
MOS-J NHrZXolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PaOWlEPTB;MUCg{txO97zOIFnDPVA:OzZizszN M3q3VFI1QTZzN{mw
POS-1 MnzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KyUWlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= NFG4fHQzPDl4MUe5NC=>
92.1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXFcmpCPTByLUKwNFAhdk1? MlPZOUBl NHqwVndqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NHq0RoQzPDV4M{W0NC=>
Mel270 NUnlTnNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[ycnU2ODBvMkCwNEBvVQ>? MWK1JIQ> MU\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> Mn\ENlQ2PjN3NEC=
Omm1.3 NGfHcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fIZ|UxOC1{MECwJI5O MWq1JIQ> NF3BfWZqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NYrIcphjOjR3NkO1OFA>
Omm1 NGPUZ2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2WwcVUxOC1{MECwJI5O Ml6wOUBl NYHGTo5jcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MkTuNlQ2PjN3NEC=
C918 M4jTTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITGNZk2ODBvMkCwNEBvVQ>? NEnXS2w2KGR? NI\yXmxqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M{e0cVI1PTZ|NUSw
Mel290 NIDNOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHKOVAxNTJyMECgcm0> MYO1JIQ> NV\qcW1ycW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MUOyOFU3OzV2MB?=
OPM2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnMW2ExNjVvMj61JO69VQ>? NFvUVHo1QCCq MkLubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1HGdFI1PDB3MUKx
OPM1 NXTPb2ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTIRYFXOC53LUKuOUDPxE1? M375S|Q5KGh? NVvWbWY3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MkjLNlQ1ODVzMkG=
U266 NWGzco97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDFNIYxNjVvMj61JO69VQ>? Moq5OFghcA>? NVfGcI5VcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmLaNlQ1ODVzMkG=
MM1R M3jOfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jjbFAvPS1{LkWg{txO MUm0PEBp MlTWbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUDqbYRUOjR2MEWxNlE>
MM1S NXXUXm97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6wMlUuOi53IN88US=> Mn3COFghcA>? MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF21Rm4zPDRyNUGyNS=>
H929 NIPHNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\ENE42NTJwNTFOwG0> NF[0fVk1QCCq MnPDbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYCyOFQxPTF{MR?=
RPMI NXfiZ|N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVn5TnVMOC53LUKuOUDPxE1? NY\ZZ4M1PDhiaB?= MUTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mle4NlQ1ODVzMkG=
SKBR3 MnTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jWTFM{KM7:TR?= NHGySFQ2KGR? M{PXeIlvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To M2XGblI{QTF6N{m3
MDA453 Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPEXYVEOzNizszN NX\HT2dzPSCm Ml:zbY5pcWKrdIOgN|jwxIViY3XscEBoem:5dHi= NGPjTnMzOzlzOEe5Oy=>
EFM192A M1juWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nyV|M{KM7:TR?= NFqxVG02KGR? MWTpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NFrhbnczOzlzOEe5Oy=>
AU565 M3nJcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Plb|M{KM7:TR?= NWOy[3RGPSCm MYDpcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?= MXGyN|kyQDd7Nx?=
MDA361 NXvySXNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOzN{DPxE1? NXv2do9zPSCm NGDnb5VqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> NVz5WpNnOjN7MUi3PVc>
BT474 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXuzN{DPxE1? MoP2OUBl NVfjRYdncW6qaXLpeJMhOTcxvJWgZ4VtdCCpcn;3eIg> MWiyN|kyQDd7Nx?=
HCC202 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnNPIY{OyEQvF2= NWfscGk5PSCm NUO4dXJTcW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> MUSyN|kyQDd7Nx?=
KPL4 NHjTU|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTCN|Mh|ryP NWrmO2diPSCm NF7KPWhqdmirYnn0d{A2QO,:hTDj[YxtKGe{b4f0bC=> NYHXOmZNOjN7MUi3PVc>
NCL-N87 NELTTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVezN{DPxE1? NEHjR4U2KGR? NUjpNYVycW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> Ml7WNlM6OTh5OUe=
UACC812 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXKzN{DPxE1? MV61JIQ> NF;oUZpqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> M1KxPVI{QTF6N{m3
HCC2218 NU\YUow2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWezN{DPxE1? M2DoOVUh\A>? MVLpcohq[mm2czCxOg+9jSClZXzsJIdzd3e2aB?= MnTqNlM6OTh5OUe=
HCC1569 MmrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUizN{DPxE1? M{\G[FUh\A>? NEDRe3RqdmirYnn0d{A297zHIHPlcIwh\3Kxd4To NXnWXHpDOjN7MUi3PVc>
OE19 NFrvToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHEN|Mh|ryP M1PyWVUh\A>? MYLpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NGP6XVEzOzlzOEe5Oy=>
OE33 MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknZN|Mh|ryP NXTuN3N7PSCm NXP0bZJxcW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> MVSyN|kyQDd7Nx?=
JIMT1 NULSe5J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:zN{DPxE1? NULzRlVyPSCm M2PNWIlvcGmkaYTzJFnwxIViY3XscEBoem:5dHi= MXOyN|kyQDd7Nx?=
HCC1954 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4eyWVM{KM7:TR?= MWW1JIQ> MnXjbY5pcWKrdIOgNlnwxIViY3XscEBoem:5dHi= NE\5NpUzOzlzOEe5Oy=>
NUGC4 M2S0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[zN{DPxE1? MW[1JIQ> NGnCfXVqdmirYnn0d{AyPO,:hTDj[YxtKGe{b4f0bC=> M37aVlI{QTF6N{m3
ZR-75-30 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnq5N|Mh|ryP M{PQSlUh\A>? Mn7kbY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To M2H4dlI{QTF6N{m3

... 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)
Water Insoluble
Ethanol '2 mg/mL
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(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