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
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Cited by 9 Publications

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 MnfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXJNE4yNTFyMDFOwG0> NHP5fnc4OiCq M3PZRWlEPTB;MT6xNEDPxE1? M4nweFI2PTVyNUS5
SNU-1076 NWLNUoZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13sVFAvOS1zMECg{txO M360ZlczKGh? NGrKdYFKSzVyPU[uPFIh|ryP MmXJNlU2PTB3NEm=
SNU-1066 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvFNE4yNTFyMDFOwG0> NHrkc2w4OiCq NXWzT5h5UUN3ME2xMlE{KM7:TR?= M2nj[FI2PTVyNUS5
FaDu NIPtZZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PCbVAvOS1zMECg{txO NXixNJQ4PzJiaB?= M2jv[WlEPTB;MUmuOlYh|ryP MYOyOVU2ODV2OR?=
SNU1041 NWO3UolwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD3d5BOOC5zLUGwNEDPxE1? NE\TV2w4OiCq MlzVTWM2OD1{MD62OUDPxE1? MX2yOVU2ODV2OR?=
SCC25 NITZ[ZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDESVFHOC5zLUGwNEDPxE1? MWi3NkBp MXHJR|UxRTR7LkOwJO69VQ>? MXOyOVU2ODV2OR?=
BON-1 Ml;mSpVv[3Srb36gRZN{[Xl? NHzCTlQyNzFyIN88US=> MmnIOEBp NYnD[moycW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= NI\3bVIzPTB{NkK5Ni=>
QGP-1 M4KyUWZ2dmO2aX;uJGF{e2G7 Mn;PNU8yOCEQvF2= MlrHOEBp M2HBXolvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| M{O5W|I2ODJ4Mkmy
MG-63 MofBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLWTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= MUKyOFk3OTd7MB?=
HOS MlfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPuSm83UUN3ME2xOUDPxE4xvJygTWM6OD12MjFOwG0> MYqyOFk3OTd7MB?=
MOS-J NUDyVnBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWS0NnZIUUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> M1TYSVI1QTZzN{mw
POS-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnyTWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?= MWSyOFk3OTd7MB?=
92.1 M2P3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDKOVAxNTJyMECgcm0> M33ReVUh\A>? M13BbolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NX;CXIFLOjR3NkO1OFA>
Mel270 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYm1NFAuOjByMDDuUS=> MUm1JIQ> NUXyc4hYcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NUjkNHdnOjR3NkO1OFA>
Omm1.3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWm1NFAuOjByMDDuUS=> NHP2OHU2KGR? MYTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NH23NWUzPDV4M{W0NC=>
Omm1 NHqzcnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LGRVUxOC1{MECwJI5O MlPXOUBl NFX1XIJqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NF\JbWMzPDV4M{W0NC=>
C918 NHvxPIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3rOVAxNTJyMECgcm0> NXzwWnJ6PSCm MkLybY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MWKyOFU3OzV2MB?=
Mel290 NVXzNpZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvHOVAxNTJyMECgcm0> M1u5SVUh\A>? M3PkR4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MWGyOFU3OzV2MB?=
OPM2 NGHzTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXtNE42NTJwNTFOwG0> NFfhSIU1QCCq NH;McWlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4j5TFI1PDB3MUKx
OPM1 NYTsVXhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfOb|QxNjVvMj61JO69VQ>? MXK0PEBp NE[xXHBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVOyOFQxPTF{MR?=
U266 M4j4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnOVYJSOC53LUKuOUDPxE1? MY[0PEBp M2LqXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnHxNlQ1ODVzMkG=
MM1R MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHKPZQxNjVvMj61JO69VQ>? M4izWFQ5KGh? MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2rMS|I1PDB3MUKx
MM1S M3LLTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2OwPVAvPS1{LkWg{txO M2nnblQ5KGh? NV3FTZc{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIq3b40zPDRyNUGyNS=>
H929 MoPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLMXYNSOC53LUKuOUDPxE1? NWLBd2s3PDhiaB?= NW\HfnVucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVy1ZotUOjR2MEWxNlE>
RPMI M{TOb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfycGRiOC53LUKuOUDPxE1? NX3xfWU6PDhiaB?= NUC2No9wcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVrLOVFDOjR2MEWxNlE>
SKBR3 NUfEbYY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPRTZg{OyEQvF2= NHzN[nU2KGR? MoTqbY5pcWKrdIOgN|XwxIViY3XscEBoem:5dHi= MXGyN|kyQDd7Nx?=
MDA453 MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO5foU{OyEQvF2= M{jIflUh\A>? MYXpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= NX\4b4R3OjN7MUi3PVc>
EFM192A NWm4UnFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGzN{DPxE1? MlT6OUBl NYjpeIlCcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> NEHIXpgzOzlzOEe5Oy=>
AU565 NWHzN5RMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPnN4ZsOzNizszN MV:1JIQ> MmHJbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= NFzweFMzOzlzOEe5Oy=>
MDA361 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nhXFM{KM7:TR?= Mmi4OUBl M1S0fYlvcGmkaYTzJFQ197zHIHPlcIwh\3Kxd4To NF\DeWEzOzlzOEe5Oy=>
BT474 NWm1W21CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTKdXJTOzNizszN MmXoOUBl MlTObY5pcWKrdIOgNVbwxIViY3XscEBoem:5dHi= MXWyN|kyQDd7Nx?=
HCC202 NEHaOVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;pN|Mh|ryP MlT3OUBl NI\meYRqdmirYnn0d{AzOO,:hTDj[YxtKGe{b4f0bC=> NGD2[HEzOzlzOEe5Oy=>
KPL4 NF2wWZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\KN|Mh|ryP MnzCOUBl NUfnPIhlcW6qaXLpeJMhPTkxvJWgZ4VtdCCpcn;3eIg> NEXDWWIzOzlzOEe5Oy=>
NCL-N87 M4ThWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4e1UlM{KM7:TR?= NUXU[|JJPSCm NUj1RWxpcW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> NYPKSXBOOjN7MUi3PVc>
UACC812 M4fySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS2N|Mh|ryP NETZUYg2KGR? MmnjbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= MkHrNlM6OTh5OUe=
HCC2218 NWDsO4gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOzN{DPxE1? NXjCOIoyPSCm NFP0PHRqdmirYnn0d{AyPe,:hTDj[YxtKGe{b4f0bC=> MmnQNlM6OTh5OUe=
HCC1569 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjMR5I{OyEQvF2= NXnwN3JbPSCm M4HsUYlvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= NE\DU24zOzlzOEe5Oy=>
OE19 M1rxSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfPe5A{OyEQvF2= NY\ON3ZEPSCm NHG3e3NqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> M1PmelI{QTF6N{m3
OE33 NIiyeJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUCyPHg5OzNizszN MV61JIQ> NWGyZlVzcW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> NH7zd3YzOzlzOEe5Oy=>
JIMT1 NVPkUllwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonCN|Mh|ryP NEO5eVA2KGR? MnjzbY5pcWKrdIOgPg+9jSClZXzsJIdzd3e2aB?= NW[yPXE{OjN7MUi3PVc>
HCC1954 M{HlWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjyU|U{OyEQvF2= M3nn[|Uh\A>? MYLpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= NXjKeHRLOjN7MUi3PVc>
NUGC4 M4riZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmzN{DPxE1? NVnvXpFkPSCm M{XUTolvcGmkaYTzJFE197zHIHPlcIwh\3Kxd4To MXeyN|kyQDd7Nx?=
ZR-75-30 NGDqT|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mne1N|Mh|ryP M{LoOlUh\A>? NVjzcoN3cW6qaXLpeJMhNTF378{FJINmdGxiZ4Lve5Rp Mmf3NlM6OTh5OUe=

... 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
NCT03207529 Not yet recruiting Malignant Neoplasm of Breast M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc. March 31 2019 Phase 1
NCT03207529 Not yet recruiting Malignant Neoplasm of Breast M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc. March 31 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03601507 Recruiting CDKN2A-p16 Positive|Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 University of Arizona|National Cancer Institute (NCI) December 14 2018 Phase 2
NCT03601507 Recruiting CDKN2A-p16 Positive|Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 University of Arizona|National Cancer Institute (NCI) December 14 2018 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