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 NITPNIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\kUndpOC5zLUGwNEDPxE1? NEjwc|E4OiCq MYjJR|UxRTFwMUCg{txO M3rCV|I2PTVyNUS5
SNU-1076 NUL2dJh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M135cFAvOS1zMECg{txO M2HBWVczKGh? M3;NdmlEPTB;Nj64NkDPxE1? M1LTNFI2PTVyNUS5
SNU-1066 M1TTT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPtdXR6OC5zLUGwNEDPxE1? MXW3NkBp NFTXTXBKSzVyPUGuNVMh|ryP MX2yOVU2ODV2OR?=
FaDu MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDBd5oxNjFvMUCwJO69VQ>? MojNO|IhcA>? MWjJR|UxRTF7Lk[2JO69VQ>? MV:yOVU2ODV2OR?=
SNU1041 NYjnb3dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofsNE4yNTFyMDFOwG0> NYDBZWxqPzJiaB?= NGnEeldKSzVyPUKwMlY2KM7:TR?= Mmf4NlU2PTB3NEm=
SCC25 NHXNdIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmwMlEuOTByIN88US=> NELQfYQ4OiCq MoLOTWM2OD12OT6zNEDPxE1? NGXTfI4zPTV3MEW0PS=>
BON-1 MYjGeY5kfGmxbjDBd5NigQ>? NHS3XoQyNzFyIN88US=> M1G2XlQhcA>? NUW0eIY{cW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= NUPVRYsyOjVyMk[yPVI>
QGP-1 NHPicGRHfW6ldHnvckBCe3OjeR?= MUWxM|ExKM7:TR?= NWr1fFZDPCCq M4nZT4lvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| NVnOdpF6OjVyMk[yPVI>
MG-63 NH;TdmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGe0TWRKSzVyPU[g{txO97zOIFnDPVA:OjRizszN MnTxNlQ6PjF5OUC=
HOS NIHxSmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W5dmlEPTB;MUWg{txO97zOIFnDPVA:PDJizszN MUWyOFk3OTd7MB?=
MOS-J M1zId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTwTWM2OD1zMDFOwG3wxIxiSVO5NF0{PiEQvF2= Mne0NlQ6PjF5OUC=
POS-1 NHLaT3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TxUWlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= Mn63NlQ6PjF5OUC=
92.1 NFnl[2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUO3ZlY6PTByLUKwNFAhdk1? NH6wWWI2KGR? Mn;ybY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NWjTUIZMOjR3NkO1OFA>
Mel270 NHi5XmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnrenU4PTByLUKwNFAhdk1? NYrDTphQPSCm MUHpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MUGyOFU3OzV2MB?=
Omm1.3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD0T41SPTByLUKwNFAhdk1? Mn7LOUBl M3vDSYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M2XVTlI1PTZ|NUSw
Omm1 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nFcFUxOC1{MECwJI5O MVK1JIQ> M{LXU4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NFzFVnAzPDV4M{W0NC=>
C918 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLVdmp3PTByLUKwNFAhdk1? M{fHRlUh\A>? NHewWXBqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NXewcFZDOjR3NkO1OFA>
Mel290 MmX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWO1NFAuOjByMDDuUS=> M3juXlUh\A>? NXu0dJhwcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MUOyOFU3OzV2MB?=
OPM2 NU\rdHN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkW4NE42NTJwNTFOwG0> NUCwb|ZKPDhiaB?= NHHYW4dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF73UXozPDRyNUGyNS=>
OPM1 NYLmUGp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PLelAvPS1{LkWg{txO M{fWOVQ5KGh? NI\0fJdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXSyOFQxPTF{MR?=
U266 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3rNE42NTJwNTFOwG0> M1fkdVQ5KGh? MljybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWCxUWZtOjR2MEWxNlE>
MM1R NG[xdlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jSTlAvPS1{LkWg{txO MXi0PEBp MnfSbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3nzbVI1PDB3MUKx
MM1S MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfTe|YxNjVvMj61JO69VQ>? NHLU[Ho1QCCq NXvHRoZlcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYOyOFQxPTF{MR?=
H929 M{fyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGwMlUuOi53IN88US=> MXS0PEBp MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1TSPFI1PDB3MUKx
RPMI NH7tW2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfOTIFmOC53LUKuOUDPxE1? NF34eng1QCCq M1;N[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXOyOFQxPTF{MR?=
SKBR3 NH3MeY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf3N|Mh|ryP M{fjelUh\A>? MVTpcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= NHL4RVkzOzlzOEe5Oy=>
MDA453 NGXaeGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D6OVM{KM7:TR?= NHnteHk2KGR? MYLpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= MVyyN|kyQDd7Nx?=
EFM192A NH3JdGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfJN|Mh|ryP MnTZOUBl NGfWeVlqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> MXuyN|kyQDd7Nx?=
AU565 NIO1[lZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[zN{DPxE1? NXHySGo1PSCm M1rWTIlvcGmkaYTzJFI397zHIHPlcIwh\3Kxd4To MnfiNlM6OTh5OUe=
MDA361 M1rocGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXvT3E{OyEQvF2= MkfkOUBl NY\RXY9icW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> NUjwNpVQOjN7MUi3PVc>
BT474 MoCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWezN{DPxE1? NEPLcVQ2KGR? MWXpcohq[mm2czCxOw+9jSClZXzsJIdzd3e2aB?= M2H0SlI{QTF6N{m3
HCC202 NVK0emFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfYZYc{OyEQvF2= MVG1JIQ> MVLpcohq[mm2czCyNQ+9jSClZXzsJIdzd3e2aB?= NIKzWYQzOzlzOEe5Oy=>
KPL4 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2zN{DPxE1? MWC1JIQ> M1jkbolvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To M3r3VlI{QTF6N{m3
NCL-N87 MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vlUlM{KM7:TR?= M1Tab|Uh\A>? NF;oXFFqdmirYnn0d{A{Oe,:hTDj[YxtKGe{b4f0bC=> NIPXb2MzOzlzOEe5Oy=>
UACC812 MmO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXezN{DPxE1? MYq1JIQ> NF\reG9qdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> M1rZU|I{QTF6N{m3
HCC2218 M{nTOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTPN|Mh|ryP NHXTWJc2KGR? MV7pcohq[mm2czCxOg+9jSClZXzsJIdzd3e2aB?= NI\JRWczOzlzOEe5Oy=>
HCC1569 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSzN{DPxE1? NVTEUlJwPSCm MVfpcohq[mm2czC189yGKGOnbHyg[5Jwf3Sq NHe5b5MzOzlzOEe5Oy=>
OE19 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\Vemc{OyEQvF2= NIPsWYo2KGR? MYTpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NX[2WGM3OjN7MUi3PVc>
OE33 M3j6NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVWzN{DPxE1? NIjNcYk2KGR? MlL5bY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= MmPvNlM6OTh5OUe=
JIMT1 M1m2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYizN{DPxE1? NXjTUY9nPSCm M2fpe4lvcGmkaYTzJFnwxIViY3XscEBoem:5dHi= NXXtZpBpOjN7MUi3PVc>
HCC1954 MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[zN{DPxE1? M2PFOVUh\A>? M3z1TYlvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4To MVyyN|kyQDd7Nx?=
NUGC4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPafI1iOzNizszN NF3vd4U2KGR? M1;6dIlvcGmkaYTzJFE197zHIHPlcIwh\3Kxd4To MWSyN|kyQDd7Nx?=
ZR-75-30 M4TkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPrNnQ{OyEQvF2= NVvBXpV1PSCm NI\y[HdqdmirYnn0d{AuOTYxvJWgZ4VtdCCpcn;3eIg> NWS4b4s5OjN7MUi3PVc>

... 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
NCT02058381 Completed Pre-menopausal Breast Cancer|PI3K Pathway Inhibition Novartis Pharmaceuticals|Novartis May 6 2014 Phase 1
NCT02051751 Completed Neoplasms Breast Neoplasms Head and Neck Neoplasms Novartis Pharmaceuticals|Novartis March 5 2014 Phase 1
NCT01219699 Active not recruiting Advanced Solid Tumors With an Alteration of the PIK3CA Gene|Estrogen Receptor Positive Breast Cancer Novartis Pharmaceuticals|Novartis October 5 2010 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) September 30 2018 Phase 2
NCT02282371 Active not recruiting Head and Neck Squamous Cell Cancer Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals October 30 2014 Phase 1
NCT02155088 Active not recruiting Pancreatic Cancer H. Lee Moffitt Cancer Center and Research Institute|Novartis October 30 2014 Phase 1

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID