Alpelisib (BYL719)

For research use only.

Catalog No.S2814

114 publications

Alpelisib (BYL719) Chemical Structure

CAS No. 1217486-61-7

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.

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Selleck's Alpelisib (BYL719) has been cited by 114 publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

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 MkXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLuVVAxNjFvMUCwJO69VQ>? NIfwfo04OiCq M3LVXGlEPTB;MT6xNEDPxE1? MkTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
SNU-1076 NWmxb29zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4i2d|AvOS1zMECg{txO NUj6[|VJPzJiaB?= M1ywPGlEPTB;Nj64NkDPxE1? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3MEW0PUc,OjV3NUC1OFk9N2F-
SNU-1066 NHG4SYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnUNE4yNTFyMDFOwG0> MlPWO|IhcA>? MYjJR|UxRTFwMUOg{txO MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3MEW0PUc,OjV3NUC1OFk9N2F-
FaDu NHXNS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vOfVAvOS1zMECg{txO MVe3NkBp MoX2TWM2OD1zOT62OkDPxE1? MnHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
SNU1041 NXHB[FFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[wMlEuOTByIN88US=> MUi3NkBp MljHTWM2OD1{MD62OUDPxE1? NGGwcJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW1NFU1QSd-MkW1OVA2PDl:L3G+
SCC25 M2fBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMlEuOTByIN88US=> NFXpR4s4OiCq M1yzfmlEPTB;NEmuN|Ah|ryP M3rEeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWwOVQ6Lz5{NUW1NFU1QTxxYU6=
BON-1 MkjoSpVv[3Srb36gRZN{[Xl? MX:xM|ExKM7:TR?= MlHTOEBp MULpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? NELvPWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyOlI6Oid-MkWwNlYzQTJ:L3G+
QGP-1 MVjGeY5kfGmxbjDBd5NigQ>? NUnkcI83OS9zMDFOwG0> MUW0JIg> NFztRZBqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NG[yfZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyOlI6Oid-MkWwNlYzQTJ:L3G+
MG-63 MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MluxTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= MlHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkG3PVAoRjJ2OU[xO|kxRC:jPh?=
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Mel290 NF\YeIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jUZ|UxOC1{MECwJI5O MYW1JIQ> NEjRd5RqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M1O0b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NU[zOVQxLz5{NEW2N|U1ODxxYU6=
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ZR-75-30 M{LYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXzSlM{OyEQvF2= NUC4WlhXPSCm MWjpcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi= MnW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ|OUG4O|k4RC:jPh?=
Rat1 MmHVVFEyOGGucHjhJIlvcGmkaYTpc44h[XO|YYm= NUPucmxZUUN3MDC9JFAvODd2IN88US=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF4NEG4PUc,OjZzNkSxPFk9N2F-
Rat1 M37xN3BKO0ujbIDoZUBqdmirYnn0bY9vKGG|c3H5 NX3Lc2ZWUUN3MDC9JFAvODd2IN88US=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1 NWrOSmd4WDFzMHHsdIhiKGmwaHnibZRqd25iYYPzZZk> NXmzOYNXUUN3MDC9JFAvODd2IN88US=> NX\zVZdzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NlYxOzRpPkKzO|I3ODN2PD;hQi=>
Rat1 NVq3WHRbWDFzMHTlcJRiKGmwaHnibZRqd25iYYPzZZk> MlHUTWM2OCB;IEGuNkDPxE1? NEj6Xog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG2OFE5QSd-Mk[xOlQyQDl:L3G+
Rat1 M4e0PXBKO0upYX3tZUBqdmirYnn0bY9vKGG|c3H5 MlnXTWM2OCB;IEGuNkDPxE1? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1 MUHQNVEx\GWudHGgbY5pcWKrdHnvckBie3OjeR?= M2Hme2lEPTBiPTCxMlIh|ryP MkDyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mk[wN|QoRjJ|N{K2NFM1RC:jPh?=
Rat1 M2j6[HAyOTCkZYThJIlvcGmkaYTpc44h[XO|YYm= MXjJR|UxKD1iMj6yJO69VQ>? Ml;BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzNkSxPFkoRjJ4MU[0NVg6RC:jPh?=
Rat1 Mmj6VGk{U2KndHGgbY5pcWKrdHnvckBie3OjeR?= MkP4TWM2OCB;IEKuNkDPxE1? NXHPfXN6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNFY2ODRpPkK2NlA3PTB2PD;hQi=>
Rat1 M4rveHAyOTCjbIDoZUBqdmirYnn0bY9vKGG|c3H5 NIHjcHNKSzVyIE2gNk4zKM7:TR?= M{T5WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{K2NFM1Lz5{M{eyOlA{PDxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT(S473) / p-AKT(T308); 

PubMed: 25544637     


PIK3CA hot-spot mutant cell lines were treated with 1 µM BYL719 for the indicated period of time. Lysates were immunoblotted to detect the indicated proteins.

p100β / p110α / p85 / p-ERBB3(Y1289); 

PubMed: 25544637     


BT474 cells were treated with 1 µM BYL719 alone for different durations of time and lysates were immunoprecipitated with ERBB3 antibody. Precipitates were analyzed by western blot with the indicated antibodies.

p-HER2 / IGF-1R; 

PubMed: 25544637     


Cells were treated with 1 μM BYL719 for 24 hr and lysates were immunoblotted to detect the indicated proteins.

pS6 (Ser235-236); 

PubMed: 27048245     


Immunoblots of lysates from parental and resistant cells treated for 24 hours as indicated.

PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD; 

PubMed: 27604488     


T47D cells cultured to resistance in the presence of BYL719. Both parental (T47D) and resistant (T47DR) cells were treated with BYL719 at 1μM, and cell lysates were prepared at 0, 4, 24 hours for immunoblotting for the indicated proteins.

25544637 27048245 27604488
Growth inhibition assay
Cell viability; 

PubMed: 27602501     


The effect of BYL719 on cellular viability was evaluated in HCT116 (A) and SW480 (B) CRC cells. Briefly, cells were grown, treated with increasing concentrations of BYL719 (5, 10 and 20 μM) and cellular viability determined by MTS assay 72h after treatments. Controls included cells that remained untreated (media ctrl) and vehicle-treated controls (DMSO). Data represent means ± SEM of at least triplicate experiments normalized to controls. All conditions were compared with DMSO. Ctrl, control; DMSO, dimethyl sulfoxide. **, p< 0.01; ***, p< 0.001; ****, p< 0.0001.

27602501
Immunofluorescence
LC3; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 5 days with DMSO, 500 nM BKM120 or 500 nM BYL719. Cells were treated with DMSO or 1 μM Lapatinib for the final 18 h. GFP-LC3 localization was captured by fluorescent microscopy.

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

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):
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 powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04589650 Not yet recruiting Drug: Alpelisib|Drug: Placebo PIK3CA-related Overgrowth Spectrum (PROS) Novartis Pharmaceuticals|Novartis February 2 2021 Phase 2
NCT04544189 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant|Drug: Placebo Breast Neoplasms Novartis Pharmaceuticals|Novartis December 31 2020 Phase 2
NCT04524000 Recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis November 20 2020 Phase 2
NCT04300790 Recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis October 23 2020 Phase 2
NCT04526470 Not yet recruiting Drug: Alpelisib|Drug: Paclitaxel Solid Tumor|Stomach Cancer Seoul National University Bundang Hospital September 1 2020 Phase 1|Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID