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, 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.
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 M1zwPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFuxUYQxNjFvMUCwJO69VQ>? M3nkXVczKGh? MUPJR|UxRTFwMUCg{txO MlLGNlU2PTB3NEm=
SNU-1076 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnHOnA1OC5zLUGwNEDPxE1? M3rPZVczKGh? Mn;kTWM2OD14LkiyJO69VQ>? NYXCepNuOjV3NUC1OFk>
SNU-1066 Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XaO|AvOS1zMECg{txO NF\oVGE4OiCq NXzKOYdSUUN3ME2xMlE{KM7:TR?= MYGyOVU2ODV2OR?=
SNU1041 MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXT2do06OC5zLUGwNEDPxE1? NWj2NGZ1PzJiaB?= M3;VW2lEPTB;MkCuOlUh|ryP MUeyOVU2ODV2OR?=
QGP-1 NGXacXdHfW6ldHnvckBCe3OjeR?= MkiyNU8yOCEQvF2= MmnoOEBp NUnLe2lxcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= Mn\NNlUxOjZ{OUK=
MG-63 M2Cwc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETnVGZKSzVyPU[g{txO97zOIFnDPVA:OjRizszN NWnV[5lOOjR7NkG3PVA>
HOS MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i5VGlEPTB;MUWg{txO97zOIFnDPVA:PDJizszN NH;iboMzPDl4MUe5NC=>
POS-1 NWW5clY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRThizszN89yNKEmFOUC9N|Yh|ryP MmnXNlQ6PjF5OUC=
92.1 M13B[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW5OVAxNTJyMECgcm0> NVv6NYxmPSCm MnPTbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NI\HXJkzPDV4M{W0NC=>
Mel270 NEWzPHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TOWFUxOC1{MECwJI5O NFn2fm42KGR? NIj0S5RqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NWH0bmJKOjR3NkO1OFA>
Omm1.3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILRRYI2ODBvMkCwNEBvVQ>? NX3Uem5oPSCm NGrabINqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M3LvclI1PTZ|NUSw
Omm1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r2XVUxOC1{MECwJI5O NGrCR2U2KGR? MULpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MmjsNlQ2PjN3NEC=
C918 M{fNbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrSWVE2ODBvMkCwNEBvVQ>? M3P1OVUh\A>? NHLOfYFqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NF7WR4szPDV4M{W0NC=>
Mel290 M1XSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rmS|UxOC1{MECwJI5O NYDZ[lVqPSCm MoHLbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> M{fNbVI1PTZ|NUSw
OPM2 NIju[mZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWwMlUuOi53IN88US=> MYq0PEBp NILFbIZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHzQSJUzPDRyNUGyNS=>
OPM1 NEnUR3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPLdHNlOC53LUKuOUDPxE1? M{nUTlQ5KGh? NWrSdGNLcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M{LDelI1PDB3MUKx
U266 NELkcohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDNfo94OC53LUKuOUDPxE1? MUi0PEBp NETK[GlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn\DNlQ1ODVzMkG=
MM1R NIKzOoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:wMlUuOi53IN88US=> NHzhNVA1QCCq MonkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVOyOFQxPTF{MR?=
MM1S MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID5e4ExNjVvMj61JO69VQ>? M{HDRVQ5KGh? NUnCV3lFcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGLQbYkzPDRyNUGyNS=>
H929 NHnL[I5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3flR|AvPS1{LkWg{txO MX60PEBp Mn\lbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGC1d|QzPDRyNUGyNS=>
RPMI M3LCSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[4bXoxNjVvMj61JO69VQ>? M1ziclQ5KGh? M3XweolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVGyOFQxPTF{MR?=
SKBR3 NEf1SG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\vRlM{KM7:TR?= NF2yRYE2KGR? M4fybolvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To NVL4[5NLOjN7MUi3PVc>
MDA453 MmPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPCRm1nOzNizszN NGnPe4k2KGR? NF2wepVqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> M17lPVI{QTF6N{m3
EFM192A MoDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTuN|Mh|ryP NXzFeJBUPSCm Mn;3bY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= MmfwNlM6OTh5OUe=
AU565 MnfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PRUVM{KM7:TR?= MV21JIQ> NVP3eph4cW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg> MVqyN|kyQDd7Nx?=
MDA361 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrLN|k{OyEQvF2= MYC1JIQ> NFK4cpJqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> MmLoNlM6OTh5OUe=
BT474 NV\WXnhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzDbWs{OyEQvF2= NX;Eb2J6PSCm M3TRbolvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To NGfseoEzOzlzOEe5Oy=>
HCC202 NF3nUXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjiXYx2OzNizszN MXu1JIQ> Ml7FbY5pcWKrdIOgNlDwxIViY3XscEBoem:5dHi= MkTtNlM6OTh5OUe=
KPL4 MlvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnmN|Mh|ryP M33INFUh\A>? NFfBO4pqdmirYnn0d{A2QO,:hTDj[YxtKGe{b4f0bC=> NUHSb3dFOjN7MUi3PVc>
NCL-N87 MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnv5N|Mh|ryP MX:1JIQ> NXPn[|N3cW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> NE[zZ2ozOzlzOEe5Oy=>
UACC812 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jINFM{KM7:TR?= NVz6eIk4PSCm NUXFbotqcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> NFmzOIYzOzlzOEe5Oy=>
HCC2218 NUnpcmxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDjbpk{OyEQvF2= MUC1JIQ> NUjkcHRncW6qaXLpeJMhOTYxvJWgZ4VtdCCpcn;3eIg> Mli3NlM6OTh5OUe=
HCC1569 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonnN|Mh|ryP NIP6Wo42KGR? NIeyfHNqdmirYnn0d{A297zHIHPlcIwh\3Kxd4To M2n3d|I{QTF6N{m3
OE19 M1PSbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSzN{DPxE1? NHPPZVY2KGR? MXHpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NYjQRmVyOjN7MUi3PVc>
OE33 NF\CW|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOzN{DPxE1? M{nXW|Uh\A>? M1X4UYlvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To MU[yN|kyQDd7Nx?=
JIMT1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO4NI9yOzNizszN MU[1JIQ> MYrpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq MWiyN|kyQDd7Nx?=
HCC1954 Mlm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj1N|Mh|ryP NU\HU2U3PSCm NIHSVVhqdmirYnn0d{AzQe,:hTDj[YxtKGe{b4f0bC=> MmfoNlM6OTh5OUe=
NUGC4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PVN|M{KM7:TR?= M2[0eVUh\A>? MWLpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= NVPmcFMyOjN7MUi3PVc>
ZR-75-30 NXiyNVJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmzN{DPxE1? NILpclE2KGR? MkTPbY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To NXrwbHAyOjN7MUi3PVc>

... 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]


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:
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


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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID