Alpelisib (BYL719)

Catalog No.S2814

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.

Size Price Stock Quantity  
In DMSO USD 592 In stock
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Cited by 52 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 MmLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TlRVAvOS1zMECg{txO M1PLU|czKGh? NVi2c2xvUUN3ME2xMlExKM7:TR?= M1OzO|I2PTVyNUS5
SNU-1076 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnJUpYxNjFvMUCwJO69VQ>? NV73TFdyPzJiaB?= NWrUV|JOUUN3ME22MlgzKM7:TR?= M1XpTVI2PTVyNUS5
SNU-1066 NV23TnhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MViwMlEuOTByIN88US=> M{PRZ|czKGh? Mk[yTWM2OD1zLkGzJO69VQ>? NX\1dWtrOjV3NUC1OFk>
FaDu MmO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{npd|AvOS1zMECg{txO NV\T[|RFPzJiaB?= NYHT[VhMUUN3ME2xPU43PiEQvF2= NIPKUHMzPTV3MEW0PS=>
SNU1041 NX74clQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMlEuOTByIN88US=> NGnTUXA4OiCq NXH2U|NDUUN3ME2yNE43PSEQvF2= M4\aT|I2PTVyNUS5
SCC25 M4L2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLHW3hQOC5zLUGwNEDPxE1? NUfSd|BxPzJiaB?= NXzMdmd{UUN3ME20PU4{OCEQvF2= M3vMb|I2PTVyNUS5
BON-1 M1HubmZ2dmO2aX;uJGF{e2G7 Mnn6NU8yOCEQvF2= NIjjeJQ1KGh? MX3pcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? M2DzU|I2ODJ4Mkmy
QGP-1 NEjnOo5HfW6ldHnvckBCe3OjeR?= M{jFWFEwOTBizszN MUm0JIg> M{jFc4lvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| MnvSNlUxOjZ{OUK=
MG-63 NFHO[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TNcGlEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= MWCyOFk3OTd7MB?=
HOS M4Dtfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTRcmduUUN3ME2xOUDPxE4xvJygTWM6OD12MjFOwG0> NVr2VYtlOjR7NkG3PVA>
MOS-J Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj6O2RVUUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> NH[wOnAzPDl4MUe5NC=>
POS-1 MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTUcnVQUUN3ME24JO69Ve,:jDDJR|kxRTN4IN88US=> NHPvWGYzPDl4MUe5NC=>
92.1 M3OxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C3RVUxOC1{MECwJI5O Mnn4OUBl NWLmWIFvcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MkLhNlQ2PjN3NEC=
Mel270 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD3OVAxNTJyMECgcm0> MYi1JIQ> NF3EXFdqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MXWyOFU3OzV2MB?=
Omm1.3 MmHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rqb|UxOC1{MECwJI5O MXq1JIQ> MnfXbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MY[yOFU3OzV2MB?=
Omm1 NWnOXZVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\jfo42ODBvMkCwNEBvVQ>? NXW1XVFrPSCm M{P6U4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MkfPNlQ2PjN3NEC=
C918 M3K5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUG1NFAuOjByMDDuUS=> NGLjVIc2KGR? NH3oXVdqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NYf4PIVMOjR3NkO1OFA>
Mel290 NVHjRmw1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j1[lUxOC1{MECwJI5O MUC1JIQ> NG\ZdGdqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NHLaToUzPDV4M{W0NC=>
OPM2 MoLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMlUuOi53IN88US=> Moe2OFghcA>? NUfFbGVZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MX[yOFQxPTF{MR?=
OPM1 Mk\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HEUVAvPS1{LkWg{txO NFzS[Ic1QCCq NVLRU2xwcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIrh[nIzPDRyNUGyNS=>
U266 NGLrd5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3tNE42NTJwNTFOwG0> NX3YemlbPDhiaB?= NGTXNHRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFvHN5kzPDRyNUGyNS=>
MM1R MlrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\1NE42NTJwNTFOwG0> MWW0PEBp MmfCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVmzUlB1OjR2MEWxNlE>
MM1S MnztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnhVJExNjVvMj61JO69VQ>? NWjwdZIzPDhiaB?= MkTlbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlO0NlQ1ODVzMkG=
H929 MmCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[0NE42NTJwNTFOwG0> MYi0PEBp NH20SoNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MV2yOFQxPTF{MR?=
RPMI M2\oZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCwMlUuOi53IN88US=> M3XxZ|Q5KGh? MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MljONlQ1ODVzMkG=
SKBR3 M3;FR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X0cVM{KM7:TR?= NVfHbmdPPSCm NXrMXJdFcW6qaXLpeJMhOzYxvJWgZ4VtdCCpcn;3eIg> NYWzZpFEOjN7MUi3PVc>
MDA453 NGf5XplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWezN{DPxE1? MWS1JIQ> M4n4WolvcGmkaYTzJFM597zHIHPlcIwh\3Kxd4To MmH0NlM6OTh5OUe=
EFM192A MojES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4i4bVM{KM7:TR?= M4H4SlUh\A>? MlnqbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= MmHsNlM6OTh5OUe=
AU565 NVToXXhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXaVHE{OyEQvF2= NXrncHZqPSCm MnjDbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= MlfjNlM6OTh5OUe=
MDA361 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHwN|Mh|ryP NHy2doI2KGR? NXrrfVZ3cW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> M4rpWlI{QTF6N{m3
BT474 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zESFM{KM7:TR?= NGLybHI2KGR? NVLtT3g2cW6qaXLpeJMhOTcxvJWgZ4VtdCCpcn;3eIg> MmHhNlM6OTh5OUe=
HCC202 NWDjRZJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:xSWN6OzNizszN NUfWW5N4PSCm M1PzfIlvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To MlLrNlM6OTh5OUe=
KPL4 NFLwSZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq3SZM{OyEQvF2= MoDvOUBl MXzpcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= MojnNlM6OTh5OUe=
NCL-N87 MoTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEP6Z2I{OyEQvF2= M4XZNlUh\A>? MnfMbY5pcWKrdIOgN|HwxIViY3XscEBoem:5dHi= M2\yblI{QTF6N{m3
UACC812 M3PicWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:zN{DPxE1? MkDJOUBl M1nFbolvcGmkaYTzJFI497zHIHPlcIwh\3Kxd4To NIfXdIMzOzlzOEe5Oy=>
HCC2218 M4H4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfwTIo{OyEQvF2= M3nuUlUh\A>? MXfpcohq[mm2czCxOg+9jSClZXzsJIdzd3e2aB?= MknGNlM6OTh5OUe=
HCC1569 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUezN{DPxE1? MkCxOUBl NFWzVXNqdmirYnn0d{A297zHIHPlcIwh\3Kxd4To M4PQdlI{QTF6N{m3
OE19 MnP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOzN{DPxE1? MkL6OUBl MoG0bY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= NHrhN24zOzlzOEe5Oy=>
OE33 NYrQWG9kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHr4fGI{OyEQvF2= MXy1JIQ> MXvpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= M4HuZlI{QTF6N{m3
JIMT1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vsTlM{KM7:TR?= NFfsNGU2KGR? M3LXbYlvcGmkaYTzJFnwxIViY3XscEBoem:5dHi= MWOyN|kyQDd7Nx?=
HCC1954 NX73R2xGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSzN{DPxE1? NXfW[WdzPSCm MXvpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= M3fIUFI{QTF6N{m3
NUGC4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUizN{DPxE1? MlraOUBl MXHpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= MUiyN|kyQDd7Nx?=
ZR-75-30 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2zN{DPxE1? NGGwcYs2KGR? MWHpcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi= NUjVb4s4OjN7MUi3PVc>

... 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

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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