Alpelisib (BYL719)

For research use only.

Catalog No.S2814

83 publications

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  
10mM (1mL in DMSO) USD 592 In stock
USD 370 In stock
USD 570 In stock
USD 870 In stock
USD 1270 In stock
USD 1670 In stock
USD 2670 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Alpelisib (BYL719) has been cited by 83 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 MlrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzmU2wxNjFvMUCwJO69VQ>? MX:3NkBp NET6e3FKSzVyPUGuNVAh|ryP Ml7aNlU2PTB3NEm=
SNU-1076 NG\oZllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuwMlEuOTByIN88US=> NGKycXo4OiCq MVTJR|UxRTZwOEKg{txO NYP5[XZFOjV3NUC1OFk>
SNU-1066 NYjQclByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKwMlEuOTByIN88US=> NUHGb|ZPPzJiaB?= NXv1fYR7UUN3ME2xMlE{KM7:TR?= NF34eXYzPTV3MEW0PS=>
FaDu MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYKxZVFnOC5zLUGwNEDPxE1? MmD2O|IhcA>? MYHJR|UxRTF7Lk[2JO69VQ>? NECyOIczPTV3MEW0PS=>
SNU1041 M2j1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4e2TlAvOS1zMECg{txO NFfSbIs4OiCq M3fxV2lEPTB;MkCuOlUh|ryP M1XQSVI2PTVyNUS5
SCC25 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjHeIdXOC5zLUGwNEDPxE1? MoPrO|IhcA>? NYrnSYhCUUN3ME20PU4{OCEQvF2= NXLhVVhuOjV3NUC1OFk>
BON-1 NWHyfIRnTnWwY4Tpc44hSXO|YYm= M1\afVEwOTBizszN NXW4fI52PCCq MoH6bY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? M4LVUVI2ODJ4Mkmy
QGP-1 NWDiSm1TTnWwY4Tpc44hSXO|YYm= MkLDNU8yOCEQvF2= MYm0JIg> NFr2NZNqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= MWCyOVAzPjJ7Mh?=
MG-63 M3Ptemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTZizszN89yNKEmFOUC9NlQh|ryP MmjENlQ6PjF5OUC=
HOS NU\WUo5[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTyTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= MYqyOFk3OTd7MB?=
MOS-J NGXpNYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPEZ5h[UUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> MoeyNlQ6PjF5OUC=
POS-1 NVrPZlVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRThizszN89yNKEmFOUC9N|Yh|ryP MWKyOFk3OTd7MB?=
92.1 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HWb|UxOC1{MECwJI5O MorIOUBl M1H1folvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MliyNlQ2PjN3NEC=
Mel270 NWHncGZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDOOVAxNTJyMECgcm0> M1TmVVUh\A>? Ml\PbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NXHKNJloOjR3NkO1OFA>
Omm1.3 NUXPU3JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnzR2Q2ODBvMkCwNEBvVQ>? MoLNOUBl M3PnUYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M{TJbFI1PTZ|NUSw
Omm1 Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fRblUxOC1{MECwJI5O Ml7zOUBl M{H5XIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NHHyU|AzPDV4M{W0NC=>
C918 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf5OVAxNTJyMECgcm0> MX21JIQ> MYnpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> M3rvWFI1PTZ|NUSw
Mel290 NXT6T4lHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUi1NFAuOjByMDDuUS=> M1zkb|Uh\A>? MYPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MWSyOFU3OzV2MB?=
OPM2 NYnlOFNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzJSHZXOC53LUKuOUDPxE1? NHPFUnQ1QCCq MXLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVyyOFQxPTF{MR?=
OPM1 M37FTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDzSmJWOC53LUKuOUDPxE1? M3;QbFQ5KGh? NFOxO5dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M17qbVI1PDB3MUKx
U266 MnPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTn[I5zOC53LUKuOUDPxE1? NIjNZpA1QCCq MofxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYjJVmJlOjR2MEWxNlE>
MM1R M4\QN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnFRlRIOC53LUKuOUDPxE1? M2jWOlQ5KGh? NF7xb3JqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVr3foxsOjR2MEWxNlE>
MM1S MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fqdVAvPS1{LkWg{txO MYW0PEBp MX3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVyyOFQxPTF{MR?=
H929 NFruUYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq2SXBbOC53LUKuOUDPxE1? MomyOFghcA>? NXKxboNzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1fSWFI1PDB3MUKx
RPMI NEfjOndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zROlAvPS1{LkWg{txO NIroOFg1QCCq MnLWbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkPaNlQ1ODVzMkG=
SKBR3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[2emlrOzNizszN MVW1JIQ> M1vwPIlvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To M2TFclI{QTF6N{m3
MDA453 M1;sNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vZXFM{KM7:TR?= NX\0dmY4PSCm NELCcJVqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> NWrEZ4VVOjN7MUi3PVc>
EFM192A MlGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rUN|M{KM7:TR?= M4TYcVUh\A>? NUjrbXhRcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> MnPzNlM6OTh5OUe=
AU565 NFrqZWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PaPVM{KM7:TR?= NVe4XoF6PSCm M2PGbYlvcGmkaYTzJFI397zHIHPlcIwh\3Kxd4To NGHuT5AzOzlzOEe5Oy=>
MDA361 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\hdFI{OyEQvF2= MW[1JIQ> NIG1WVZqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> M3nQdFI{QTF6N{m3
BT474 M1q1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXCN|Mh|ryP MWq1JIQ> NH\KOmtqdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> M2X4SlI{QTF6N{m3
HCC202 NX76bmFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTnR3U{OyEQvF2= NH3yPYY2KGR? M3nrRYlvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To NV;XOpZGOjN7MUi3PVc>
KPL4 NVrrfGd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjzT2w{OyEQvF2= NFXmNJo2KGR? NWfNXmN2cW6qaXLpeJMhPTkxvJWgZ4VtdCCpcn;3eIg> Mn3NNlM6OTh5OUe=
NCL-N87 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LFVVM{KM7:TR?= NGPpTVk2KGR? MojZbY5pcWKrdIOgN|HwxIViY3XscEBoem:5dHi= NFr2NmozOzlzOEe5Oy=>
UACC812 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfBN|Mh|ryP MUC1JIQ> MlHPbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= MY[yN|kyQDd7Nx?=
HCC2218 NHXldJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDYfZR3OzNizszN MlTWOUBl MljUbY5pcWKrdIOgNVXwxIViY3XscEBoem:5dHi= M2LUPFI{QTF6N{m3
HCC1569 NEjhbopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH2NYxVOzNizszN M1TwZlUh\A>? MnXobY5pcWKrdIOgOg+9jSClZXzsJIdzd3e2aB?= M{jtS|I{QTF6N{m3
OE19 NWDzW4JHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfOW3Q{OyEQvF2= NFrLSZU2KGR? NFL3e3dqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> MoPtNlM6OTh5OUe=
OE33 M{DkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6zN{DPxE1? M1ToeVUh\A>? NFjkT4dqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> MnO3NlM6OTh5OUe=
JIMT1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnDN|Mh|ryP M17WOVUh\A>? NXy4XW86cW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=> NGXxZY8zOzlzOEe5Oy=>
HCC1954 NVXTW4NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfsUIlHOzNizszN M{PBR|Uh\A>? NGrmZplqdmirYnn0d{AzQe,:hTDj[YxtKGe{b4f0bC=> MXeyN|kyQDd7Nx?=
NUGC4 M2XOXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjYRZE{OyEQvF2= MV61JIQ> MlX5bY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= NWPWUYdiOjN7MUi3PVc>
ZR-75-30 NF3FTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj5UHVQOzNizszN NH;jVXA2KGR? M2PhbolvcGmkaYTzJE0yPe,:hTDj[YxtKGe{b4f0bC=> MYqyN|kyQDd7Nx?=

... 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)
Water Insoluble
Ethanol '2 mg/mL
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
CalculateReset

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
    Concentration
    Volume
    Molecular Weight

*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
NCT04524000 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis October 1 2020 Phase 2
NCT04526470 Not yet recruiting Drug: Alpelisib + Paclitaxel Solid Tumor|Stomach Cancer Seoul National University Bundang Hospital September 1 2020 Phase 1|Phase 2
NCT04300790 Not yet recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis June 30 2020 Phase 2
NCT04251533 Recruiting Drug: alpelisib|Drug: placebo|Drug: nab-paclitaxel Triple Negative Breast Neoplasms Novartis Pharmaceuticals|Novartis June 8 2020 Phase 3

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

Tags: buy Alpelisib (BYL719) | Alpelisib (BYL719) supplier | purchase Alpelisib (BYL719) | Alpelisib (BYL719) cost | Alpelisib (BYL719) manufacturer | order Alpelisib (BYL719) | Alpelisib (BYL719) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID