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
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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 NH3JS5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjIeW8xNjFvMUCwJO69VQ>? MYO3NkBp M4ToSWlEPTB;MT6xNEDPxE1? NIXPRZczPTV3MEW0PS=>
SNU-1076 MoGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\COWgxNjFvMUCwJO69VQ>? NXjs[3FOPzJiaB?= MofUTWM2OD14LkiyJO69VQ>? MV:yOVU2ODV2OR?=
SNU-1066 M2rUW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{K5e|AvOS1zMECg{txO NULtemVHPzJiaB?= MYHJR|UxRTFwMUOg{txO MWqyOVU2ODV2OR?=
FaDu M1;vZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzt[pMxNjFvMUCwJO69VQ>? M1fU[lczKGh? NXy2fWhDUUN3ME2xPU43PiEQvF2= NHn3bmEzPTV3MEW0PS=>
SNU1041 NYPoVXp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmwMlEuOTByIN88US=> NXTkeno{PzJiaB?= MoXXTWM2OD1{MD62OUDPxE1? NHrUfVYzPTV3MEW0PS=>
SCC25 M3\lTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXznc5VJOC5zLUGwNEDPxE1? MVS3NkBp NWjPSI9bUUN3ME20PU4{OCEQvF2= NH;sbGgzPTV3MEW0PS=>
BON-1 NIO1WJdHfW6ldHnvckBCe3OjeR?= MUixM|ExKM7:TR?= MnPuOEBp NULIfXFHcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= MkL4NlUxOjZ{OUK=
QGP-1 NWjMUGN2TnWwY4Tpc44hSXO|YYm= NFjyRlcyNzFyIN88US=> MkPzOEBp NWnFeZVtcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= MVWyOVAzPjJ7Mh?=
MG-63 NGS3fpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTTTWl1UUN3ME22JO69Ve,:jDDJR|kxRTJ2IN88US=> NXvV[mNGOjR7NkG3PVA>
HOS NWe4Rm1TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknnTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2= NWizS5J{OjR7NkG3PVA>
MOS-J Mo\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nr[WlEPTB;MUCg{txO97zOIFnDPVA:OzZizszN M4rXN|I1QTZzN{mw
POS-1 NEnS[ZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PsdWlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= MYGyOFk3OTd7MB?=
92.1 MlvqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVu1NFAuOjByMDDuUS=> MWq1JIQ> MYrpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MnX5NlQ2PjN3NEC=
Mel270 NXzwfYV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzJe5I{PTByLUKwNFAhdk1? MVS1JIQ> MVTpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> M3q4SFI1PTZ|NUSw
Omm1.3 NXO2d|Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\sPJQ2ODBvMkCwNEBvVQ>? MWi1JIQ> MorHbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NHHvXpQzPDV4M{W0NC=>
Omm1 M1fWZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXO1NFAuOjByMDDuUS=> NWK5R28xPSCm MYjpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NEe2b4YzPDV4M{W0NC=>
C918 Mlu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm2OVAxNTJyMECgcm0> M2PmS|Uh\A>? MYPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> M2ewTFI1PTZ|NUSw
Mel290 NUHCUFBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjqO2k2ODBvMkCwNEBvVQ>? MYe1JIQ> NHrCU4JqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M4DGfFI1PTZ|NUSw
OPM2 NYLnUoo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXJT2QxNjVvMj61JO69VQ>? MXi0PEBp MkLkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEjIWmUzPDRyNUGyNS=>
OPM1 NGntdllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mke5NE42NTJwNTFOwG0> M3HUdlQ5KGh? Mo[2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M4DyTVI1PDB3MUKx
U266 NH3qTFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r1VFAvPS1{LkWg{txO NX7yZolvPDhiaB?= M1W1eIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlrCNlQ1ODVzMkG=
MM1R M2f2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;obG9mOC53LUKuOUDPxE1? NUfOVnhJPDhiaB?= MnrDbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWiyOFQxPTF{MR?=
MM1S NIXaTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTy[ZMxNjVvMj61JO69VQ>? MVe0PEBp NXyzN3V1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFzKc20zPDRyNUGyNS=>
H929 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTpNE42NTJwNTFOwG0> M4fQd|Q5KGh? MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUOyOFQxPTF{MR?=
RPMI NHLqTINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYewMlUuOi53IN88US=> NWrhcVJLPDhiaB?= M3njSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkD4NlQ1ODVzMkG=
SKBR3 M{\VXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHDOVA{OyEQvF2= NH;FSoo2KGR? NUHsblVlcW6qaXLpeJMhOzYxvJWgZ4VtdCCpcn;3eIg> MlHnNlM6OTh5OUe=
MDA453 M{PZRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXLN|Mh|ryP NYHMdI5XPSCm M4ewU4lvcGmkaYTzJFM597zHIHPlcIwh\3Kxd4To M{jaVlI{QTF6N{m3
EFM192A NF;4VI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLtN2Q{OzNizszN MnnzOUBl NGXpb4xqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> MV:yN|kyQDd7Nx?=
AU565 Mkm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\5b|M{KM7:TR?= NYf2boE4PSCm Mn;QbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= M2rZZVI{QTF6N{m3
MDA361 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnKUmg{OyEQvF2= NEP4SoM2KGR? NVfMVndocW6qaXLpeJMhPDUxvJWgZ4VtdCCpcn;3eIg> MljUNlM6OTh5OUe=
BT474 NYTL[lZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWf5[Fg1OzNizszN MUi1JIQ> M4rKOIlvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To NUnpRVJROjN7MUi3PVc>
HCC202 M1;JS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmzN{DPxE1? NGToZpE2KGR? MmOxbY5pcWKrdIOgNlDwxIViY3XscEBoem:5dHi= NFvwO5YzOzlzOEe5Oy=>
KPL4 NHLGZ2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fzWVM{KM7:TR?= MnTiOUBl M4frNolvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To NEH3PY4zOzlzOEe5Oy=>
NCL-N87 NXnsXpp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTHRZF5OzNizszN M4P4U|Uh\A>? MlPrbY5pcWKrdIOgN|HwxIViY3XscEBoem:5dHi= NEXKOIYzOzlzOEe5Oy=>
UACC812 NHXadIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWzN{DPxE1? MXq1JIQ> Mk\MbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= NVW1TWxZOjN7MUi3PVc>
HCC2218 M{XEPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;NR|M{KM7:TR?= MYG1JIQ> M4HWUolvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To M2ryeVI{QTF6N{m3
HCC1569 M2fCbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrq[44{OyEQvF2= M3v6OFUh\A>? M{jIcolvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= NXPGWHB1OjN7MUi3PVc>
OE19 NV;VOnhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\VW2dXOzNizszN MV61JIQ> NELldGpqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> M3jNT|I{QTF6N{m3
OE33 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3DV3NlOzNizszN NXm1R5NpPSCm MUfpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NXTSZYF[OjN7MUi3PVc>
JIMT1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELDVWw{OyEQvF2= MlHqOUBl MXTpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq MYOyN|kyQDd7Nx?=
HCC1954 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOzN{DPxE1? NXrDPYdWPSCm MlH4bY5pcWKrdIOgNlnwxIViY3XscEBoem:5dHi= NU\aVZU5OjN7MUi3PVc>
NUGC4 M{DVZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPzeZU{OyEQvF2= MlvhOUBl MWDpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= NIT6fW4zOzlzOEe5Oy=>
ZR-75-30 MkXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqzN{DPxE1? NVyxblVnPSCm MYPpcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi= MYmyN|kyQDd7Nx?=

... 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
NCT02058381 Completed Pre-menopausal Breast Cancer|PI3K Pathway Inhibition Novartis Pharmaceuticals|Novartis May 6 2014 Phase 1
NCT02051751 Completed Neoplasms Breast Neoplasms Head and Neck Neoplasms Novartis Pharmaceuticals|Novartis March 5 2014 Phase 1
NCT01219699 Active not recruiting Advanced Solid Tumors With an Alteration of the PIK3CA Gene|Estrogen Receptor Positive Breast Cancer Novartis Pharmaceuticals|Novartis October 5 2010 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) September 30 2018 Phase 2
NCT02282371 Active not recruiting Head and Neck Squamous Cell Cancer Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals October 30 2014 Phase 1
NCT02155088 Active not recruiting Pancreatic Cancer H. Lee Moffitt Cancer Center and Research Institute|Novartis October 30 2014 Phase 1

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID