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 M3zORWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOwMlEuOTByIN88US=> MUi3NkBp NIfXNWFKSzVyPUGuNVAh|ryP MmnyNlU2PTB3NEm=
SNU-1076 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXYNE4yNTFyMDFOwG0> MnvKO|IhcA>? M{jxcWlEPTB;Nj64NkDPxE1? M3;nXlI2PTVyNUS5
SNU-1066 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVewMlEuOTByIN88US=> M1LrNFczKGh? MlL5TWM2OD1zLkGzJO69VQ>? NUnOO|ZJOjV3NUC1OFk>
FaDu MlXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGSyPYQxNjFvMUCwJO69VQ>? MlPxO|IhcA>? MVfJR|UxRTF7Lk[2JO69VQ>? MUiyOVU2ODV2OR?=
SNU1041 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH70T3MxNjFvMUCwJO69VQ>? NX7mSoRnPzJiaB?= NFXGU4ZKSzVyPUKwMlY2KM7:TR?= NGnneYczPTV3MEW0PS=>
SCC25 MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGwMlEuOTByIN88US=> Mn;wO|IhcA>? NW\zNnVMUUN3ME20PU4{OCEQvF2= M2XKcVI2PTVyNUS5
BON-1 NF3leJFHfW6ldHnvckBCe3OjeR?= NGHL[IEyNzFyIN88US=> MX60JIg> NGfQOnZqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NH;OWWUzPTB{NkK5Ni=>
QGP-1 NY\nTVd5TnWwY4Tpc44hSXO|YYm= M3ywWVEwOTBizszN M3;NdlQhcA>? NHfDRWhqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= Mn6xNlUxOjZ{OUK=
MG-63 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3K3fGlEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= MmKxNlQ6PjF5OUC=
HOS MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnmyTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= NU\wU4dyOjR7NkG3PVA>
MOS-J NHTyc3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPTN2VwUUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> MWWyOFk3OTd7MB?=
POS-1 M{L0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXLbGdKSzVyPUig{txO97zOIFnDPVA:OzZizszN NEnyO24zPDl4MUe5NC=>
92.1 Mof5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPDOVAxNTJyMECgcm0> NETlepk2KGR? MmDCbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MWGyOFU3OzV2MB?=
Mel270 Mo\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XCclUxOC1{MECwJI5O MljOOUBl M{KzPYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MkPnNlQ2PjN3NEC=
Omm1.3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjJe|BkPTByLUKwNFAhdk1? NHu4XZQ2KGR? NHm2cJJqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M1zJNFI1PTZ|NUSw
Omm1 NHPGSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqyVGk2ODBvMkCwNEBvVQ>? M3HiPVUh\A>? NULvZ4dKcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MnLpNlQ2PjN3NEC=
C918 NXrhU4hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;PS4FyPTByLUKwNFAhdk1? NXHjepdpPSCm NUKxO|hpcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M4rweVI1PTZ|NUSw
Mel290 MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvmR5FTPTByLUKwNFAhdk1? NFTPOGY2KGR? Mkn5bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NWDUblg2OjR3NkO1OFA>
OPM2 NETMeZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\4OGoxNjVvMj61JO69VQ>? MUm0PEBp MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUeyOFQxPTF{MR?=
OPM1 NYrhbmxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPPNE42NTJwNTFOwG0> MkntOFghcA>? Ml:5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NELtS4IzPDRyNUGyNS=>
U266 NIW0T2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfNNE42NTJwNTFOwG0> M{PQS|Q5KGh? M{TocIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3ToTFI1PDB3MUKx
MM1R MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHYdHV1OC53LUKuOUDPxE1? NH;UNlY1QCCq MnzrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2m5V|I1PDB3MUKx
MM1S Mk\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDDTncxNjVvMj61JO69VQ>? NGnKOpk1QCCq M124TolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIC5VIozPDRyNUGyNS=>
H929 NVHtUlJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vIXVAvPS1{LkWg{txO Mo\WOFghcA>? NXfuXZJNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnzMNlQ1ODVzMkG=
RPMI MkXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrZNE42NTJwNTFOwG0> NWjB[2ZnPDhiaB?= M2PzUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlTNNlQ1ODVzMkG=
SKBR3 NIDWNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPMN|Mh|ryP NEXYNIw2KGR? NYC0c3EycW6qaXLpeJMhOzYxvJWgZ4VtdCCpcn;3eIg> NIDONlIzOzlzOEe5Oy=>
MDA453 MlWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDGN|Mh|ryP NH3GU5I2KGR? NELNeGVqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> MWOyN|kyQDd7Nx?=
EFM192A M{D4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOzN{DPxE1? NFX6VGM2KGR? MmPIbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= M2XsclI{QTF6N{m3
AU565 MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDMdJA{OyEQvF2= MVO1JIQ> NXW5[pRwcW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg> M2fX[|I{QTF6N{m3
MDA361 NI\Vb5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO5XXY{OyEQvF2= MmPCOUBl NV3BflVkcW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> M4nMd|I{QTF6N{m3
BT474 NX3yZY45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPjOZI{OyEQvF2= NVrqOXBsPSCm MljibY5pcWKrdIOgNVbwxIViY3XscEBoem:5dHi= M3fjSlI{QTF6N{m3
HCC202 Mof6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4GxNFM{KM7:TR?= M1K2[FUh\A>? NV3WXFdqcW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> MV[yN|kyQDd7Nx?=
KPL4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLtXmU{OyEQvF2= NFXDXoU2KGR? NGfrUndqdmirYnn0d{A2QO,:hTDj[YxtKGe{b4f0bC=> NFHUenkzOzlzOEe5Oy=>
NCL-N87 NXjQTYFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrLNnA{OyEQvF2= NVPST4lnPSCm M1fjcolvcGmkaYTzJFMy97zHIHPlcIwh\3Kxd4To MXyyN|kyQDd7Nx?=
UACC812 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWizN{DPxE1? NXHGcYxnPSCm NFjvWGpqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> M1rRbFI{QTF6N{m3
HCC2218 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUezN{DPxE1? NF;jZ3Y2KGR? MYDpcohq[mm2czCxOg+9jSClZXzsJIdzd3e2aB?= NFq1c4czOzlzOEe5Oy=>
HCC1569 M4HoTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[zN{DPxE1? NUTP[Ig1PSCm MoXDbY5pcWKrdIOgOg+9jSClZXzsJIdzd3e2aB?= M1LB[lI{QTF6N{m3
OE19 MmTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGzN{DPxE1? NF\WbmM2KGR? NGH1VYxqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> Ml;xNlM6OTh5OUe=
OE33 M2TMeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn22N|Mh|ryP M{XkPVUh\A>? NGizbnBqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> NV7LVlRbOjN7MUi3PVc>
JIMT1 M4D6Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HTS|M{KM7:TR?= MkjwOUBl MYDpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq MWmyN|kyQDd7Nx?=
HCC1954 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f0OVM{KM7:TR?= MWm1JIQ> MnvBbY5pcWKrdIOgNlnwxIViY3XscEBoem:5dHi= M1q4cFI{QTF6N{m3
NUGC4 NF3ZWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[zN{DPxE1? M3XjbFUh\A>? NY\mU4FbcW6qaXLpeJMhOTUxvJWgZ4VtdCCpcn;3eIg> NV;RTIwzOjN7MUi3PVc>
ZR-75-30 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle1N|Mh|ryP NGnSbZY2KGR? MnPobY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To M4PaPFI{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 slightly soluble or 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
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