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. 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 Mn3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXoNE4yNTFyMDFOwG0> M2\aPVczKGh? M2PjSmlEPTB;MT6xNEDPxE1? NUC4XJB5OjV3NUC1OFk>
SNU-1076 NVn4boxoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXlNE4yNTFyMDFOwG0> NWfyVYhCPzJiaB?= MoDiTWM2OD14LkiyJO69VQ>? NHrTOGIzPTV3MEW0PS=>
SNU-1066 NHTRfZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHYNE4yNTFyMDFOwG0> NWX1[2o2PzJiaB?= NGrjXpNKSzVyPUGuNVMh|ryP NWnofWhrOjV3NUC1OFk>
FaDu MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfvTnMxNjFvMUCwJO69VQ>? MlLqO|IhcA>? MWfJR|UxRTF7Lk[2JO69VQ>? M1LpN|I2PTVyNUS5
SNU1041 Ml;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\Q[FNHOC5zLUGwNEDPxE1? MlLhO|IhcA>? M3yxOGlEPTB;MkCuOlUh|ryP NF\IXpozPTV3MEW0PS=>
SCC25 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX:wMlEuOTByIN88US=> MmC2O|IhcA>? NVvL[JpyUUN3ME20PU4{OCEQvF2= M3\hSVI2PTVyNUS5
BON-1 NYfTOXpXTnWwY4Tpc44hSXO|YYm= MXyxM|ExKM7:TR?= MX20JIg> Mk[3bY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? NV22T2RkOjVyMk[yPVI>
QGP-1 MVrGeY5kfGmxbjDBd5NigQ>? MVyxM|ExKM7:TR?= MUK0JIg> NHHLWGVqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NH;pTJAzPTB{NkK5Ni=>
MG-63 NGXQT3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TzVGlEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= M3i3[VI1QTZzN{mw
HOS MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTF3IN88Ug+9lCCLQ{mwQVQzKM7:TR?= NGqwVXIzPDl4MUe5NC=>
MOS-J NWnIRVJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\ITWM2OD1zMDFOwG3wxIxiSVO5NF0{PiEQvF2= M3niNVI1QTZzN{mw
POS-1 NIPz[oVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jiZmlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= MXmyOFk3OTd7MB?=
92.1 NF3JcWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnraOVAxNTJyMECgcm0> NFX1dnA2KGR? MXLpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MkLsNlQ2PjN3NEC=
Mel270 MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LHcVUxOC1{MECwJI5O NF\LcFM2KGR? M2PPVolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NW\nXGsxOjR3NkO1OFA>
Omm1.3 NVfLOo41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jpOlUxOC1{MECwJI5O NE\pVXI2KGR? NHHpTW5qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MYeyOFU3OzV2MB?=
Omm1 M3TWPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17RU|UxOC1{MECwJI5O NFvZVHU2KGR? MnLFbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NWrOOZdkOjR3NkO1OFA>
C918 NIXSenhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\mTIZGPTByLUKwNFAhdk1? M1z4RlUh\A>? MVjpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> M1XyXlI1PTZ|NUSw
Mel290 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3O2d|UxOC1{MECwJI5O Mk\xOUBl NFzZO4NqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NXrqeGllOjR3NkO1OFA>
OPM2 NF7zNotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\ZdlAvPS1{LkWg{txO M{HUc|Q5KGh? NVLxZ5RLcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEDFbWozPDRyNUGyNS=>
OPM1 M3\mZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;STlAvPS1{LkWg{txO NGfSeVY1QCCq MmPQbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2H4U|I1PDB3MUKx
U266 NWTSZ2tlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XTPFAvPS1{LkWg{txO MWO0PEBp NYTYbJY3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmPpNlQ1ODVzMkG=
MM1R MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\ZR3JUOC53LUKuOUDPxE1? MnrIOFghcA>? MojObY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3PUclI1PDB3MUKx
MM1S MlXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmwMlUuOi53IN88US=> NEPEVms1QCCq NV3KUoFycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWSyOFQxPTF{MR?=
H929 NXfhV4M{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUmwMlUuOi53IN88US=> MV20PEBp NEnqUW9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2TNR|I1PDB3MUKx
RPMI MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITncHExNjVvMj61JO69VQ>? Ml6yOFghcA>? MmTibY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2H5VVI1PDB3MUKx
SKBR3 M2\ES2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSzN{DPxE1? M1S1c|Uh\A>? NHfyVWZqdmirYnn0d{A{Pe,:hTDj[YxtKGe{b4f0bC=> NFflbZUzOzlzOEe5Oy=>
MDA453 NH\pRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXVdYd3OzNizszN MlnOOUBl MYnpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= MYGyN|kyQDd7Nx?=
EFM192A NGLFeHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jlZlM{KM7:TR?= M2PR[|Uh\A>? MULpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= MXyyN|kyQDd7Nx?=
AU565 M3LFXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13EV|M{KM7:TR?= NXP2dItHPSCm MnnqbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= NITkSmozOzlzOEe5Oy=>
MDA361 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX:zN{DPxE1? NILCe|Q2KGR? MlrCbY5pcWKrdIOgOFTwxIViY3XscEBoem:5dHi= M2CzclI{QTF6N{m3
BT474 NV\IU5lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPvTVg{OyEQvF2= MmD4OUBl NX\YVlZ7cW6qaXLpeJMhOTcxvJWgZ4VtdCCpcn;3eIg> MUiyN|kyQDd7Nx?=
HCC202 Mm\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKzN{DPxE1? M3;HelUh\A>? M1nJT4lvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To NVv5R4U{OjN7MUi3PVc>
KPL4 NVzYRoR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml60N|Mh|ryP NXWwVZQ2PSCm M3nGTIlvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To Moj3NlM6OTh5OUe=
NCL-N87 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofXN|Mh|ryP MkjLOUBl NV7HblNucW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> M{K3bVI{QTF6N{m3
UACC812 NEjEOYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zmTFM{KM7:TR?= MXq1JIQ> NV\UfXk3cW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> MXWyN|kyQDd7Nx?=
HCC2218 MnLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHGR24{OyEQvF2= MUm1JIQ> M1n6dolvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To NFrpNlMzOzlzOEe5Oy=>
HCC1569 M3SxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\3dY9DOzNizszN NHG1RlA2KGR? NXe5[plqcW6qaXLpeJMhPe,:hTDj[YxtKGe{b4f0bC=> MV2yN|kyQDd7Nx?=
OE19 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTtN|Mh|ryP M37UZVUh\A>? NVHTWG5ncW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> MojDNlM6OTh5OUe=
OE33 MojsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlG3N|Mh|ryP MWG1JIQ> MWHpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NEnxcYczOzlzOEe5Oy=>
JIMT1 M2HEe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT2eWM{OyEQvF2= NFXmVVI2KGR? MVrpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq M4jPNlI{QTF6N{m3
HCC1954 NFvrUZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfGZ|c{OyEQvF2= NFr6fZk2KGR? MlzObY5pcWKrdIOgNlnwxIViY3XscEBoem:5dHi= NHfTSFUzOzlzOEe5Oy=>
NUGC4 NWTidVZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mor6N|Mh|ryP NV:1No1HPSCm Mn3CbY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= Mln0NlM6OTh5OUe=
ZR-75-30 NVjRXoZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjQcFI{OyEQvF2= M1ThUlUh\A>? NH;Wd4pqdmirYnn0d{AuOTYxvJWgZ4VtdCCpcn;3eIg> NHX4TXYzOzlzOEe5Oy=>

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID