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
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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. 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 M171PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33yZVAvOS1zMECg{txO NUX1fmRrPzJiaB?= NGnsSYZKSzVyPUGuNVAh|ryP MmizNlU2PTB3NEm=
SNU-1076 NI\sVFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjY[WlqOC5zLUGwNEDPxE1? NEPoXIs4OiCq MXHJR|UxRTZwOEKg{txO NITze|IzPTV3MEW0PS=>
SNU-1066 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M376WVAvOS1zMECg{txO M1K3eFczKGh? Mn[5TWM2OD1zLkGzJO69VQ>? NH;RSGQzPTV3MEW0PS=>
FaDu M4\iWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL3WXoxNjFvMUCwJO69VQ>? M4jO[FczKGh? NVzLTWlwUUN3ME2xPU43PiEQvF2= MkHvNlU2PTB3NEm=
SNU1041 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO0N2gxNjFvMUCwJO69VQ>? MofIO|IhcA>? MkL2TWM2OD1{MD62OUDPxE1? NH\r[nIzPTV3MEW0PS=>
SCC25 NW\uNHNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:0WnMxNjFvMUCwJO69VQ>? MXm3NkBp MV7JR|UxRTR7LkOwJO69VQ>? NH3VUWkzPTV3MEW0PS=>
BON-1 NYLrRmRYTnWwY4Tpc44hSXO|YYm= MXqxM|ExKM7:TR?= NXjrcmt3PCCq NFe0e5pqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= M3vvOFI2ODJ4Mkmy
QGP-1 MkjZSpVv[3Srb36gRZN{[Xl? MmT6NU8yOCEQvF2= M3XHXVQhcA>? NFLuclRqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= MYqyOVAzPjJ7Mh?=
MG-63 NELPW4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPOfmhwUUN3ME22JO69Ve,:jDDJR|kxRTJ2IN88US=> NWX2UGlyOjR7NkG3PVA>
HOS MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknvTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= MUWyOFk3OTd7MB?=
MOS-J M1fjc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= NVHGdXJSOjR7NkG3PVA>
POS-1 NI\3PHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrkTWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?= NH;0UGozPDl4MUe5NC=>
92.1 NWrrO3o{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[1NFAuOjByMDDuUS=> NVLRUXBxPSCm MUDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MYSyOFU3OzV2MB?=
Mel270 NUHIb2ZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVm1NFAuOjByMDDuUS=> NV[wVJI3PSCm NWr1dWVtcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NV3Cc4NQOjR3NkO1OFA>
Omm1.3 MoPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjXbJo2ODBvMkCwNEBvVQ>? MnzDOUBl M13RTYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NVrUXXRKOjR3NkO1OFA>
Omm1 NVjxXld{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[4Xox6PTByLUKwNFAhdk1? MVm1JIQ> Mo[0bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> Mn;pNlQ2PjN3NEC=
C918 MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTrXGI2ODBvMkCwNEBvVQ>? MX61JIQ> NYLxTGMzcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MorqNlQ2PjN3NEC=
Mel290 NIDGd4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHieHM2ODBvMkCwNEBvVQ>? MWS1JIQ> MVfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NHvRfYwzPDV4M{W0NC=>
OPM2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j3VVAvPS1{LkWg{txO NIPqO4M1QCCq NXvTXGpOcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3fhOFI1PDB3MUKx
OPM1 NXL3RXVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nM[VAvPS1{LkWg{txO MojpOFghcA>? MWTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGf1WYwzPDRyNUGyNS=>
U266 NUnNUnZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:wMlUuOi53IN88US=> MYG0PEBp NGGyRWxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYDTdZhVOjR2MEWxNlE>
MM1R NXfmNmFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXi0NYFzOC53LUKuOUDPxE1? M{PLWlQ5KGh? NFjIeXRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUfCWHdROjR2MEWxNlE>
MM1S M4jFcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHHSHQxNjVvMj61JO69VQ>? NUfoXGxLPDhiaB?= NX2zOZVCcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHTUUVQzPDRyNUGyNS=>
H929 NEXqTpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PVelAvPS1{LkWg{txO M1S1[VQ5KGh? MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NIf4VlYzPDRyNUGyNS=>
RPMI MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuwMlUuOi53IN88US=> NWDWUG1rPDhiaB?= NFzZN4lqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYLLfYh6OjR2MEWxNlE>
SKBR3 NFjQ[W1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfiN|Mh|ryP M{fCblUh\A>? MVXpcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= NEj2bZIzOzlzOEe5Oy=>
MDA453 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\uTFQ{OyEQvF2= M3fXdFUh\A>? MV3pcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= MnXQNlM6OTh5OUe=
EFM192A NVPDN|A4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j1bVM{KM7:TR?= NXT5[VBiPSCm Mn\jbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= M2HxXFI{QTF6N{m3
AU565 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DJdlM{KM7:TR?= NX61PYduPSCm M1jqfIlvcGmkaYTzJFI397zHIHPlcIwh\3Kxd4To MnjXNlM6OTh5OUe=
MDA361 M1nHU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj6fJE{OyEQvF2= NXvHS|FsPSCm NYPaS2lucW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> MonLNlM6OTh5OUe=
BT474 NFLmU|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLwU2p1OzNizszN M3vtSlUh\A>? MlP6bY5pcWKrdIOgNVbwxIViY3XscEBoem:5dHi= MV[yN|kyQDd7Nx?=
HCC202 MoTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKzN{DPxE1? NY\WVVlHPSCm M1PrTYlvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To MWWyN|kyQDd7Nx?=
KPL4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWzN{DPxE1? MljzOUBl M4iyNIlvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To M3HiVFI{QTF6N{m3
NCL-N87 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfGfXc{OyEQvF2= M3XDNlUh\A>? NXr5XGo3cW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> MkLlNlM6OTh5OUe=
UACC812 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLX[2ZxOzNizszN NGflcIw2KGR? NULkfHNWcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> NFvz[2kzOzlzOEe5Oy=>
HCC2218 NYH0SWtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nRe|M{KM7:TR?= MX61JIQ> NX[0VINrcW6qaXLpeJMhOTYxvJWgZ4VtdCCpcn;3eIg> NHP3OWEzOzlzOEe5Oy=>
HCC1569 MkDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rr[FM{KM7:TR?= MUG1JIQ> NGjIOXVqdmirYnn0d{A297zHIHPlcIwh\3Kxd4To MXWyN|kyQDd7Nx?=
OE19 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzwW3g{OyEQvF2= NVTJco82PSCm MmHvbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= MlXRNlM6OTh5OUe=
OE33 NEH3TopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnSN|Mh|ryP NF;wVW82KGR? MVPpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= MUSyN|kyQDd7Nx?=
JIMT1 NF\LU2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Hrc|M{KM7:TR?= M{m1flUh\A>? NWfHSVlqcW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=> M2X1dVI{QTF6N{m3
HCC1954 M{TsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzVUY8{OyEQvF2= MVW1JIQ> NY\xPVNUcW6qaXLpeJMhOjoxvJWgZ4VtdCCpcn;3eIg> NUjUcnU1OjN7MUi3PVc>
NUGC4 NILndJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Pkb|M{KM7:TR?= MYS1JIQ> M3HKWYlvcGmkaYTzJFE197zHIHPlcIwh\3Kxd4To MVqyN|kyQDd7Nx?=
ZR-75-30 M1Prfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;0cFM{KM7:TR?= M2P2TFUh\A>? Ml6ybY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To MlXpNlM6OTh5OUe=

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
Synonyms N/A

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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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID