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, 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 MoqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP4WHdFOC5zLUGwNEDPxE1? MmT0O|IhcA>? Mm\NTWM2OD1zLkGwJO69VQ>? NHnSb2UzPTV3MEW0PS=>
SNU-1076 M3qyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHZT2E4OC5zLUGwNEDPxE1? NXjqcFdbPzJiaB?= NILPOVRKSzVyPU[uPFIh|ryP NFnIWoEzPTV3MEW0PS=>
SNU-1066 NXjXd|R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmwMlEuOTByIN88US=> MmP5O|IhcA>? NFTld3RKSzVyPUGuNVMh|ryP NF64coszPTV3MEW0PS=>
FaDu NFLnZW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGwMlEuOTByIN88US=> NEWxTJE4OiCq NXfMdIlWUUN3ME2xPU43PiEQvF2= NFLGXVQzPTV3MEW0PS=>
SNU1041 NVvz[II4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPBb5RrOC5zLUGwNEDPxE1? NVmxZYdnPzJiaB?= NYe3SmJ7UUN3ME2yNE43PSEQvF2= Ml\PNlU2PTB3NEm=
SCC25 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYX1fGR{OC5zLUGwNEDPxE1? NFXTU|c4OiCq MlHuTWM2OD12OT6zNEDPxE1? NYj4XIdqOjV3NUC1OFk>
BON-1 M1jIc2Z2dmO2aX;uJGF{e2G7 NGrWT|gyNzFyIN88US=> MUe0JIg> MULpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? MX[yOVAzPjJ7Mh?=
QGP-1 NF63OYFHfW6ldHnvckBCe3OjeR?= NGq1XHYyNzFyIN88US=> NFXyV|E1KGh? M1vRTIlvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| MkLlNlUxOjZ{OUK=
MG-63 Mk\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj3UYFxUUN3ME22JO69Ve,:jDDJR|kxRTJ2IN88US=> Mn31NlQ6PjF5OUC=
HOS Mn[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrLbohKSzVyPUG1JO69Ve,:jDDJR|kxRTR{IN88US=> M2HSblI1QTZzN{mw
MOS-J MlXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL1eFg1UUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> MWSyOFk3OTd7MB?=
POS-1 NVfBW|VST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXKTGdKSzVyPUig{txO97zOIFnDPVA:OzZizszN NFLyWVUzPDl4MUe5NC=>
92.1 NXi4d2hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe1NFAuOjByMDDuUS=> NIH4T4g2KGR? M2nxXYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MV:yOFU3OzV2MB?=
Mel270 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXHRnMzPTByLUKwNFAhdk1? MmfGOUBl Ml:1bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MU[yOFU3OzV2MB?=
Omm1.3 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLOS2s2ODBvMkCwNEBvVQ>? MX[1JIQ> MmTCbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NFzHc5EzPDV4M{W0NC=>
Omm1 M1fyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH2SHM2ODBvMkCwNEBvVQ>? M3TEclUh\A>? Mn\jbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> M3jMdFI1PTZ|NUSw
C918 NY\EZVhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXSOVAxNTJyMECgcm0> NU\y[|dHPSCm MVfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> Ml23NlQ2PjN3NEC=
Mel290 NVvTN5JQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHrdmQ2ODBvMkCwNEBvVQ>? NYLoTWUyPSCm M1XZ[olvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NUe3eppuOjR3NkO1OFA>
OPM2 MoDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXi5eWo1OC53LUKuOUDPxE1? NIWzTWk1QCCq M{DIVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3zMWVI1PDB3MUKx
OPM1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD2NE42NTJwNTFOwG0> NYGybnpMPDhiaB?= MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGPNSGEzPDRyNUGyNS=>
U266 M1Hn[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPDVmcxNjVvMj61JO69VQ>? NV7GTnhKPDhiaB?= MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXPmNJJ5OjR2MEWxNlE>
MM1R M3H6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUewMlUuOi53IN88US=> NWjWS4QxPDhiaB?= NI\tWpRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnrGNlQ1ODVzMkG=
MM1S MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3jU49UOC53LUKuOUDPxE1? NXPvV3NiPDhiaB?= MWTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFXKRpgzPDRyNUGyNS=>
H929 M{nP[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrx[|I3OC53LUKuOUDPxE1? MUC0PEBp NF7HTGVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVyyOFQxPTF{MR?=
RPMI MoTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jVb|AvPS1{LkWg{txO M2jRdlQ5KGh? MmDzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mn;rNlQ1ODVzMkG=
SKBR3 M3rJ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HvXVM{KM7:TR?= MWi1JIQ> NWnQcVRtcW6qaXLpeJMhOzYxvJWgZ4VtdCCpcn;3eIg> M4OxXFI{QTF6N{m3
MDA453 NVvoellHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknlN|Mh|ryP M2Hvd|Uh\A>? MYjpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= MnH3NlM6OTh5OUe=
EFM192A NIDzWY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzjbHE{OyEQvF2= NHHhWFQ2KGR? NWfpSG1vcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> MVyyN|kyQDd7Nx?=
AU565 MkTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7iN|Mh|ryP MXu1JIQ> MmTKbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= MlH0NlM6OTh5OUe=
MDA361 NIK3Z2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT1N|Mh|ryP M3q3UFUh\A>? MWXpcohq[mm2czC0OQ+9jSClZXzsJIdzd3e2aB?= MVqyN|kyQDd7Nx?=
BT474 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHiN|Mh|ryP MWC1JIQ> NEXROnNqdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> MUSyN|kyQDd7Nx?=
HCC202 M1r0Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3jNnA{OyEQvF2= MX61JIQ> Mn;tbY5pcWKrdIOgNlDwxIViY3XscEBoem:5dHi= MonjNlM6OTh5OUe=
KPL4 M{nkZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TKbFM{KM7:TR?= MmPvOUBl MY\pcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= NXLJNHFsOjN7MUi3PVc>
NCL-N87 NELZ[olIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\EN|Mh|ryP M4rXR|Uh\A>? MoLJbY5pcWKrdIOgN|HwxIViY3XscEBoem:5dHi= NWH3fJZIOjN7MUi3PVc>
UACC812 NV7KNlRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUezN{DPxE1? MlLCOUBl MXXpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= M4n3TVI{QTF6N{m3
HCC2218 NXfweWlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK1ZYI{OyEQvF2= M{jielUh\A>? NGO1c5ZqdmirYnn0d{AyPe,:hTDj[YxtKGe{b4f0bC=> MmHWNlM6OTh5OUe=
HCC1569 NGfNN45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljuN|Mh|ryP NVy0cok1PSCm MlPNbY5pcWKrdIOgOg+9jSClZXzsJIdzd3e2aB?= NXjmNIcxOjN7MUi3PVc>
OE19 NX22Z2VrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDnN|Mh|ryP MXK1JIQ> MXLpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NGXOeVczOzlzOEe5Oy=>
OE33 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSzN{DPxE1? NFrIWHc2KGR? M1PpdolvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To NGT1S5kzOzlzOEe5Oy=>
JIMT1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuzN{DPxE1? NITLZoQ2KGR? NGLEPHBqdmirYnn0d{A697zHIHPlcIwh\3Kxd4To M3rSclI{QTF6N{m3
HCC1954 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\ae|FrOzNizszN MXW1JIQ> MUPpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= M4C1b|I{QTF6N{m3
NUGC4 M1ux[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXBT48xOzNizszN NFiwSZo2KGR? M2n6XolvcGmkaYTzJFE197zHIHPlcIwh\3Kxd4To NYXMS2lxOjN7MUi3PVc>
ZR-75-30 NHjwO|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnnU2RHOzNizszN M4j0PFUh\A>? MmHGbY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To NEnKXZozOzlzOEe5Oy=>

... 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
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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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID