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. 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.

Purity & Quality Control

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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 NEjpOZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqwMlEuOTByIN88US=> MVG3NkBp MnfJTWM2OD1zLkGwJO69VQ>? M2LydFI2PTVyNUS5
SNU-1076 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;mSWZTOC5zLUGwNEDPxE1? MX[3NkBp NF61doJKSzVyPU[uPFIh|ryP M2LFNVI2PTVyNUS5
SNU-1066 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXewPI5wOC5zLUGwNEDPxE1? MXy3NkBp M2rOWWlEPTB;MT6xN{DPxE1? MV2yOVU2ODV2OR?=
FaDu Moi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjtT45yOC5zLUGwNEDPxE1? MYW3NkBp MWLJR|UxRTF7Lk[2JO69VQ>? MnjaNlU2PTB3NEm=
SNU1041 M2Dvb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX1NE4yNTFyMDFOwG0> MUW3NkBp M1;KRmlEPTB;MkCuOlUh|ryP Mn\XNlU2PTB3NEm=
SCC25 NVXwfYNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fub|AvOS1zMECg{txO NUO4d2FoPzJiaB?= M4TTdGlEPTB;NEmuN|Ah|ryP MnjsNlU2PTB3NEm=
BON-1 M4\ucmZ2dmO2aX;uJGF{e2G7 NVLlZZdEOS9zMDFOwG0> Ml;aOEBp M{\mWIlvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| M3fVTFI2ODJ4Mkmy
QGP-1 NIKxS3JHfW6ldHnvckBCe3OjeR?= M3jCTFEwOTBizszN MkPFOEBp MlexbY5pcWKrdIOgVGk{UyBqQVvUJHNmejNyODmgZY5lKG2WT2LDNU8zKGGldHn2bZRq\XN? MnLsNlUxOjZ{OUK=
MG-63 M{[xSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnRU4pXUUN3ME22JO69Ve,:jDDJR|kxRTJ2IN88US=> NV7RdppKOjR7NkG3PVA>
HOS MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFuyfXhKSzVyPUG1JO69Ve,:jDDJR|kxRTR{IN88US=> MVuyOFk3OTd7MB?=
MOS-J NXXtcG5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= MYmyOFk3OTd7MB?=
POS-1 NXPBUHVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGntenRKSzVyPUig{txO97zOIFnDPVA:OzZizszN MnP2NlQ6PjF5OUC=
92.1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vqOVUxOC1{MECwJI5O MljMOUBl M4\WOYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M2TWb|I1PTZ|NUSw
Mel270 M{nHeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUG1NFAuOjByMDDuUS=> Mn[yOUBl MofibY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> M2jEd|I1PTZ|NUSw
Omm1.3 M3jheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV6yUppwPTByLUKwNFAhdk1? NF3vbpU2KGR? Mo\BbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NEm3W5AzPDV4M{W0NC=>
Omm1 M1v4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mof2OVAxNTJyMECgcm0> MWW1JIQ> NEDwTZdqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M{\kNVI1PTZ|NUSw
C918 NGHVUVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;uc|UxOC1{MECwJI5O NHy2[ZQ2KGR? MoH6bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MYSyOFU3OzV2MB?=
Mel290 Mne4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYC1NFAuOjByMDDuUS=> MlXVOUBl M3nMUYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NGeyWYwzPDV4M{W0NC=>
OPM2 NXLnOYpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPOZnUxNjVvMj61JO69VQ>? NUDFU3A1PDhiaB?= M{K0colvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoL4NlQ1ODVzMkG=
OPM1 Mlm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{flTFAvPS1{LkWg{txO NEfObZE1QCCq NHj3VXZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUGyOFQxPTF{MR?=
U266 MkHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLkOmNiOC53LUKuOUDPxE1? MnHuOFghcA>? NW[xcHNWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MljGNlQ1ODVzMkG=
MM1R M4\QWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX1[YoxNjVvMj61JO69VQ>? MV:0PEBp NHf3SJRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn3ZNlQ1ODVzMkG=
MM1S MmnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz1NE42NTJwNTFOwG0> MVy0PEBp NWXiZpJ3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXWyOFQxPTF{MR?=
H929 NXrufplNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHP2PHAxNjVvMj61JO69VQ>? MYC0PEBp MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUPKbIF[OjR2MEWxNlE>
RPMI NWHIe3p1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7QW2FbOC53LUKuOUDPxE1? NWTGcoY6PDhiaB?= M3\ySolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUXFc4ZHOjR2MEWxNlE>
SKBR3 M3LWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX4XGo{OyEQvF2= Mm\pOUBl M1LxOIlvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To MnHQNlM6OTh5OUe=
MDA453 NGDadFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfVfHc{OyEQvF2= MXe1JIQ> M4fYb4lvcGmkaYTzJFM597zHIHPlcIwh\3Kxd4To M2DBZVI{QTF6N{m3
EFM192A NVHXO2Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XCS|M{KM7:TR?= NGjkeFI2KGR? MULpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NWD2[JhwOjN7MUi3PVc>
AU565 NIXIVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvSUJNXOzNizszN M33TXVUh\A>? MXnpcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?= MnzQNlM6OTh5OUe=
MDA361 NWLWdHA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHF[Gk{OyEQvF2= NVHlVWw{PSCm Ml;CbY5pcWKrdIOgOFTwxIViY3XscEBoem:5dHi= M1K1d|I{QTF6N{m3
BT474 NUjlO2drT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X3TlM{KM7:TR?= NHvqdWE2KGR? NWPh[JdzcW6qaXLpeJMhOTcxvJWgZ4VtdCCpcn;3eIg> MW[yN|kyQDd7Nx?=
HCC202 Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHMfmM{OyEQvF2= MoLrOUBl M1\QUIlvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To MnG3NlM6OTh5OUe=
KPL4 NVz2eWJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PhPVM{KM7:TR?= MWW1JIQ> M1\1R4lvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To MVmyN|kyQDd7Nx?=
NCL-N87 NYHpeYdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3roTlM{KM7:TR?= M2\pblUh\A>? NUK1W2d{cW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> MXmyN|kyQDd7Nx?=
UACC812 NXLzdZFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljYN|Mh|ryP NVuxXIl4PSCm M3HGOolvcGmkaYTzJFI497zHIHPlcIwh\3Kxd4To M{j0[FI{QTF6N{m3
HCC2218 M{n3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXvcZFkOzNizszN M4DQfFUh\A>? Mk\RbY5pcWKrdIOgNVXwxIViY3XscEBoem:5dHi= NIHFT4ozOzlzOEe5Oy=>
HCC1569 M4\Ed2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPQU3c{OyEQvF2= NXn2clZJPSCm M1LPV4lvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= NICyS|kzOzlzOEe5Oy=>
OE19 M1r5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn3bmE{OyEQvF2= Mkj2OUBl NFTnTHlqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> NYflWJNoOjN7MUi3PVc>
OE33 NWPTeGk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqzN{DPxE1? NY\BWnVHPSCm M37ycIlvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To NF23c5czOzlzOEe5Oy=>
JIMT1 NXux[pVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7qbXQ{OyEQvF2= MVG1JIQ> Mk\ObY5pcWKrdIOgPg+9jSClZXzsJIdzd3e2aB?= NWfJWnhMOjN7MUi3PVc>
HCC1954 NWGwcHNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXWN|Mh|ryP MWm1JIQ> M{H0[IlvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4To NVrpVZFjOjN7MUi3PVc>
NUGC4 MkDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DrXVM{KM7:TR?= Mle2OUBl MlrFbY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= NWjCWVR2OjN7MUi3PVc>
ZR-75-30 NYLrXZBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrsfI5VOzNizszN MkPOOUBl NU[1VJcycW6qaXLpeJMhNTF378{FJINmdGxiZ4Lve5Rp M1XnXlI{QTF6N{m3

... 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:
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
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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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID