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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2 Customer Reviews

  • 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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M1fldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XFflAvOS1zMECg{txO MVq3NkBp MkTRTWM2OD1zLkGwJO69VQ>? MYWyOVU2ODV2OR?=
SNU-1076 M1LETmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\JTYhjOC5zLUGwNEDPxE1? NE\hcIw4OiCq NIO4OGpKSzVyPU[uPFIh|ryP NFm1UFkzPTV3MEW0PS=>
SNU-1066 NUHHWJR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGwMlEuOTByIN88US=> MUm3NkBp MorTTWM2OD1zLkGzJO69VQ>? MnrINlU2PTB3NEm=
FaDu MlXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1W5bVAvOS1zMECg{txO MoO4O|IhcA>? NVe3dHh2UUN3ME2xPU43PiEQvF2= MmXDNlU2PTB3NEm=
SNU1041 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[wMlEuOTByIN88US=> MY[3NkBp MkfoTWM2OD1{MD62OUDPxE1? NHTrS3EzPTV3MEW0PS=>
SCC25 NV3OZWFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOxNGttOC5zLUGwNEDPxE1? MWW3NkBp NXnlfHY1UUN3ME20PU4{OCEQvF2= NIHO[m4zPTV3MEW0PS=>
BON-1 Ml7TSpVv[3Srb36gRZN{[Xl? MmXTNU8yOCEQvF2= MXy0JIg> MWTpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? Mnn0NlUxOjZ{OUK=
QGP-1 NWjibmEzTnWwY4Tpc44hSXO|YYm= NE\FU2syNzFyIN88US=> M4CzcVQhcA>? NHjC[VhqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= M3XYcFI2ODJ4Mkmy
MG-63 NXS1OW4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX32XWxYUUN3ME22JO69Ve,:jDDJR|kxRTJ2IN88US=> NYjsOnc1OjR7NkG3PVA>
HOS M3fRU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTYTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= NFv5RlYzPDl4MUe5NC=>
MOS-J NH33NHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= NXLlbVRkOjR7NkG3PVA>
POS-1 NWSxOI5yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmO1TWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?= NHjRfmYzPDl4MUe5NC=>
92.1 M{P3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;PRlUxOC1{MECwJI5O NVLQb5ZtPSCm NUPBdmZlcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MX2yOFU3OzV2MB?=
Mel270 Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXROVAxNTJyMECgcm0> MVW1JIQ> M3iyVolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MXyyOFU3OzV2MB?=
Omm1.3 NEOw[FFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWO1NFAuOjByMDDuUS=> MVy1JIQ> NYDsXG92cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NGflUlczPDV4M{W0NC=>
Omm1 NYTPNYN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXQNFg1PTByLUKwNFAhdk1? NIHCU5U2KGR? MnrGbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> M1\Gc|I1PTZ|NUSw
C918 NV7mPGZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnK[o8zPTByLUKwNFAhdk1? MonlOUBl M2XMT4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M2HSZ|I1PTZ|NUSw
Mel290 M2PMUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELHR4I2ODBvMkCwNEBvVQ>? MYS1JIQ> NXf4XGttcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? Mo\uNlQ2PjN3NEC=
OPM2 NFmxSWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmwMlUuOi53IN88US=> NIX6S5Y1QCCq NWjlU5hmcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVXIN4pwOjR2MEWxNlE>
OPM1 Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlUuOi53IN88US=> NFnhdWc1QCCq MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXSyOFQxPTF{MR?=
U266 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zlUFAvPS1{LkWg{txO NVGxdHNiPDhiaB?= NF\I[YxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHjLXmozPDRyNUGyNS=>
MM1R MljOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDCcFUxOC53LUKuOUDPxE1? MlHROFghcA>? MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWn6VHZVOjR2MEWxNlE>
MM1S Mlq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHKeZAxNjVvMj61JO69VQ>? MXW0PEBp Ml74bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUnSV5VROjR2MEWxNlE>
H929 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXleXcxNjVvMj61JO69VQ>? NX\YXHl[PDhiaB?= Mo\LbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYTIUoZTOjR2MEWxNlE>
RPMI MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zhRlAvPS1{LkWg{txO MlrwOFghcA>? NF7YU4tqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2q3blI1PDB3MUKx
SKBR3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPhdYU{OyEQvF2= M{LMTlUh\A>? M3v3fIlvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To NV;6dVJkOjN7MUi3PVc>
MDA453 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnoVFVbOzNizszN MWi1JIQ> Mkm5bY5pcWKrdIOgN|jwxIViY3XscEBoem:5dHi= MXiyN|kyQDd7Nx?=
EFM192A NVfDcYZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjVN|Mh|ryP MYi1JIQ> MXTpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NEn4W4IzOzlzOEe5Oy=>
AU565 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVezN{DPxE1? MWK1JIQ> MX;pcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?= Mn\HNlM6OTh5OUe=
MDA361 M1LGcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF2zSVE{OyEQvF2= MVe1JIQ> NX;ESlZFcW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> NY\OZndCOjN7MUi3PVc>
BT474 M1OzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[zN{DPxE1? MWW1JIQ> M3zWVYlvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To NUfMfXRIOjN7MUi3PVc>
HCC202 NVzTUFdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLHeWV4OzNizszN Ml\LOUBl MXvpcohq[mm2czCyNQ+9jSClZXzsJIdzd3e2aB?= MXOyN|kyQDd7Nx?=
KPL4 MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfwN|Mh|ryP M3jYNVUh\A>? M{TPUYlvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To NUSyeIt{OjN7MUi3PVc>
NCL-N87 MkXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjHd|A{OyEQvF2= MV:1JIQ> MkjObY5pcWKrdIOgN|HwxIViY3XscEBoem:5dHi= NEXwO5kzOzlzOEe5Oy=>
UACC812 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuzN{DPxE1? MlrYOUBl MXrpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= Mn\TNlM6OTh5OUe=
HCC2218 NYjwZpNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PxTlM{KM7:TR?= M4HrXFUh\A>? NGLleIdqdmirYnn0d{AyPe,:hTDj[YxtKGe{b4f0bC=> NWjBeopQOjN7MUi3PVc>
HCC1569 NYS1c5RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zhcVM{KM7:TR?= M1njNVUh\A>? M1LSSIlvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= NHW1OZYzOzlzOEe5Oy=>
OE19 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[zN{DPxE1? NEexSnE2KGR? M1zoOIlvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To NI\Qe48zOzlzOEe5Oy=>
OE33 NUPBW5dNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS1bnpEOzNizszN NYTGVpNWPSCm NIDL[o5qdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> M1z5blI{QTF6N{m3
JIMT1 M3vCPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYq2e49KOzNizszN MlG4OUBl MXjpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq NFnqZYozOzlzOEe5Oy=>
HCC1954 M2DzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7GcnQ{OyEQvF2= Ml[wOUBl NVLFRWk4cW6qaXLpeJMhOjoxvJWgZ4VtdCCpcn;3eIg> MmD0NlM6OTh5OUe=
NUGC4 NV\RXoFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7FN|Mh|ryP MlfKOUBl MWPpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= NV7X[YxKOjN7MUi3PVc>
ZR-75-30 NUHwPGo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXHcGlLOzNizszN NHvRV|I2KGR? MorsbY5pcWKrdIOgMVE297zHIHPlcIwh\3Kxd4To NUnWNm43OjN7MUi3PVc>

... 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
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
NCT02145312 Not yet recruiting Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck Yonsei University March 2016 Phase 2
NCT02624557 Recruiting Hepatic Impairment Novartis Pharmaceuticals|Novartis December 2015 Phase 1
NCT02620839 Not yet recruiting Solid Tumors Pamela Munster|University of California, San Francisco December 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID