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

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

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

Choose Selective PI3K Inhibitors

Click to view more

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 NYDZOHFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf3NE4yNTFyMDFOwG0> M3Tk[lczKGh? MUDJR|UxRTFwMUCg{txO MkGwNlU2PTB3NEm=
SNU-1076 NW\0WFJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmSyNE4yNTFyMDFOwG0> NIHxXIU4OiCq M37WS2lEPTB;Nj64NkDPxE1? MYCyOVU2ODV2OR?=
SNU-1066 M2LZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWiwMlEuOTByIN88US=> NIXOb3A4OiCq MYnJR|UxRTFwMUOg{txO MV[yOVU2ODV2OR?=
FaDu MofCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGwMlEuOTByIN88US=> MXm3NkBp MU\JR|UxRTF7Lk[2JO69VQ>? M13jflI2PTVyNUS5
SNU1041 NFfjSWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zhSVAvOS1zMECg{txO M1XwO|czKGh? NX63bJA1UUN3ME2yNE43PSEQvF2= NXn1PJQ3OjV3NUC1OFk>
SCC25 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXPXYFPOC5zLUGwNEDPxE1? NW\JeHpZPzJiaB?= NGTZblBKSzVyPUS5MlMxKM7:TR?= NEj5XHozPTV3MEW0PS=>
BON-1 NYP5XHg5TnWwY4Tpc44hSXO|YYm= MVSxM|ExKM7:TR?= Mk\QOEBp M4XnfolvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| NHXCUZUzPTB{NkK5Ni=>
QGP-1 NEX2RVZHfW6ldHnvckBCe3OjeR?= NV\Uc4txOS9zMDFOwG0> MV60JIg> NWfod4p5cW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= NH;6SlIzPTB{NkK5Ni=>
MG-63 NV\wcGFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\mR3ZKSzVyPU[g{txO97zOIFnDPVA:OjRizszN NVzUb4dROjR7NkG3PVA>
HOS MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF3IN88Ug+9lCCLQ{mwQVQzKM7:TR?= NF3KepQzPDl4MUe5NC=>
MOS-J MnvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jEcWlEPTB;MUCg{txO97zOIFnDPVA:OzZizszN NHzSO|AzPDl4MUe5NC=>
POS-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRThizszN89yNKEmFOUC9N|Yh|ryP MVeyOFk3OTd7MB?=
92.1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnZdJNiPTByLUKwNFAhdk1? NHrlWoM2KGR? NVXNVFdncW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M4nL[|I1PTZ|NUSw
Mel270 NVzHN2dsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDpWHA2ODBvMkCwNEBvVQ>? NF\nWpc2KGR? NUjFTmNvcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MmfSNlQ2PjN3NEC=
Omm1.3 NVPQelNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH3XZM2ODBvMkCwNEBvVQ>? M37BblUh\A>? MmTBbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MViyOFU3OzV2MB?=
Omm1 NXjDclhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTlOVAxNTJyMECgcm0> M2TLZlUh\A>? NIHIcoVqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NV;5doFLOjR3NkO1OFA>
C918 Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;wRXc2ODBvMkCwNEBvVQ>? NXn2TJZjPSCm Mn[5bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MkPJNlQ2PjN3NEC=
Mel290 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXDcW1tPTByLUKwNFAhdk1? NFXXZ3I2KGR? NHjZNZdqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M1TxRVI1PTZ|NUSw
OPM2 NHnhPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zRZlAvPS1{LkWg{txO MkjPOFghcA>? NH3ZcYpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUWyOFQxPTF{MR?=
OPM1 M17LTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[wMlUuOi53IN88US=> NVHLWplyPDhiaB?= MlfwbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXi4WmdCOjR2MEWxNlE>
U266 Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV2wMlUuOi53IN88US=> MV20PEBp M4\XeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlzKNlQ1ODVzMkG=
MM1R NXv0PJliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:0NE42NTJwNTFOwG0> NFnUV3c1QCCq NHPaU5ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVyyOFQxPTF{MR?=
MM1S NFy1[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnGNE42NTJwNTFOwG0> NGHHd2c1QCCq NHPQeGhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFrwfG0zPDRyNUGyNS=>
H929 MlewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XzcVAvPS1{LkWg{txO MUC0PEBp M{DiPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NInNO4QzPDRyNUGyNS=>
RPMI MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDNNE42NTJwNTFOwG0> MorpOFghcA>? NULPPGw5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MVSyOFQxPTF{MR?=
SKBR3 M3rMWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\ESFdXOzNizszN M1H3RlUh\A>? MnvibY5pcWKrdIOgN|XwxIViY3XscEBoem:5dHi= MmHLNlM6OTh5OUe=
MDA453 NGmzeGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3obGU{OyEQvF2= MYe1JIQ> NYizcopocW6qaXLpeJMhOzkxvJWgZ4VtdCCpcn;3eIg> M1LIU|I{QTF6N{m3
EFM192A NYjCRnlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonEN|Mh|ryP NUTVOVZUPSCm NHS4UYxqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> MVKyN|kyQDd7Nx?=
AU565 MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTaXotUOzNizszN MnvSOUBl MVLpcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?= M3PIW|I{QTF6N{m3
MDA361 NWrCOmQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPqN|Mh|ryP Mki2OUBl NF\rSJJqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> NVXBR44{OjN7MUi3PVc>
BT474 NGHuR5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjMZnc{OyEQvF2= NHKwZnU2KGR? MkWybY5pcWKrdIOgNVbwxIViY3XscEBoem:5dHi= M1LZe|I{QTF6N{m3
HCC202 NF;JPHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;HS2g{OyEQvF2= M3XjSlUh\A>? NWqxcXM6cW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> NF3EXYMzOzlzOEe5Oy=>
KPL4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUezN{DPxE1? M1L6ZlUh\A>? NVmyTo81cW6qaXLpeJMhPTkxvJWgZ4VtdCCpcn;3eIg> NXXtUoloOjN7MUi3PVc>
NCL-N87 NGnURpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2f5eFM{KM7:TR?= M4jUNFUh\A>? MlLmbY5pcWKrdIOgN|HwxIViY3XscEBoem:5dHi= NH7hO4kzOzlzOEe5Oy=>
UACC812 Mkn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHON|Mh|ryP NGTGd2Y2KGR? NIqwTGhqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> M1HDOVI{QTF6N{m3
HCC2218 NY\rNIZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGzN{DPxE1? NF3Wc2E2KGR? MV;pcohq[mm2czCxOg+9jSClZXzsJIdzd3e2aB?= MkTNNlM6OTh5OUe=
HCC1569 Mo\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KzRlM{KM7:TR?= MkK2OUBl M3rydolvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= NXrjUVZ5OjN7MUi3PVc>
OE19 Ml72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnjfpl5OzNizszN M1jrOVUh\A>? MYHpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NH3nOo4zOzlzOEe5Oy=>
OE33 NH3SXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPtT2hjOzNizszN M4fyTlUh\A>? MnXxbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= MV6yN|kyQDd7Nx?=
JIMT1 M2frR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfkNmo{OyEQvF2= NHT5XI02KGR? NYfRNlhpcW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=> MnfONlM6OTh5OUe=
HCC1954 NHK0VZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLHUXk{OyEQvF2= NWHhbo5EPSCm NY[xXVU1cW6qaXLpeJMhOjoxvJWgZ4VtdCCpcn;3eIg> MnHmNlM6OTh5OUe=
NUGC4 NIT6U|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[5UFM{KM7:TR?= MXS1JIQ> MYnpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= NV\OZ3l3OjN7MUi3PVc>
ZR-75-30 MlPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjBSVlmOzNizszN MmXQOUBl NV\2XHpIcW6qaXLpeJMhNTF378{FJINmdGxiZ4Lve5Rp M4fISlI{QTF6N{m3

... 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

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 (g) = Concentration (mol/L) × Volume (L) × 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 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.

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