Alpelisib (BYL719)

Catalog No.S2814

For research use only.

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.

Alpelisib (BYL719) Chemical Structure

CAS No. 1217486-61-7

Selleck's Alpelisib (BYL719) has been cited by 133 publications

Purity & Quality Control

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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 MkTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXaOJpzOC5zLUGwNEDPxE1? MXG3NkBp MVPJR|UxRTFwMUCg{txO M2\FU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWwOVQ6Lz5{NUW1NFU1QTxxYU6=
SNU-1076 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVewMlEuOTByIN88US=> M3TvN|czKGh? NYS3UYM1UUN3ME22MlgzKM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3MEW0PUc,OjV3NUC1OFk9N2F-
SNU-1066 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqwMlEuOTByIN88US=> MYG3NkBp MlOzTWM2OD1zLkGzJO69VQ>? MmfxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
FaDu MnPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\xU|AvOS1zMECg{txO NET0OW84OiCq M4DKVGlEPTB;MUmuOlYh|ryP M3y4b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWwOVQ6Lz5{NUW1NFU1QTxxYU6=
SNU1041 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3sNE4yNTFyMDFOwG0> NW\NZmhlPzJiaB?= M2HF[GlEPTB;MkCuOlUh|ryP NVrYXXJURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVA2PDlpPkK1OVUxPTR7PD;hQi=>
SCC25 M1SwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHqNmkxNjFvMUCwJO69VQ>? NVTlcYJwPzJiaB?= MmTwTWM2OD12OT6zNEDPxE1? NYXTW4Z{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVA2PDlpPkK1OVUxPTR7PD;hQi=>
BON-1 MoniSpVv[3Srb36gRZN{[Xl? NIfsVIgyNzFyIN88US=> NXHVUnd{PCCq MYDpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? MoTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMk[yPVIoRjJ3MEK2NlkzRC:jPh?=
QGP-1 M33HNmZ2dmO2aX;uJGF{e2G7 NF;yWVkyNzFyIN88US=> NW\xbpg3PCCq MXvpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? NXLFUmNNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlYzQTJpPkK1NFI3Ojl{PD;hQi=>
MG-63 M3O4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHRTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl4MUe5NEc,OjR7NkG3PVA9N2F-
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Rat1 MkTsVFEyOGGucHjhJIlvcGmkaYTpc44h[XO|YYm= M2C2UGlEPTBiPTCwMlA4PCEQvF2= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{NkCzOEc,OjN5Mk[wN|Q9N2F-
Rat1 NYG4T411WDFzMHTlcJRiKGmwaHnibZRqd25iYYPzZZk> M1X2[2lEPTBiPTCxMlIh|ryP MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF4NEG4PUc,OjZzNkSxPFk9N2F-
Rat1 MXLQTVNM\2GvbXGgbY5pcWKrdHnvckBie3OjeR?= NELwXlRKSzVyIE2gNU4zKM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1 M4jrSnAyOTCmZXz0ZUBqdmirYnn0bY9vKGG|c3H5 NWPGfJdLUUN3MDC9JFEvOiEQvF2= MmnzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mk[wN|QoRjJ|N{K2NFM1RC:jPh?=
Rat1 NHnaOIFROTFyYnX0ZUBqdmirYnn0bY9vKGG|c3H5 NGOxS3lKSzVyIE2gNk4zKM7:TR?= NIXMdHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG2OFE5QSd-Mk[xOlQyQDl:L3G+
Rat1 NWjGb49SWEl|S3LleIEhcW6qaXLpeIlwdiCjc4PhfS=> NXTMPXNLUUN3MDC9JFIvOiEQvF2= NUf0TINsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNFY2ODRpPkK2NlA3PTB2PD;hQi=>
Rat1 NIPKXVlROTFyYXzwbIEhcW6qaXLpeIlwdiCjc4PhfS=> MnqyTWM2OCB;IEKuNkDPxE1? NETYNHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyOlA{PCd-MkO3NlYxOzR:L3G+
Assay
Methods Test Index PMID
Western blot p-AKT(S473) / p-AKT(T308) ; p100β / p110α / p85 / p-ERBB3(Y1289) ; p-HER2 / IGF-1R ; pS6 (Ser235-236) ; PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD 25544637 27048245 27604488
Growth inhibition assay Cell viability 27602501
Immunofluorescence LC3 26637440
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 (from reference)

Solubility (25°C)

In vitro

DMSO 88 mg/mL
(199.33 mM)
Water Insoluble
Ethanol '2 mg/mL warmed

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.

4.4 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04997902 Not yet recruiting Drug: Tipifarnib|Drug: Alpelisib HNSCC Kura Oncology Inc. October 2021 Phase 1|Phase 2
NCT05022342 Not yet recruiting Other: alpelisib plus fulvestrant Breast Cancer Novartis Pharmaceuticals|Novartis September 15 2021 --
NCT04980833 Not yet recruiting Drug: Alpelisib PIK3CA-related Overgrowth Spectrum (PROS) Novartis Pharmaceuticals|Novartis September 30 2021 Phase 2
NCT04589650 Recruiting Drug: Alpelisib|Drug: Placebo PIK3CA-related Overgrowth Spectrum (PROS) Novartis Pharmaceuticals|Novartis April 19 2021 Phase 2
NCT04762979 Recruiting Drug: Alpelisib|Drug: Fulvestrant|Drug: Aromatase inhibitor Hormone Receptor Positive Breast Carcinoma|HER2-negative Breast Cancer|PIK3CA Mutant Metastatic Breast Cancer Amanda Parkes|Novartis|University of Wisconsin Madison|Big Ten Cancer Research Consortium February 12 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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