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.
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 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKwMlEuOTByIN88US=> Ml;YO|IhcA>? MkOzTWM2OD1zLkGwJO69VQ>? MUCyOVU2ODV2OR?=
SNU-1076 MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrDUFkxNjFvMUCwJO69VQ>? M37ZRVczKGh? M3rycmlEPTB;Nj64NkDPxE1? MUiyOVU2ODV2OR?=
SNU-1066 NF2zcpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKwMlEuOTByIN88US=> MmGzO|IhcA>? MmnuTWM2OD1zLkGzJO69VQ>? MorxNlU2PTB3NEm=
FaDu MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XRNFAvOS1zMECg{txO MUW3NkBp NXnNOop6UUN3ME2xPU43PiEQvF2= MVKyOVU2ODV2OR?=
SNU1041 NULxUVVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M320[FAvOS1zMECg{txO M4S1V|czKGh? M4Hj[GlEPTB;MkCuOlUh|ryP M2HRd|I2PTVyNUS5
SCC25 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4GyPVAvOS1zMECg{txO NWD1[XRFPzJiaB?= M{O5fGlEPTB;NEmuN|Ah|ryP M33QWlI2PTVyNUS5
BON-1 MXTGeY5kfGmxbjDBd5NigQ>? MoPhNU8yOCEQvF2= MmHxOEBp MV;pcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? MkfQNlUxOjZ{OUK=
QGP-1 MYLGeY5kfGmxbjDBd5NigQ>? MVuxM|ExKM7:TR?= NUG2PZEyPCCq M4[0O4lvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| MXqyOVAzPjJ7Mh?=
MG-63 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fqXWlEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= Mn;BNlQ6PjF5OUC=
HOS NGjXSYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonkTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= NVvO[4JtOjR7NkG3PVA>
MOS-J NYq2Zpd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrOTWM2OD1zMDFOwG3wxIxiSVO5NF0{PiEQvF2= NGHLSYIzPDl4MUe5NC=>
POS-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTtOYRYUUN3ME24JO69Ve,:jDDJR|kxRTN4IN88US=> MUKyOFk3OTd7MB?=
92.1 MlPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3TR5A2ODBvMkCwNEBvVQ>? NFuxfVE2KGR? NVTHRXJHcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M1TO[VI1PTZ|NUSw
Mel270 M3y4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXpOVAxNTJyMECgcm0> MU[1JIQ> MljYbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NHjn[JgzPDV4M{W0NC=>
Omm1.3 NX3yPZpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEniOZA2ODBvMkCwNEBvVQ>? NV;sSZdFPSCm MW\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MXyyOFU3OzV2MB?=
Omm1 M4\sSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWm1NFAuOjByMDDuUS=> MkTMOUBl NYD5[Yk1cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NEHWV4wzPDV4M{W0NC=>
C918 M2nXc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK1NFAuOjByMDDuUS=> MmToOUBl Mmm2bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NHLCOYIzPDV4M{W0NC=>
Mel290 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\6OVAxNTJyMECgcm0> M{\DdlUh\A>? NHPYR2tqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NFqybW4zPDV4M{W0NC=>
OPM2 MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4X4OVAvPS1{LkWg{txO NXywT2dMPDhiaB?= MnPxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVeyOFQxPTF{MR?=
OPM1 M2\PWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXNZnExNjVvMj61JO69VQ>? MWO0PEBp M1vtfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVT4XGgzOjR2MEWxNlE>
U266 Ml\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrmNE42NTJwNTFOwG0> MljEOFghcA>? M3TxRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUTOSVBlOjR2MEWxNlE>
MM1R MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYewMlUuOi53IN88US=> NXnaSnA1PDhiaB?= NV6xWXdJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWLBUHNyOjR2MEWxNlE>
MM1S NFO2[mZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\RNE42NTJwNTFOwG0> NVP3NoVSPDhiaB?= NUXWSIhpcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1XzW|I1PDB3MUKx
H929 M4G5O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj1b2w{OC53LUKuOUDPxE1? MWi0PEBp NFXBNXhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHHCOpczPDRyNUGyNS=>
RPMI MnvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7LNE42NTJwNTFOwG0> NGe0ToE1QCCq M3jJfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmS1NlQ1ODVzMkG=
SKBR3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PW[VM{KM7:TR?= NIKxN5E2KGR? MV3pcohq[mm2czCzOg+9jSClZXzsJIdzd3e2aB?= MUeyN|kyQDd7Nx?=
MDA453 NYjQUmpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfkN|Mh|ryP M1q1cVUh\A>? NEPyemZqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> MoP6NlM6OTh5OUe=
EFM192A NFixfohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnhUIQ{OyEQvF2= MofEOUBl MXPpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= MYiyN|kyQDd7Nx?=
AU565 M3KydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrXUIY{OyEQvF2= NF;BS4s2KGR? M360cIlvcGmkaYTzJFI397zHIHPlcIwh\3Kxd4To NEDNSm4zOzlzOEe5Oy=>
MDA361 M1nudGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSzN{DPxE1? MWe1JIQ> NXLDOZZEcW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> NYnRSZg6OjN7MUi3PVc>
BT474 NUPFflJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorGN|Mh|ryP MYe1JIQ> MYDpcohq[mm2czCxOw+9jSClZXzsJIdzd3e2aB?= NYXvO2IyOjN7MUi3PVc>
HCC202 NITTSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIf4Now{OyEQvF2= NWn5b4dpPSCm NXjEPHhncW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> M3PmVFI{QTF6N{m3
KPL4 NYrHfJA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HNTlM{KM7:TR?= NU\JN2ZSPSCm M2DO[olvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To NE\IWFYzOzlzOEe5Oy=>
NCL-N87 NH3TdotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LrXFM{KM7:TR?= NYDvSGZmPSCm MojNbY5pcWKrdIOgN|HwxIViY3XscEBoem:5dHi= MUCyN|kyQDd7Nx?=
UACC812 MlT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jj[|M{KM7:TR?= M{TMXVUh\A>? Mm\rbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= MXWyN|kyQDd7Nx?=
HCC2218 M33xSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv4U3M{OyEQvF2= M2nuelUh\A>? MkHGbY5pcWKrdIOgNVXwxIViY3XscEBoem:5dHi= MXuyN|kyQDd7Nx?=
HCC1569 NGXDbXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\IXlM{KM7:TR?= NXiyTFBFPSCm M1rO[IlvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= Mk\MNlM6OTh5OUe=
OE19 NYfsNJMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYiyXnlzOzNizszN MXy1JIQ> NHrjTpFqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> MlyyNlM6OTh5OUe=
OE33 NUH5XFh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYizN{DPxE1? M4[zUFUh\A>? MX;pcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= M1rZOVI{QTF6N{m3
JIMT1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm0eJA{OyEQvF2= NEPVV242KGR? MnrjbY5pcWKrdIOgPg+9jSClZXzsJIdzd3e2aB?= NIn0T4MzOzlzOEe5Oy=>
HCC1954 NYTUcpcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTWfJV1OzNizszN M2X6dlUh\A>? MmPYbY5pcWKrdIOgNlnwxIViY3XscEBoem:5dHi= NX\VVnUxOjN7MUi3PVc>
NUGC4 NUfjXY5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVywTW9ZOzNizszN NHrzZm82KGR? MVzpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= MWKyN|kyQDd7Nx?=
ZR-75-30 NWqwUmk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYOzN{DPxE1? NUnaeIpPPSCm M3Pr[4lvcGmkaYTzJE0yPe,:hTDj[YxtKGe{b4f0bC=> MmGyNlM6OTh5OUe=

... 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 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03207529 Not yet recruiting Malignant Neoplasm of Breast M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc. January 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03601507 Not yet recruiting CDKN2A-p16 Positive|Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 University of Arizona|National Cancer Institute (NCI) November 30 2018 Phase 2
NCT03386162 Recruiting Breast Cancer PI3K Alpelisib UNICANCER March 15 2018 Phase 2
NCT03138070 Recruiting Head and Neck Squamous Cell Cancer Lawson Health Research Institute October 20 2017 Not Applicable
NCT03292250 Recruiting HNSCC|Head and Neck Neoplasms Seoul National University Hospital|Korean Cancer Study Group|Chungnam National University Hospital September 10 2017 Phase 2

Tech Support

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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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID