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
USD 370 In stock
USD 570 In stock
USD 870 In stock
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3 Customer Reviews

  • 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.

    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.

  • 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.

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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 MlXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M135WlAvOS1zMECg{txO M2nTW|czKGh? MnfNTWM2OD1zLkGwJO69VQ>? M2OzUlI2PTVyNUS5
SNU-1076 NV6xWodMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvXNE4yNTFyMDFOwG0> NUHUTY1qPzJiaB?= M4HmVGlEPTB;Nj64NkDPxE1? Mn3uNlU2PTB3NEm=
SNU-1066 NF\Uc|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu3NE4yNTFyMDFOwG0> M13VflczKGh? NHvXbo1KSzVyPUGuNVMh|ryP MV[yOVU2ODV2OR?=
FaDu MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKwMlEuOTByIN88US=> M1fCc|czKGh? NInIWmJKSzVyPUG5MlY3KM7:TR?= M1XKSVI2PTVyNUS5
SNU1041 MoiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnVZmExNjFvMUCwJO69VQ>? MXS3NkBp MYLJR|UxRTJyLk[1JO69VQ>? NIG0cVAzPTV3MEW0PS=>
SCC25 NEDLUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHMWnoxNjFvMUCwJO69VQ>? M3P5S|czKGh? MWLJR|UxRTR7LkOwJO69VQ>? Mn;1NlU2PTB3NEm=
BON-1 MUTGeY5kfGmxbjDBd5NigQ>? MnmyNU8yOCEQvF2= M325W|QhcA>? MWXpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? MUOyOVAzPjJ7Mh?=
QGP-1 NH7UbG1HfW6ldHnvckBCe3OjeR?= NEnicosyNzFyIN88US=> NITvTG41KGh? M4PHW4lvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| NHe4NJAzPTB{NkK5Ni=>
MG-63 NXHmdWJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljpTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= M1jURlI1QTZzN{mw
HOS MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7nUJF7UUN3ME2xOUDPxE4xvJygTWM6OD12MjFOwG0> M{LxUVI1QTZzN{mw
MOS-J NXWxeINLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr6WYU{UUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> NYnsSnQ5OjR7NkG3PVA>
POS-1 NEK4ZlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRThizszN89yNKEmFOUC9N|Yh|ryP MVqyOFk3OTd7MB?=
92.1 NWPwWlQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnOPIlyPTByLUKwNFAhdk1? NFH5Vok2KGR? NIPheoxqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NVnuSpcyOjR3NkO1OFA>
Mel270 M3PnOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;ZcVQ2PTByLUKwNFAhdk1? NXfKS5VUPSCm NWnremdxcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MU[yOFU3OzV2MB?=
Omm1.3 M332XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PFdlUxOC1{MECwJI5O MoLHOUBl MWTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NH3rOngzPDV4M{W0NC=>
Omm1 NXOxOHBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;jdnM1PTByLUKwNFAhdk1? M1PXeFUh\A>? NH3IeXNqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MVyyOFU3OzV2MB?=
C918 M3TWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWO1NFAuOjByMDDuUS=> M1j4ZlUh\A>? NUXLOpJscW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MVSyOFU3OzV2MB?=
Mel290 MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXQOVAxNTJyMECgcm0> MknTOUBl NGeyZnRqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NGDIVGgzPDV4M{W0NC=>
OPM2 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfyNE42NTJwNTFOwG0> NWf4NpRjPDhiaB?= NVzYeZNIcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnLSNlQ1ODVzMkG=
OPM1 Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\qeVAvPS1{LkWg{txO MlnNOFghcA>? NF7PXI9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlzrNlQ1ODVzMkG=
U266 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jPWlAvPS1{LkWg{txO MYC0PEBp MmfnbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHzOcnozPDRyNUGyNS=>
MM1R NYLFVIhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3SbJMxNjVvMj61JO69VQ>? Mn22OFghcA>? M1zsfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYeyOFQxPTF{MR?=
MM1S NVqyb4RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjPR4lxOC53LUKuOUDPxE1? MonPOFghcA>? NEDhbWFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUWyOFQxPTF{MR?=
H929 NVT1S3dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL0NE42NTJwNTFOwG0> M1;Dc|Q5KGh? MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVrMRmhnOjR2MEWxNlE>
RPMI NEXpNGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nlSlAvPS1{LkWg{txO NHPzZ2w1QCCq NI\aUndqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1LoXlI1PDB3MUKx
SKBR3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLrb|hIOzNizszN NFzQWHM2KGR? MVrpcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= MVqyN|kyQDd7Nx?=
MDA453 NFq5XoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDENnU{OyEQvF2= M1PtUVUh\A>? NGnteYJqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> NVy4bIpqOjN7MUi3PVc>
EFM192A MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLiN|Mh|ryP MUm1JIQ> MYXpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= MnHyNlM6OTh5OUe=
AU565 NVP1T445T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXsN|Mh|ryP MWG1JIQ> NXz6XXRpcW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg> NFi4OWYzOzlzOEe5Oy=>
MDA361 NIK4dYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYq0PZdTOzNizszN MWK1JIQ> NX;0OWhzcW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> MXSyN|kyQDd7Nx?=
BT474 NX7vZ4JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L1TlM{KM7:TR?= NIriSpQ2KGR? NFL0d|dqdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> NWnVcotbOjN7MUi3PVc>
HCC202 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSzN{DPxE1? MYC1JIQ> MnXCbY5pcWKrdIOgNlDwxIViY3XscEBoem:5dHi= NX7NVJRoOjN7MUi3PVc>
KPL4 NF3xNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXizN{DPxE1? NE[w[402KGR? NYO5e5VMcW6qaXLpeJMhPTkxvJWgZ4VtdCCpcn;3eIg> MX6yN|kyQDd7Nx?=
NCL-N87 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDMNnc{OyEQvF2= MljmOUBl NEXPU|VqdmirYnn0d{A{Oe,:hTDj[YxtKGe{b4f0bC=> NGnTdoYzOzlzOEe5Oy=>
UACC812 M{jMRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTYXJFpOzNizszN MWm1JIQ> M2e2UolvcGmkaYTzJFI497zHIHPlcIwh\3Kxd4To MnryNlM6OTh5OUe=
HCC2218 MkPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvPWWI5OzNizszN MYG1JIQ> MWXpcohq[mm2czCxOg+9jSClZXzsJIdzd3e2aB?= NW\JbnFLOjN7MUi3PVc>
HCC1569 NWL5XZVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELmeYo{OyEQvF2= M1vPT|Uh\A>? Ml20bY5pcWKrdIOgOg+9jSClZXzsJIdzd3e2aB?= Mn;hNlM6OTh5OUe=
OE19 NVO5SXdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zqUlM{KM7:TR?= NULmNHhIPSCm NUHLemtkcW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> NHjBOYgzOzlzOEe5Oy=>
OE33 M4ridGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HVUVM{KM7:TR?= NHLOW2E2KGR? MXHpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= MnjzNlM6OTh5OUe=
JIMT1 Mlq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzsXnE{OyEQvF2= NVmyeXBKPSCm MXrpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq MlHHNlM6OTh5OUe=
HCC1954 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuzN{DPxE1? Mn[4OUBl NYnze2h6cW6qaXLpeJMhOjoxvJWgZ4VtdCCpcn;3eIg> MVqyN|kyQDd7Nx?=
NUGC4 M2H1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXRVmlvOzNizszN M1XSN|Uh\A>? M17xb4lvcGmkaYTzJFE197zHIHPlcIwh\3Kxd4To NHTFUnMzOzlzOEe5Oy=>
ZR-75-30 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\NNoM5OzNizszN M3rL[VUh\A>? MVjpcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi= M4nlVlI{QTF6N{m3

... Click to View More Cell Line Experimental Data

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:
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
NCT01872260 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 22, 2013 Phase 1
NCT02624557 Recruiting Hepatic Impairment Novartis Pharmaceuticals|Novartis December 21, 2015 Phase 1
NCT02145312 Not yet recruiting Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck Yonsei University October 2016 Phase 2
NCT02298595 Not yet recruiting Carcinoma, Squamous|Squamous Cell Carcinoma|Oropharyngeal Neoplasms|Oropharyngeal Cancer Julie E. Bauman, MD, MPH|Novartis|University of Pittsburgh August 2016 Phase 1|Phase 2
NCT02550743 Recruiting Rectal Cancer howard safran|Brown University|Lifespan|Novartis Pharmaceuticals Corporation (Financial supporter) June 2016 Phase 1
NCT02734615 Recruiting Advanced or Metastatic ER+ Breast Cancer Novartis Pharmaceuticals|Novartis June 2016 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID