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 MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkS2NE4yNTFyMDFOwG0> M{fmR|czKGh? M4jlV2lEPTB;MT6xNEDPxE1? MkfHNlU2PTB3NEm=
SNU-1076 NFP2NoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMlEuOTByIN88US=> Ml\PO|IhcA>? MnjNTWM2OD14LkiyJO69VQ>? M4O3d|I2PTVyNUS5
SNU-1066 NF6wcm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\jVZBOOC5zLUGwNEDPxE1? M17xPVczKGh? M1\SeGlEPTB;MT6xN{DPxE1? MUiyOVU2ODV2OR?=
FaDu MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;HZoZrOC5zLUGwNEDPxE1? NGnzZ|c4OiCq NYHoS3ZwUUN3ME2xPU43PiEQvF2= NWrVVVFQOjV3NUC1OFk>
SNU1041 M2nqVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T6flAvOS1zMECg{txO MoLHO|IhcA>? M{TuNmlEPTB;MkCuOlUh|ryP NH;MT|IzPTV3MEW0PS=>
SCC25 M1TvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOwMlEuOTByIN88US=> Mn72O|IhcA>? NX7OT3kyUUN3ME20PU4{OCEQvF2= NHPWcWEzPTV3MEW0PS=>
BON-1 MnPESpVv[3Srb36gRZN{[Xl? NXnmNJU4OS9zMDFOwG0> M3HwZ|QhcA>? NIKwRZlqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= MX[yOVAzPjJ7Mh?=
QGP-1 NV7ZUpNsTnWwY4Tpc44hSXO|YYm= MnfvNU8yOCEQvF2= MWS0JIg> NUn0OIFucW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= MlLVNlUxOjZ{OUK=
MG-63 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrCTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= NGm4cmQzPDl4MUe5NC=>
HOS NEOxUmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHYTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= MUGyOFk3OTd7MB?=
MOS-J M{Dldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= MX:yOFk3OTd7MB?=
POS-1 Mm\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvTTWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?= M{GwUlI1QTZzN{mw
92.1 MoXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu5OVAxNTJyMECgcm0> NXjicHVVPSCm NV;Wco5ocW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NF\KNo8zPDV4M{W0NC=>
Mel270 NF7JZYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2njW|UxOC1{MECwJI5O MYW1JIQ> M2HqU4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO Mn6xNlQ2PjN3NEC=
Omm1.3 M{DxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfEOVAxNTJyMECgcm0> MVm1JIQ> Ml;4bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MlHHNlQ2PjN3NEC=
Omm1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYG1NFAuOjByMDDuUS=> NXzrO4F5PSCm MnXkbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MVyyOFU3OzV2MB?=
C918 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzaZ4g2PTByLUKwNFAhdk1? MlHiOUBl NVjGRXVmcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NXf3dncyOjR3NkO1OFA>
Mel290 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXZToNoPTByLUKwNFAhdk1? M4rudVUh\A>? M1XRZYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NWLQcnZ7OjR3NkO1OFA>
OPM2 MkTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T6NVAvPS1{LkWg{txO M{jWNFQ5KGh? NHnBSJVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWLvWYFtOjR2MEWxNlE>
OPM1 Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjkO5NvOC53LUKuOUDPxE1? MVu0PEBp M1ToZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{LUVlI1PDB3MUKx
U266 M4XqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv3Z2MxNjVvMj61JO69VQ>? NYrVPIJUPDhiaB?= NX\KNINucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1Lt[|I1PDB3MUKx
MM1R Mn64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXnbIQxNjVvMj61JO69VQ>? M4fvZVQ5KGh? MV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYPwdFhNOjR2MEWxNlE>
MM1S NIPicYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jCWVAvPS1{LkWg{txO Mn\QOFghcA>? Mm\xbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MorINlQ1ODVzMkG=
H929 NXLMZ|U3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL4NE42NTJwNTFOwG0> NILWTmU1QCCq MkXqbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUiyOFQxPTF{MR?=
RPMI NEGx[IdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHJNE42NTJwNTFOwG0> NUjqWlV5PDhiaB?= NU\ZN3JNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV;EVHNyOjR2MEWxNlE>
SKBR3 NYG0e3ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\DN|Mh|ryP M4q5b|Uh\A>? NGTtd|lqdmirYnn0d{A{Pe,:hTDj[YxtKGe{b4f0bC=> MVWyN|kyQDd7Nx?=
MDA453 MmfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPkN|Mh|ryP M1nHdVUh\A>? MVXpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= M17JZVI{QTF6N{m3
EFM192A MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqzN{DPxE1? NEfFT4k2KGR? MXfpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NHr1VmEzOzlzOEe5Oy=>
AU565 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTKWo8{OyEQvF2= MoCyOUBl Ml7GbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= NEnBVoEzOzlzOEe5Oy=>
MDA361 MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\4N|Mh|ryP MkXPOUBl Mlr2bY5pcWKrdIOgOFTwxIViY3XscEBoem:5dHi= M1r4Z|I{QTF6N{m3
BT474 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfpcJQ{OyEQvF2= M{G5flUh\A>? NUXPTXo4cW6qaXLpeJMhOTcxvJWgZ4VtdCCpcn;3eIg> MoTkNlM6OTh5OUe=
HCC202 NHPUSohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i4dlM{KM7:TR?= M3LwZ|Uh\A>? MYXpcohq[mm2czCyNQ+9jSClZXzsJIdzd3e2aB?= NIfFXHczOzlzOEe5Oy=>
KPL4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TQS|M{KM7:TR?= MWK1JIQ> NXXkfGtncW6qaXLpeJMhPTkxvJWgZ4VtdCCpcn;3eIg> Ml:0NlM6OTh5OUe=
NCL-N87 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjFN|Mh|ryP M3\6fFUh\A>? M3rad4lvcGmkaYTzJFMy97zHIHPlcIwh\3Kxd4To MUOyN|kyQDd7Nx?=
UACC812 NUX0Xm1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKzN{DPxE1? MojoOUBl MWTpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NX7hW4NLOjN7MUi3PVc>
HCC2218 Mn;oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGC0Xos{OyEQvF2= NE\qXGo2KGR? M2DvWolvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To NHjtPFAzOzlzOEe5Oy=>
HCC1569 NXuwZnRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4SwVVM{KM7:TR?= M1z5R|Uh\A>? NXL6S5U1cW6qaXLpeJMhPe,:hTDj[YxtKGe{b4f0bC=> MXOyN|kyQDd7Nx?=
OE19 M{LnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zXNVM{KM7:TR?= Ml;hOUBl MlX3bY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= NX\6eZNpOjN7MUi3PVc>
OE33 NFPQflBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv5Vm45OzNizszN MoPxOUBl M3jzXolvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To M1ntN|I{QTF6N{m3
JIMT1 NXT2TZpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7VRpo{OyEQvF2= MV21JIQ> NHfqbIlqdmirYnn0d{A697zHIHPlcIwh\3Kxd4To Mnz6NlM6OTh5OUe=
HCC1954 NVnkVoJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXDN|Mh|ryP NH\0PXU2KGR? NGf5dm9qdmirYnn0d{AzQe,:hTDj[YxtKGe{b4f0bC=> MVWyN|kyQDd7Nx?=
NUGC4 M{L3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX2zN{DPxE1? NInWSnU2KGR? MoL6bY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= M1\D[FI{QTF6N{m3
ZR-75-30 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUezN{DPxE1? MmrBOUBl NHT3T3dqdmirYnn0d{AuOTYxvJWgZ4VtdCCpcn;3eIg> MorhNlM6OTh5OUe=

... 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

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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