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
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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 MkHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TjXlAvOS1zMECg{txO MVG3NkBp MXTJR|UxRTFwMUCg{txO Mmf0NlU2PTB3NEm=
SNU-1076 NWDqXJluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH6d3YxNjFvMUCwJO69VQ>? MYm3NkBp MULJR|UxRTZwOEKg{txO M3zHUlI2PTVyNUS5
SNU-1066 M3W0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHqNE4yNTFyMDFOwG0> MXO3NkBp NVjuN4twUUN3ME2xMlE{KM7:TR?= M{HuSFI2PTVyNUS5
FaDu NVPi[Hp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHOWVAxNjFvMUCwJO69VQ>? M1TnVFczKGh? MU\JR|UxRTF7Lk[2JO69VQ>? M{K5OVI2PTVyNUS5
SNU1041 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDjNE4yNTFyMDFOwG0> M1PjZ|czKGh? NGfEZ3dKSzVyPUKwMlY2KM7:TR?= NIPH[|gzPTV3MEW0PS=>
SCC25 M4[2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnUdJUxNjFvMUCwJO69VQ>? NISzS4E4OiCq NV3CR|FQUUN3ME20PU4{OCEQvF2= MUiyOVU2ODV2OR?=
BON-1 M1\FVWZ2dmO2aX;uJGF{e2G7 MnjTNU8yOCEQvF2= M1z2N|QhcA>? Ml\CbY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? NGPF[FAzPTB{NkK5Ni=>
QGP-1 NG[yVXNHfW6ldHnvckBCe3OjeR?= NGHhcmYyNzFyIN88US=> MoiyOEBp MU\pcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? NUn2dm1tOjVyMk[yPVI>
MG-63 Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{H6c2lEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= M3HYbVI1QTZzN{mw
HOS M3qwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XYR2lEPTB;MUWg{txO97zOIFnDPVA:PDJizszN MoLLNlQ6PjF5OUC=
MOS-J NEKycmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= NEL2bmczPDl4MUe5NC=>
POS-1 NVHtTJlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHq[JR{UUN3ME24JO69Ve,:jDDJR|kxRTN4IN88US=> NVfpW4NUOjR7NkG3PVA>
92.1 NY\OcZRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITBSJM2ODBvMkCwNEBvVQ>? NV32fZZYPSCm NH3wR41qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NFLxZ2MzPDV4M{W0NC=>
Mel270 NHHiUGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX21NFAuOjByMDDuUS=> NELhcIo2KGR? MVfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MVyyOFU3OzV2MB?=
Omm1.3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TNSFUxOC1{MECwJI5O MWG1JIQ> M{L3T4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NGS2R24zPDV4M{W0NC=>
Omm1 MoD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH34d4c2ODBvMkCwNEBvVQ>? NFvVeI42KGR? NYC4NmFTcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MoPXNlQ2PjN3NEC=
C918 NXrleWd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33rcFUxOC1{MECwJI5O MWm1JIQ> NYHMVnVHcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MYOyOFU3OzV2MB?=
Mel290 NFfzdG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrseYo2ODBvMkCwNEBvVQ>? MYO1JIQ> MWLpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NEm2dW4zPDV4M{W0NC=>
OPM2 NXHkbIpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW4S4RTOC53LUKuOUDPxE1? MkC5OFghcA>? Mk\TbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmHyNlQ1ODVzMkG=
OPM1 M1W1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;NToo5OC53LUKuOUDPxE1? MXe0PEBp MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{nGWVI1PDB3MUKx
U266 NVTFSlhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXmyXIFuOC53LUKuOUDPxE1? NGjYPGU1QCCq MlfabY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWKwXVZQOjR2MEWxNlE>
MM1R NG\OOI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCwMlUuOi53IN88US=> NFnXR401QCCq M4rnO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIPsVYkzPDRyNUGyNS=>
MM1S NYXuZ49uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmwMlUuOi53IN88US=> MX20PEBp NYjjNndQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYOyOFQxPTF{MR?=
H929 NETyVlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{SzTlAvPS1{LkWg{txO NGrBcHo1QCCq MnzubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYXh[XV{OjR2MEWxNlE>
RPMI MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\MbIRrOC53LUKuOUDPxE1? NXrJWGlMPDhiaB?= MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYWyOFQxPTF{MR?=
SKBR3 NULXNHZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\uN|Mh|ryP M4ToTFUh\A>? NFO1em9qdmirYnn0d{A{Pe,:hTDj[YxtKGe{b4f0bC=> NF[0VIkzOzlzOEe5Oy=>
MDA453 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[zN{DPxE1? NEn3OXM2KGR? MorXbY5pcWKrdIOgN|jwxIViY3XscEBoem:5dHi= NFjuUGMzOzlzOEe5Oy=>
EFM192A M{nXb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHjN|Mh|ryP NF;5cFU2KGR? MnnubY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= NFfJWWkzOzlzOEe5Oy=>
AU565 NUHsTnhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW5N|Mh|ryP M3zwZlUh\A>? MWrpcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?= M{PEZlI{QTF6N{m3
MDA361 NYTEcGJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOzN{DPxE1? NYjRbGVpPSCm NUXEWHZQcW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> M{LGelI{QTF6N{m3
BT474 NX7TSoJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{OyN|M{KM7:TR?= NHnkSI82KGR? MWnpcohq[mm2czCxOw+9jSClZXzsJIdzd3e2aB?= NV\xZlcxOjN7MUi3PVc>
HCC202 MknrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LibVM{KM7:TR?= MYW1JIQ> MnPvbY5pcWKrdIOgNlDwxIViY3XscEBoem:5dHi= MmXnNlM6OTh5OUe=
KPL4 M1rxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ixcFM{KM7:TR?= NYnnVG5tPSCm NHHwNmVqdmirYnn0d{A2QO,:hTDj[YxtKGe{b4f0bC=> M{HaelI{QTF6N{m3
NCL-N87 NEHwNpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWzN{DPxE1? NF7UXWw2KGR? MX7pcohq[mm2czCzNg+9jSClZXzsJIdzd3e2aB?= M4DUN|I{QTF6N{m3
UACC812 NV63[FdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTYfZFqOzNizszN MnLQOUBl MY\pcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NWTOZ3VtOjN7MUi3PVc>
HCC2218 MkHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVizN{DPxE1? NGTiRoI2KGR? MX3pcohq[mm2czCxOg+9jSClZXzsJIdzd3e2aB?= NHP1TngzOzlzOEe5Oy=>
HCC1569 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL1OHVYOzNizszN Mn;lOUBl MoTWbY5pcWKrdIOgOg+9jSClZXzsJIdzd3e2aB?= NXzjNFY6OjN7MUi3PVc>
OE19 NGLrSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGzN{DPxE1? NVTJb3dJPSCm MlrqbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= NV\JVWMzOjN7MUi3PVc>
OE33 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPOVllTOzNizszN MYG1JIQ> MnrybY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= M1vvW|I{QTF6N{m3
JIMT1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWzN{DPxE1? M1nGd|Uh\A>? NX;qRZh[cW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=> NV7iWnFIOjN7MUi3PVc>
HCC1954 M3zz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPhdHM{OyEQvF2= Mni5OUBl M3jXRYlvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4To MXeyN|kyQDd7Nx?=
NUGC4 NUH4cnVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDsSWs{OyEQvF2= M{PPPVUh\A>? MVjpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= NYmzeopUOjN7MUi3PVc>
ZR-75-30 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPZY1vOzNizszN NUfRbYtCPSCm M3\meIlvcGmkaYTzJE0yPe,:hTDj[YxtKGe{b4f0bC=> MlXCNlM6OTh5OUe=

... 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(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. January 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03601507 Not yet 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) November 30 2018 Phase 2
NCT03386162 Recruiting Breast Cancer PI3K Alpelisib UNICANCER March 15 2018 Phase 2
NCT03138070 Recruiting Head and Neck Squamous Cell Cancer Lawson Health Research Institute October 20 2017 Not Applicable
NCT03292250 Recruiting HNSCC|Head and Neck Neoplasms Seoul National University Hospital|Korean Cancer Study Group|Chungnam National University Hospital September 10 2017 Phase 2

Tech Support

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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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID