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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2 Customer Reviews

  • 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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M{fOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzFPW5xOC5zLUGwNEDPxE1? M1HMWlczKGh? MVvJR|UxRTFwMUCg{txO NGi5cVMzPTV3MEW0PS=>
SNU-1076 M{nUO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXMNE4yNTFyMDFOwG0> NV7tWI1WPzJiaB?= M4L1cGlEPTB;Nj64NkDPxE1? MXSyOVU2ODV2OR?=
SNU-1066 M4P0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jVNlAvOS1zMECg{txO MUO3NkBp NIHNXYFKSzVyPUGuNVMh|ryP M2ns[|I2PTVyNUS5
FaDu MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnxV3luOC5zLUGwNEDPxE1? MkDKO|IhcA>? Mn;vTWM2OD1zOT62OkDPxE1? NVPEZVFSOjV3NUC1OFk>
SNU1041 M1vtNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGixUm0xNjFvMUCwJO69VQ>? M3TsSlczKGh? M33SSmlEPTB;MkCuOlUh|ryP Mmf3NlU2PTB3NEm=
SCC25 NHjLUm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHz4V|kxNjFvMUCwJO69VQ>? M{DCOlczKGh? MXTJR|UxRTR7LkOwJO69VQ>? Mk[wNlU2PTB3NEm=
BON-1 NXfJdYFZTnWwY4Tpc44hSXO|YYm= M{GzO|EwOTBizszN NXPXZ|RQPCCq M3j0c4lvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| NXriTJFtOjVyMk[yPVI>
QGP-1 NUfyU2RGTnWwY4Tpc44hSXO|YYm= MlPtNU8yOCEQvF2= MXy0JIg> MonmbY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? NGDFO4YzPTB{NkK5Ni=>
MG-63 NFHEV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjHNXlKSzVyPU[g{txO97zOIFnDPVA:OjRizszN NITzZYkzPDl4MUe5NC=>
HOS MnHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnqOZFKSzVyPUG1JO69Ve,:jDDJR|kxRTR{IN88US=> M{m4SlI1QTZzN{mw
MOS-J MoDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkG2TWM2OD1zMDFOwG3wxIxiSVO5NF0{PiEQvF2= M1TBc|I1QTZzN{mw
POS-1 NWrEe4N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XLemlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= M1jjVFI1QTZzN{mw
92.1 MoTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrnOVAxNTJyMECgcm0> M16xbFUh\A>? M4qxcYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MkLUNlQ2PjN3NEC=
Mel270 M{m2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDYOVAxNTJyMECgcm0> MVi1JIQ> MXrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MnHJNlQ2PjN3NEC=
Omm1.3 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWS1NFAuOjByMDDuUS=> NUCze5RZPSCm MnL0bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MnrGNlQ2PjN3NEC=
Omm1 MoewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnqOVAxNTJyMECgcm0> MlXWOUBl MWLpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MVmyOFU3OzV2MB?=
C918 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVq1NFAuOjByMDDuUS=> MXG1JIQ> NI\wTIxqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NFnrOoUzPDV4M{W0NC=>
Mel290 M2[yeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK1NFAuOjByMDDuUS=> NFrldHU2KGR? NVmyS206cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NEXDS40zPDV4M{W0NC=>
OPM2 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGwMlUuOi53IN88US=> MX[0PEBp NIPNR29qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWKyOFQxPTF{MR?=
OPM1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uwS|AvPS1{LkWg{txO NVjtR4lYPDhiaB?= M4Xy[olvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWKyOFQxPTF{MR?=
U266 NYqxbpFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWCzcYk6OC53LUKuOUDPxE1? NX;WcWdYPDhiaB?= MlTpbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXXPfoNDOjR2MEWxNlE>
MM1R NF3Ec2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LTXFAvPS1{LkWg{txO NX3TXpJIPDhiaB?= MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3j5[lI1PDB3MUKx
MM1S NG\tbWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjCNE42NTJwNTFOwG0> MWK0PEBp NID1T|dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUKyOFQxPTF{MR?=
H929 M3HkS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfpcFcxNjVvMj61JO69VQ>? MnLrOFghcA>? NVHXSFdYcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MW[yOFQxPTF{MR?=
RPMI Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\OcFAvPS1{LkWg{txO MkPrOFghcA>? M{nOVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4DKVVI1PDB3MUKx
SKBR3 Mn;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXh[Y1sOzNizszN M13xTVUh\A>? M3fkVIlvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To M13nNVI{QTF6N{m3
MDA453 NHXQN|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;UNGt2OzNizszN NX;jcZFDPSCm M4O3S4lvcGmkaYTzJFM597zHIHPlcIwh\3Kxd4To NVzMZY01OjN7MUi3PVc>
EFM192A MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjLN|Mh|ryP NF7GUVM2KGR? NHGzbWJqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> NIHVd3EzOzlzOEe5Oy=>
AU565 NH\jPYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHvNo1nOzNizszN MWm1JIQ> MmfXbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= Mk[2NlM6OTh5OUe=
MDA361 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOzN{DPxE1? MXi1JIQ> MnHEbY5pcWKrdIOgOFTwxIViY3XscEBoem:5dHi= MlrhNlM6OTh5OUe=
BT474 NYW3S417T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoraN|Mh|ryP M2K4PFUh\A>? M2rkRolvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To M{PTRlI{QTF6N{m3
HCC202 NGrCNWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\VPFM{KM7:TR?= M4P0TlUh\A>? NFLYdFBqdmirYnn0d{AzOO,:hTDj[YxtKGe{b4f0bC=> M4LiRlI{QTF6N{m3
KPL4 NWG2V5FvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u2R|M{KM7:TR?= NHPCNIQ2KGR? NV;j[3Z6cW6qaXLpeJMhPTkxvJWgZ4VtdCCpcn;3eIg> NVfUZYk1OjN7MUi3PVc>
NCL-N87 NFvvZlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCzN{DPxE1? NH3jRoo2KGR? NYHNbYk{cW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> NHr6[3YzOzlzOEe5Oy=>
UACC812 NF;QWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVyzN{DPxE1? M1fpW|Uh\A>? Mn6zbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= M3[zdlI{QTF6N{m3
HCC2218 M1G1bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PwWlM{KM7:TR?= NVz1bItxPSCm M37wcolvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To MYCyN|kyQDd7Nx?=
HCC1569 NWHSTWJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3qN|Mh|ryP NU\qZWRmPSCm MknobY5pcWKrdIOgOg+9jSClZXzsJIdzd3e2aB?= M4XrWFI{QTF6N{m3
OE19 NUC2R5lpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[zN{DPxE1? NVLCbGt7PSCm NXP2W2V6cW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> NYPyNYx5OjN7MUi3PVc>
OE33 NWO0bWtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfRe2w{OyEQvF2= MX21JIQ> NIn1XG1qdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> NXy2NIY2OjN7MUi3PVc>
JIMT1 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzE[Fc{OyEQvF2= NXHBTnFyPSCm MVHpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq NY\RNJJROjN7MUi3PVc>
HCC1954 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rRPFM{KM7:TR?= NGPqNlA2KGR? M{Hp[YlvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4To NGXNb5IzOzlzOEe5Oy=>
NUGC4 MlLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULMOZJLOzNizszN NWTHcmVsPSCm NX;kfXB6cW6qaXLpeJMhOTUxvJWgZ4VtdCCpcn;3eIg> NEHlVpQzOzlzOEe5Oy=>
ZR-75-30 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Tkc|M{KM7:TR?= MofuOUBl NYC0W4xXcW6qaXLpeJMhNTF378{FJINmdGxiZ4Lve5Rp NY\qTIZFOjN7MUi3PVc>

... 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 <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID