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.

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In DMSO USD 592 In stock
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Cited by 17 Publications

3 Customer Reviews

  • BYL719 induces Apoptosis in MM cells. The effect of increasing concentrations of BYL719 (0-2.5 umol/l) for 48 h on the apoptosis of MM1s cells. The effect of BYL719 on the apoptosis signalling; cleaved PARP, caspase 3, caspase 9 by Western blotting. MM, multple myeloma.

    Br J Haematol 2014 165(1), 89-101. Alpelisib (BYL719) purchased from Selleck.

  • AN3CA (B), JHUEM2 (D), and MFE296 (H) cells were treated with the indicated doses of BGJ398 and BYL719 alone or in combination for 96 hours, and an SRB assay was subsequently performed.

    Mol Cancer Ther, 2017, 16(4):637-648. Alpelisib (BYL719) purchased from Selleck.

  • A549 cell was trypsinized and plated at 50% confluence in DMEM. 16 hours later, BYL719 was added at final concentrations of 0, 1, 5, 10 and 20uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using total- AKT, pS473-AKT, pT286-CyclinD1 and beta-actin (internal control) antibodies.

    Alpelisib (BYL719) purchased from Selleck.

Purity & Quality Control

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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 NWjUb5duT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XGUVAvOS1zMECg{txO M{HodVczKGh? MnfOTWM2OD1zLkGwJO69VQ>? M36wZ|I2PTVyNUS5
SNU-1076 M3T1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDGcXUxNjFvMUCwJO69VQ>? NXTXdI96PzJiaB?= MmPqTWM2OD14LkiyJO69VQ>? NHq4XoQzPTV3MEW0PS=>
SNU-1066 MnWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrDNE4yNTFyMDFOwG0> MlvzO|IhcA>? M2rVPGlEPTB;MT6xN{DPxE1? NVv1fnB7OjV3NUC1OFk>
FaDu M1TCUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrDNE4yNTFyMDFOwG0> NGrjZ2U4OiCq NWC4WHpLUUN3ME2xPU43PiEQvF2= MlXaNlU2PTB3NEm=
SNU1041 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXiwMlEuOTByIN88US=> MmTSO|IhcA>? MnvBTWM2OD1{MD62OUDPxE1? NHr3dnIzPTV3MEW0PS=>
SCC25 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\pNE4yNTFyMDFOwG0> NYrkdZd2PzJiaB?= MmDCTWM2OD12OT6zNEDPxE1? NF;5UXczPTV3MEW0PS=>
BON-1 NHHSZ3hHfW6ldHnvckBCe3OjeR?= MXuxM|ExKM7:TR?= NGXoVnE1KGh? NHHsWZZqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NUD2cGNFOjVyMk[yPVI>
QGP-1 NILIUGNHfW6ldHnvckBCe3OjeR?= NXLNZopiOS9zMDFOwG0> NEjLN5U1KGh? NIq2[nhqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= MnfuNlUxOjZ{OUK=
MG-63 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjVOFlKSzVyPU[g{txO97zOIFnDPVA:OjRizszN M{m4[VI1QTZzN{mw
HOS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjQTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= M3XhfVI1QTZzN{mw
MOS-J M1Tlb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= NGHkV5ozPDl4MUe5NC=>
POS-1 Mlq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2W1OmlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= M1TEclI1QTZzN{mw
92.1 NH7OcZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nu[lUxOC1{MECwJI5O NImwRW82KGR? NFXaRldqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MlPDNlQ2PjN3NEC=
Mel270 NVjocYFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvMfWw2ODBvMkCwNEBvVQ>? Ml3ROUBl NFzMN4lqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NVmxc29nOjR3NkO1OFA>
Omm1.3 M37STmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn2OWd2PTByLUKwNFAhdk1? MnvxOUBl MVfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MWGyOFU3OzV2MB?=
Omm1 NWqz[YtPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TWWVUxOC1{MECwJI5O MUm1JIQ> MnTUbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> M{D0S|I1PTZ|NUSw
C918 NGK1WXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:4[YgxPTByLUKwNFAhdk1? MkfCOUBl NVfNS3VQcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MlT1NlQ2PjN3NEC=
Mel290 NGrYVGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXO1NFAuOjByMDDuUS=> MY[1JIQ> MVvpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NFzqNm0zPDV4M{W0NC=>
OPM2 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPBT2IxNjVvMj61JO69VQ>? MVq0PEBp M2P5RolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXzw[Gp{OjR2MEWxNlE>
OPM1 NFHScnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCwMlUuOi53IN88US=> MXG0PEBp NIjQNIRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NV\4c5pLOjR2MEWxNlE>
U266 NFHWdJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\6TlAvPS1{LkWg{txO MoXYOFghcA>? NUnMcJlNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXKyOFQxPTF{MR?=
MM1R NFrmV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGiyfVUxNjVvMj61JO69VQ>? NYPiWo45PDhiaB?= MVLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXuyOFQxPTF{MR?=
MM1S MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXywMlUuOi53IN88US=> MoTPOFghcA>? NEHvSYFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWj0RZlxOjR2MEWxNlE>
H929 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mni3NE42NTJwNTFOwG0> NVu1dYhsPDhiaB?= NEPieVRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NX\SXXJVOjR2MEWxNlE>
RPMI MlXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfMVXYxNjVvMj61JO69VQ>? MYq0PEBp MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF3pUFEzPDRyNUGyNS=>
SKBR3 NHHIZldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr5OJE{OyEQvF2= Mn7iOUBl MUDpcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= NWrMNpZ{OjN7MUi3PVc>
MDA453 NXHKXotRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmzN{DPxE1? MoLTOUBl NFTqXXdqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> MnmzNlM6OTh5OUe=
EFM192A MmXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;5S|M{KM7:TR?= M33pW|Uh\A>? NYfVVWZFcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> MoHKNlM6OTh5OUe=
AU565 NFnxOoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LlVFM{KM7:TR?= MofKOUBl NV3iOW1scW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg> MXWyN|kyQDd7Nx?=
MDA361 MnSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PHZVM{KM7:TR?= NY\6RpI6PSCm Ml3xbY5pcWKrdIOgOFTwxIViY3XscEBoem:5dHi= NGm2NJczOzlzOEe5Oy=>
BT474 NEfF[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVqzN{DPxE1? MoP0OUBl M3LvPYlvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To MmHlNlM6OTh5OUe=
HCC202 M1rCN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKzN{DPxE1? MonJOUBl Ml7SbY5pcWKrdIOgNlDwxIViY3XscEBoem:5dHi= MUmyN|kyQDd7Nx?=
KPL4 M1GybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHKVJhMOzNizszN MnXTOUBl NEC2NpVqdmirYnn0d{A2QO,:hTDj[YxtKGe{b4f0bC=> NF7BUHozOzlzOEe5Oy=>
NCL-N87 NFqzfVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;qbmY{OyEQvF2= MlXPOUBl NWe0R21icW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> NYTk[IVFOjN7MUi3PVc>
UACC812 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\SRVM{KM7:TR?= MVO1JIQ> MXnpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NYDFb4p2OjN7MUi3PVc>
HCC2218 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKzN{DPxE1? NG\3ZWY2KGR? NIjCPHhqdmirYnn0d{AyPe,:hTDj[YxtKGe{b4f0bC=> MYeyN|kyQDd7Nx?=
HCC1569 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7ZN|Mh|ryP NGrCZW82KGR? MV\pcohq[mm2czC189yGKGOnbHyg[5Jwf3Sq NWXXSnhLOjN7MUi3PVc>
OE19 M{PZbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nVZ|M{KM7:TR?= M33t[lUh\A>? MkXqbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= MX6yN|kyQDd7Nx?=
OE33 NFf4d|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXSN|Mh|ryP MoLtOUBl NX7keGVwcW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> MY[yN|kyQDd7Nx?=
JIMT1 NIjP[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmzN{DPxE1? NEG5[VY2KGR? NIm5[pFqdmirYnn0d{A697zHIHPlcIwh\3Kxd4To M1Syb|I{QTF6N{m3
HCC1954 M4PaR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrtXoM{OyEQvF2= M1[4PFUh\A>? NYTNNoZpcW6qaXLpeJMhOjoxvJWgZ4VtdCCpcn;3eIg> NYezN3RKOjN7MUi3PVc>
NUGC4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVqzN{DPxE1? MlHPOUBl MknubY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= MYOyN|kyQDd7Nx?=
ZR-75-30 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;GN|Mh|ryP MojKOUBl NE\IenZqdmirYnn0d{AuOTYxvJWgZ4VtdCCpcn;3eIg> MViyN|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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03207529 Not yet recruiting Malignant Neoplasm of Breast M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc. March 31 2019 Phase 1
NCT03207529 Not yet recruiting Malignant Neoplasm of Breast M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc. March 31 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03601507 Recruiting CDKN2A-p16 Positive|Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 University of Arizona|National Cancer Institute (NCI) December 14 2018 Phase 2
NCT03601507 Recruiting CDKN2A-p16 Positive|Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 University of Arizona|National Cancer Institute (NCI) December 14 2018 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID