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 27 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 Moe4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMlEuOTByIN88US=> Mn74O|IhcA>? NInhXHFKSzVyPUGuNVAh|ryP NWrpflhrOjV3NUC1OFk>
SNU-1076 Ml7wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4q5cVAvOS1zMECg{txO NFzFZ3M4OiCq MU\JR|UxRTZwOEKg{txO M{fBdVI2PTVyNUS5
SNU-1066 NV;VW5dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TJZVAvOS1zMECg{txO M3m1N|czKGh? M{fRO2lEPTB;MT6xN{DPxE1? NEHQT2IzPTV3MEW0PS=>
FaDu MnG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1mwUFAvOS1zMECg{txO Mm\FO|IhcA>? MXnJR|UxRTF7Lk[2JO69VQ>? NXTUfJlUOjV3NUC1OFk>
SNU1041 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHGfFIxNjFvMUCwJO69VQ>? M1PLZlczKGh? M{jubmlEPTB;MkCuOlUh|ryP MW[yOVU2ODV2OR?=
SCC25 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[wMlEuOTByIN88US=> M4rieVczKGh? MVPJR|UxRTR7LkOwJO69VQ>? MlrINlU2PTB3NEm=
BON-1 NHPUeJpHfW6ldHnvckBCe3OjeR?= M3[xblEwOTBizszN Mn7iOEBp NFT5[YFqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= MYeyOVAzPjJ7Mh?=
QGP-1 M1vm[GZ2dmO2aX;uJGF{e2G7 NHLaUGMyNzFyIN88US=> M2XmUFQhcA>? MnvibY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? Mkf5NlUxOjZ{OUK=
MG-63 NHfLNYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHETWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= NEXJbXMzPDl4MUe5NC=>
HOS NEH6TG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrabVJKSzVyPUG1JO69Ve,:jDDJR|kxRTR{IN88US=> NH3KeGQzPDl4MUe5NC=>
MOS-J MoT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PRcmlEPTB;MUCg{txO97zOIFnDPVA:OzZizszN MWeyOFk3OTd7MB?=
POS-1 M{TXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OyU2lEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= MUeyOFk3OTd7MB?=
92.1 M37LNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWW1NFAuOjByMDDuUS=> MVu1JIQ> NIPmS|RqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MXyyOFU3OzV2MB?=
Mel270 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX61NFAuOjByMDDuUS=> M4P3d|Uh\A>? NIfTTWxqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MlqyNlQ2PjN3NEC=
Omm1.3 M{L6R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;SUFZkPTByLUKwNFAhdk1? MkXzOUBl NHn1XWdqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MVqyOFU3OzV2MB?=
Omm1 M2LldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\xdJZ7PTByLUKwNFAhdk1? MXW1JIQ> NVjyU4pEcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M13EeVI1PTZ|NUSw
C918 NX3IVlFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUe1NFAuOjByMDDuUS=> NVHjZnVrPSCm M4D3OYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M4fGUlI1PTZ|NUSw
Mel290 NGTXdnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfGUHE2ODBvMkCwNEBvVQ>? M3HZT|Uh\A>? MV\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MUiyOFU3OzV2MB?=
OPM2 MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWraTJZSOC53LUKuOUDPxE1? NWnMUpU{PDhiaB?= M4HaNolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWPheGRbOjR2MEWxNlE>
OPM1 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m5[|AvPS1{LkWg{txO MWG0PEBp MmrHbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NY\LbmZ[OjR2MEWxNlE>
U266 NHXOUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorpNE42NTJwNTFOwG0> Mor5OFghcA>? M{niZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3rj[lI1PDB3MUKx
MM1R M1PsOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGwMlUuOi53IN88US=> NYPxR3liPDhiaB?= NFLuNllqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYfVcIF5OjR2MEWxNlE>
MM1S MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMlUuOi53IN88US=> NGi3eGs1QCCq M3j1RolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXiyOFQxPTF{MR?=
H929 NHHo[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuwMlUuOi53IN88US=> M3rIclQ5KGh? NX;STGR[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mmf3NlQ1ODVzMkG=
RPMI MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnB[nJROC53LUKuOUDPxE1? MVe0PEBp Mn64bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Moj5NlQ1ODVzMkG=
SKBR3 NHLmUppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTON|Mh|ryP MXG1JIQ> MYTpcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= MlHGNlM6OTh5OUe=
MDA453 M1TrR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX6UmpPOzNizszN MYK1JIQ> MYDpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= M1[yUFI{QTF6N{m3
EFM192A NIP3WGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXTZXhTOzNizszN M3XCRlUh\A>? MlPSbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= MmjhNlM6OTh5OUe=
AU565 NWDRZYxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PIS|M{KM7:TR?= MVq1JIQ> MojpbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= M3m0[lI{QTF6N{m3
MDA361 NF;vb4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXizN{DPxE1? NF7lbXg2KGR? NVv0ZVlUcW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> NIXsXmYzOzlzOEe5Oy=>
BT474 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\MUVI{OyEQvF2= M{DselUh\A>? NFjGWm5qdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> NITKSlgzOzlzOEe5Oy=>
HCC202 NVuzWpJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6zN{DPxE1? NIT4SG02KGR? NFjWUm5qdmirYnn0d{AzOO,:hTDj[YxtKGe{b4f0bC=> M124VVI{QTF6N{m3
KPL4 NVPEV48xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHaWZY{OyEQvF2= MnzVOUBl MX;pcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= M{nW[|I{QTF6N{m3
NCL-N87 Mm\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLRe2Y{OyEQvF2= MkL3OUBl MU\pcohq[mm2czCzNg+9jSClZXzsJIdzd3e2aB?= M{Tq[VI{QTF6N{m3
UACC812 NVH3W2VtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFThXIg{OyEQvF2= MU[1JIQ> NHnvS3VqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> M{jzOVI{QTF6N{m3
HCC2218 NIXsUpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGzN{DPxE1? NW[4XopiPSCm MoDvbY5pcWKrdIOgNVXwxIViY3XscEBoem:5dHi= NVjVTXlrOjN7MUi3PVc>
HCC1569 NE\1cW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYqzN{DPxE1? M3\6VVUh\A>? M3rKfolvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= M1zBRVI{QTF6N{m3
OE19 NGC0W2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[4XFM{KM7:TR?= Ml36OUBl M{W0dolvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To MkWyNlM6OTh5OUe=
OE33 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjDe20{OyEQvF2= M2PTe|Uh\A>? NVi1NYJLcW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> M4LJUVI{QTF6N{m3
JIMT1 NVPYOnFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rrVVM{KM7:TR?= NWDRdHJlPSCm MVLpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq NG\6S2UzOzlzOEe5Oy=>
HCC1954 NVLDUFlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKzN{DPxE1? M1u2bFUh\A>? NYrsc2pwcW6qaXLpeJMhOjoxvJWgZ4VtdCCpcn;3eIg> Mmn1NlM6OTh5OUe=
NUGC4 NH73NopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrJOZQ{OyEQvF2= M3\6flUh\A>? NEPzOG5qdmirYnn0d{AyPO,:hTDj[YxtKGe{b4f0bC=> M3Sxc|I{QTF6N{m3
ZR-75-30 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjobHpKOzNizszN NUD1c4l3PSCm NELLOlFqdmirYnn0d{AuOTYxvJWgZ4VtdCCpcn;3eIg> NVHvRXpbOjN7MUi3PVc>

... 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
NCT02379247 Active not recruiting Drug: BYL719|Drug: Nab-paclitaxel Breast Cancer Priyanka Sharma|Novartis Pharmaceuticals|University of Kansas Medical Center February 2015 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID