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.

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In DMSO USD 592 In stock
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Cited by 40 Publications

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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 NEO1VXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWX1bZJFOC5zLUGwNEDPxE1? MYm3NkBp NUPMS4ROUUN3ME2xMlExKM7:TR?= NUjoOo9YOjV3NUC1OFk>
SNU-1076 M2PsRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWiwMlEuOTByIN88US=> Mor5O|IhcA>? Mkm3TWM2OD14LkiyJO69VQ>? NWTaV4ZYOjV3NUC1OFk>
SNU-1066 NUHoeGVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLqbVMzOC5zLUGwNEDPxE1? NFfNTHA4OiCq NYWwOpN5UUN3ME2xMlE{KM7:TR?= MlzCNlU2PTB3NEm=
FaDu MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXVNE4yNTFyMDFOwG0> MXK3NkBp MXjJR|UxRTF7Lk[2JO69VQ>? NFrtdIczPTV3MEW0PS=>
SNU1041 NIXseYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LaNlAvOS1zMECg{txO MnjLO|IhcA>? MlPrTWM2OD1{MD62OUDPxE1? NXOwOVFZOjV3NUC1OFk>
SCC25 NIXITIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPzd5ZDOC5zLUGwNEDPxE1? NIrNVmk4OiCq MUPJR|UxRTR7LkOwJO69VQ>? NWnsfJE{OjV3NUC1OFk>
BON-1 NVzsc2poTnWwY4Tpc44hSXO|YYm= NILZc4wyNzFyIN88US=> M1vwXVQhcA>? NIj3[olqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NHzXSZAzPTB{NkK5Ni=>
QGP-1 MnXFSpVv[3Srb36gRZN{[Xl? M4D4PVEwOTBizszN MonnOEBp MknjbY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? MWKyOVAzPjJ7Mh?=
MG-63 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTZizszN89yNKEmFOUC9NlQh|ryP MUeyOFk3OTd7MB?=
HOS MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LOcGlEPTB;MUWg{txO97zOIFnDPVA:PDJizszN NH\YR5YzPDl4MUe5NC=>
MOS-J MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXjWYZiUUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> NILRdlczPDl4MUe5NC=>
POS-1 NXLLfXR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlm3TWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?= MXyyOFk3OTd7MB?=
92.1 M3TCdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHThSpQ2ODBvMkCwNEBvVQ>? MUm1JIQ> MU\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NI\UZWczPDV4M{W0NC=>
Mel270 NV3YeFVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3iOVAxNTJyMECgcm0> MlLYOUBl MX7pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> M1XTTFI1PTZ|NUSw
Omm1.3 NFrFZ4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXlcWNEPTByLUKwNFAhdk1? MnHoOUBl NYO5cZRrcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M4rKV|I1PTZ|NUSw
Omm1 NVqw[oEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPLcG42ODBvMkCwNEBvVQ>? MnG3OUBl MUTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MXOyOFU3OzV2MB?=
C918 M3PIRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7mOVAxNTJyMECgcm0> NIfpfZo2KGR? NVzEO2ljcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NWr5U5o3OjR3NkO1OFA>
Mel290 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYX6ZWhIPTByLUKwNFAhdk1? M{jGVFUh\A>? NGq1SYVqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MlzINlQ2PjN3NEC=
OPM2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[wMlUuOi53IN88US=> MVS0PEBp MlvhbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXnJOW1xOjR2MEWxNlE>
OPM1 NEjudWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LZUlAvPS1{LkWg{txO MojpOFghcA>? NUTUVoRScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWSyOFQxPTF{MR?=
U266 M{D6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUmxdHd2OC53LUKuOUDPxE1? MlLKOFghcA>? M2n5eYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3;INVI1PDB3MUKx
MM1R MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;uc|AvPS1{LkWg{txO MYG0PEBp NUH4UZF1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NI\pRpUzPDRyNUGyNS=>
MM1S NVXaOnNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETWU4UxNjVvMj61JO69VQ>? MX[0PEBp MoXrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVXrc4o2OjR2MEWxNlE>
H929 M{W5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\XTlJUOC53LUKuOUDPxE1? MV20PEBp NILJc2FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmnENlQ1ODVzMkG=
RPMI MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf3TWV1OC53LUKuOUDPxE1? MXy0PEBp M2rnfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYK4[lRGOjR2MEWxNlE>
SKBR3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXizN{DPxE1? MXm1JIQ> MXPpcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= MknrNlM6OTh5OUe=
MDA453 NGe4clFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrvUGVGOzNizszN NVLTOYxsPSCm M4j0XIlvcGmkaYTzJFM597zHIHPlcIwh\3Kxd4To NVPvZ4M1OjN7MUi3PVc>
EFM192A NVf6XVZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\adYh3OzNizszN MUe1JIQ> MULpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= Mkj1NlM6OTh5OUe=
AU565 NVPYRll6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjiZoY{OyEQvF2= MXq1JIQ> MnXHbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= NYW4fYx4OjN7MUi3PVc>
MDA361 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37HU|M{KM7:TR?= M3\xSlUh\A>? MWrpcohq[mm2czC0OQ+9jSClZXzsJIdzd3e2aB?= MWCyN|kyQDd7Nx?=
BT474 NVjaS3ZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{H3W|M{KM7:TR?= MXm1JIQ> M3PoXYlvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To MVKyN|kyQDd7Nx?=
HCC202 M2K5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rPeFM{KM7:TR?= MXW1JIQ> NVm4OXpEcW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> Mkj5NlM6OTh5OUe=
KPL4 M3;Oc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq4N|Mh|ryP MmPsOUBl MVPpcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= NHLEd4szOzlzOEe5Oy=>
NCL-N87 M1PVPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonTN|Mh|ryP NFLZb5A2KGR? NFPCVY5qdmirYnn0d{A{Oe,:hTDj[YxtKGe{b4f0bC=> MnT1NlM6OTh5OUe=
UACC812 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TCXFM{KM7:TR?= M2i4e|Uh\A>? MXnpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= M4DU[VI{QTF6N{m3
HCC2218 NXzuVZlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XPfVM{KM7:TR?= MYm1JIQ> M4f6NIlvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To M4G3NVI{QTF6N{m3
HCC1569 NXXZbYxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLVb5JLOzNizszN M3W4UlUh\A>? NH3yfVlqdmirYnn0d{A297zHIHPlcIwh\3Kxd4To MYiyN|kyQDd7Nx?=
OE19 NGi5OZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2mzelM{KM7:TR?= NWHpdm4{PSCm MWPpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= MUeyN|kyQDd7Nx?=
OE33 M3\G[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHSW2RtOzNizszN NYniUWlbPSCm MlvGbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= MnrqNlM6OTh5OUe=
JIMT1 NFf5dHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrjN|Mh|ryP M2\XW|Uh\A>? NFHYSVVqdmirYnn0d{A697zHIHPlcIwh\3Kxd4To M{TN[lI{QTF6N{m3
HCC1954 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWzN{DPxE1? NITkRmU2KGR? M1;6W4lvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4To MWqyN|kyQDd7Nx?=
NUGC4 NYO2dYV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:zN{DPxE1? M3GzNlUh\A>? NIGzZ2tqdmirYnn0d{AyPO,:hTDj[YxtKGe{b4f0bC=> MlHSNlM6OTh5OUe=
ZR-75-30 MoPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrEN|Mh|ryP M37NUVUh\A>? MkT4bY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To M1jyXlI{QTF6N{m3

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT(S473) / p-AKT(T308); 

PubMed: 25544637     


PIK3CA hot-spot mutant cell lines were treated with 1 µM BYL719 for the indicated period of time. Lysates were immunoblotted to detect the indicated proteins.

p100β / p110α / p85 / p-ERBB3(Y1289); 

PubMed: 25544637     


BT474 cells were treated with 1 µM BYL719 alone for different durations of time and lysates were immunoprecipitated with ERBB3 antibody. Precipitates were analyzed by western blot with the indicated antibodies.

p-HER2 / IGF-1R; 

PubMed: 25544637     


Cells were treated with 1 μM BYL719 for 24 hr and lysates were immunoblotted to detect the indicated proteins.

pS6 (Ser235-236); 

PubMed: 27048245     


Immunoblots of lysates from parental and resistant cells treated for 24 hours as indicated.

PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD; 

PubMed: 27604488     


T47D cells cultured to resistance in the presence of BYL719. Both parental (T47D) and resistant (T47DR) cells were treated with BYL719 at 1μM, and cell lysates were prepared at 0, 4, 24 hours for immunoblotting for the indicated proteins.

25544637 27048245 27604488
Growth inhibition assay
Cell viability; 

PubMed: 27602501     


The effect of BYL719 on cellular viability was evaluated in HCT116 (A) and SW480 (B) CRC cells. Briefly, cells were grown, treated with increasing concentrations of BYL719 (5, 10 and 20 μM) and cellular viability determined by MTS assay 72h after treatments. Controls included cells that remained untreated (media ctrl) and vehicle-treated controls (DMSO). Data represent means ± SEM of at least triplicate experiments normalized to controls. All conditions were compared with DMSO. Ctrl, control; DMSO, dimethyl sulfoxide. **, p< 0.01; ***, p< 0.001; ****, p< 0.0001.

27602501
Immunofluorescence
LC3; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 5 days with DMSO, 500 nM BKM120 or 500 nM BYL719. Cells were treated with DMSO or 1 μM Lapatinib for the final 18 h. GFP-LC3 localization was captured by fluorescent microscopy.

26637440
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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03207529 Recruiting Drug: Alpelisib|Drug: Enzalutamide Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Androgen Receptor Positive|Estrogen Receptor Negative|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Progesterone Receptor Negative|Progesterone Receptor Positive|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|PTEN Positive|Recurrent Breast Carcinoma|Refractory Breast Carcinoma|Triple-Negative Breast Carcinoma M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Novartis|Astellas Pharma Global Development Inc. June 7 2019 Phase 1
NCT02620839 Recruiting Drug: Alpelisib|Drug: Cisplatin Solid Tumors Pamela Munster|University of California San Francisco December 1 2016 Phase 1
NCT02734615 Recruiting Drug: LSZ102|Drug: LEE011|Drug: BYL719 Advanced or Metastatic ER+ Breast Cancer Novartis Pharmaceuticals|Novartis June 14 2016 Phase 1
NCT02550743 Terminated Drug: BYL719|Drug: Capecitabine|Radiation: Radiation Rectal Cancer howard safran|Brown University|Lifespan|Novartis Pharmaceuticals Corporation (Financial supporter) June 3 2016 Phase 1
NCT02437318 Active not recruiting Drug: Fulvestrant|Drug: Alpelisib|Drug: Alpelisib placebo Breast Cancer Novartis Pharmaceuticals|Novartis July 23 2015 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID