Alpelisib (BYL719)

Catalog No.S2814

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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Alpelisib (BYL719) Chemical Structure

Alpelisib (BYL719) Chemical Structure
Molecular Weight: 441.47

Validation & Quality Control

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Quality Control & MSDS

Related Compound Libraries

Alpelisib (BYL719) is available in the following compound libraries:

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Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Detroit562MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NH3DR40xNjFvMUCwJO69VQ>?NX\XWoh3PzJiaB?=NUDJZXlQUUN3ME2xMlExKM7:TR?=M4LSVlI2PTVyNUS5
SNU-1076MlHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXPDPIE3OC5zLUGwNEDPxE1?NYrZWHdwPzJiaB?=MVjJR|UxRTZwOEKg{txONF3v[HQzPTV3MEW0PS=>
SNU-1066NF7ueoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmTNNE4yNTFyMDFOwG0>NF:xNpU4OiCqMnvSTWM2OD1zLkGzJO69VQ>?MX6yOVU2ODV2OR?=
FaDuNXjKZYdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHr2XlgxNjFvMUCwJO69VQ>?MofGO|IhcA>?NHrkZZRKSzVyPUG5MlY3KM7:TR?=MVOyOVU2ODV2OR?=
SNU1041MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXHSSI06OC5zLUGwNEDPxE1?NV;QcVExPzJiaB?=MkK3TWM2OD1{MD62OUDPxE1?M{Hrc|I2PTVyNUS5
SCC25Mo\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUDF[mtXOC5zLUGwNEDPxE1?NE[yfnA4OiCqM33jW2lEPTB;NEmuN|Ah|ryPM3u3RVI2PTVyNUS5
BON-1NHSzUmtHfW6ldHnvckBCe3OjeR?=MWKxM|ExKM7:TR?=Ml:5OEBpNVfDfFRZcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO=NV3BcolnOjVyMk[yPVI>
QGP-1MXPGeY5kfGmxbjDBd5NigQ>?NVu0ephUOS9zMDFOwG0>MmrXOEBpMVvpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>?MUWyOVAzPjJ7Mh?=
MG-63M2HmZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXPJR|UxRTZizszN89yNKEmFOUC9NlQh|ryPM1;mZlI1QTZzN{mw
HOSNFzublVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkjQTWM2OD1zNTFOwG3wxIxiSVO5NF01OiEQvF2=M3LDelI1QTZzN{mw
MOS-JNWTzRYl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXTDVnB2UUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0>MUmyOFk3OTd7MB?=
POS-1NGX6TmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkjSTWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?=NEj4UnAzPDl4MUe5NC=>
92.1MljPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHzCSlE2ODBvMkCwNEBvVQ>?NXzTW2ZlPSCmMlz0bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0>M4G1WFI1PTZ|NUSw
Mel270MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mo\wOVAxNTJyMECgcm0>MVm1JIQ>NFex[25qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>?NUP4bZIxOjR3NkO1OFA>
Omm1.3MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3fUd|UxOC1{MECwJI5ONX7VO2NPPSCmMXfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=>NGfvcFMzPDV4M{W0NC=>
Omm1NXz6XWdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVH4TYY2PTByLUKwNFAhdk1?MWG1JIQ>MYfpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=>NEnobFkzPDV4M{W0NC=>
C918NFS4U3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXO1NFAuOjByMDDuUS=>NHe2WXA2KGR?MknNbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0>NHyyR5AzPDV4M{W0NC=>
Mel290MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3TxXFUxOC1{MECwJI5OM{nG[VUh\A>?NH7Ec4VqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>?M3LJPFI1PTZ|NUSw
OPM2NISwW49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NEjOZZIxNjVvMj61JO69VQ>?MX[0PEBpMnfFbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>NIjVemgzPDRyNUGyNS=>
OPM1M{nGZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUewMlUuOi53IN88US=>M1[5RlQ5KGh?MmrPbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>MXqyOFQxPTF{MR?=
U266MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3P4SFAvPS1{LkWg{txOMoDiOFghcA>?M2PJTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzM33ZSVI1PDB3MUKx
MM1RMmDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NInBVIMxNjVvMj61JO69VQ>?MlHIOFghcA>?NWPNPJl4cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?Mnm4NlQ1ODVzMkG=
MM1SMWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MW[wMlUuOi53IN88US=>Mn[xOFghcA>?MXXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NV3le5hzOjR2MEWxNlE>
H929MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NG\0U4kxNjVvMj61JO69VQ>?NWLEW|FLPDhiaB?=NXPkWYt1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?NUmydIo1OjR2MEWxNlE>
RPMIM{TZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mn\oNE42NTJwNTFOwG0>M1fKWFQ5KGh?NULBVoE6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?NXTLZVJGOjR2MEWxNlE>
SKBR3MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1PyZVM{KM7:TR?=NUPNWoFlPSCmNEHaO4NqdmirYnn0d{A{Pe,:hTDj[YxtKGe{b4f0bC=>NYrVWlZtOjN7MUi3PVc>
MDA453Mni0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIf4Xok{OyEQvF2=MX:1JIQ>NVLJbnVGcW6qaXLpeJMhOzkxvJWgZ4VtdCCpcn;3eIg>MlKwNlM6OTh5OUe=
EFM192AM2j0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUOzN{DPxE1?Mn3mOUBlMnnMbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi=NIrCfngzOzlzOEe5Oy=>
AU565MnLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mn3lN|Mh|ryPMkDzOUBlMUHpcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?=M4nUSFI{QTF6N{m3
MDA361NUjXfGx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXizN{DPxE1?NYCxXolLPSCmM2O5T4lvcGmkaYTzJFQ197zHIHPlcIwh\3Kxd4ToNWDBN|BpOjN7MUi3PVc>
BT474MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWDkV4QzOzNizszNMUS1JIQ>NWjFO4lycW6qaXLpeJMhOTcxvJWgZ4VtdCCpcn;3eIg>MViyN|kyQDd7Nx?=
HCC202M4[wUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NIPyR3A{OyEQvF2=MnrDOUBlNIXHUZhqdmirYnn0d{AzOO,:hTDj[YxtKGe{b4f0bC=>NVTrcmdUOjN7MUi3PVc>
KPL4M2HaTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NX\0[29QOzNizszNNX;RUY46PSCmNFvZNW9qdmirYnn0d{A2QO,:hTDj[YxtKGe{b4f0bC=>NFXjfXAzOzlzOEe5Oy=>
NCL-N87MnjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHW3bpg{OyEQvF2=NF\NeWI2KGR?NWnvUWR6cW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg>M1iwTVI{QTF6N{m3
UACC812NG\Qe3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1f0XFM{KM7:TR?=MV21JIQ>NY\kPGZCcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg>MnrYNlM6OTh5OUe=
HCC2218NF\TbHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mn32N|Mh|ryPNUT4U2h{PSCmM2j4PIlvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4ToNV:zc3lPOjN7MUi3PVc>
HCC1569MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MoP6N|Mh|ryPNFzDS|M2KGR?NXrY[|V2cW6qaXLpeJMhPe,:hTDj[YxtKGe{b4f0bC=>MYmyN|kyQDd7Nx?=
OE19NVjifFRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVizN{DPxE1?NVHWbG1LPSCmM3KxSYlvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4ToNHKyXlkzOzlzOEe5Oy=>
OE33NI\6NIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{myNVM{KM7:TR?=NYrsTlQ1PSCmMUDpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?=M1Hr[VI{QTF6N{m3
JIMT1NEPsZ2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M2fNSVM{KM7:TR?=MoX1OUBlNUjQeGs3cW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=>NVzvSHVrOjN7MUi3PVc>
HCC1954NIX4XXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NW\XXYlPOzNizszNNV7WfmNQPSCmM1;xTIlvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4ToMXSyN|kyQDd7Nx?=
NUGC4MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXqzN{DPxE1?NYLleGRxPSCmMXXpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?=NHTVZY4zOzlzOEe5Oy=>
ZR-75-30M{LY[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGjNSpI{OyEQvF2=NX\xUIFnPSCmNES1WZlqdmirYnn0d{AuOTYxvJWgZ4VtdCCpcn;3eIg>MoDMNlM6OTh5OUe=

... 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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dejan Juric, et al. 2012, AACR 103rd Annual Meeting. Abst CT-01.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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 Pharmace  ...more 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

view more

Chemical Information

Download Alpelisib (BYL719) SDF
Molecular Weight (MW) 441.47
Formula

C19H22F3N5O2S

CAS No. 1217486-61-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 88 mg/mL (199.33 mM)
Ethanol 2 mg/mL (4.53 mM)
Water <1 mg/mL (<1 mM)
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 Name 1,2-Pyrrolidinedicarboxamide, N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-, (2S)-

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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