Home PI3K/Akt/mTOR PI3K inhibitor Alpelisib (BYL719) For research use only.

Alpelisib (BYL719)

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.

Alpelisib (BYL719) Chemical Structure

Alpelisib (BYL719) Chemical Structure

CAS No. 1217486-61-7

Purity & Quality Control

Alpelisib (BYL719) Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Detroit562 Growth Inhibition Assay 0.1-100 μM 72 h IC50=1.10 μM 25550549
SNU-1076 Growth Inhibition Assay 0.1-100 μM 72 h IC50=6.82 μM 25550549
SNU-1066 Growth Inhibition Assay 0.1-100 μM 72 h IC50=1.13 μM 25550549
FaDu Growth Inhibition Assay 0.1-100 μM 72 h IC50=19.66 μM 25550549
SNU1041 Growth Inhibition Assay 0.1-100 μM 72 h IC50=20.65 μM 25550549
SCC25 Growth Inhibition Assay 0.1-100 μM 72 h IC50=49.30 μM 25550549
BON-1 Function Assay 1/10 μM 4 h inhibits PI3K (AKT Ser308) and mTORC1/2 activities 25026292
QGP-1 Function Assay 1/10 μM 4 h inhibits PI3K (AKT Ser308) and mTORC1/2 activities 25026292
MG-63 Growth Inhibition Assay IC50=6 μM， IC90=24 μM 24961790
HOS Growth Inhibition Assay IC50=15 μM， IC90=42 μM 24961790
MOS-J Growth Inhibition Assay IC50=10 μM， IC90=36 μM 24961790
POS-1 Growth Inhibition Assay IC50=8 μM， IC90=36 μM 24961790
92.1 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Mel270 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Omm1.3 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Omm1 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
C918 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Mel290 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
OPM2 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
OPM1 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
U266 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
MM1R Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
MM1S Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
H929 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
RPMI Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
SKBR3 Growth Inhibition Assay 33 μM 5 d inhibits 35％ cell growth 23918797
MDA453 Growth Inhibition Assay 33 μM 5 d inhibits 38％ cell growth 23918797
EFM192A Growth Inhibition Assay 33 μM 5 d inhibits 27％ cell growth 23918797
AU565 Growth Inhibition Assay 33 μM 5 d inhibits 26％ cell growth 23918797
MDA361 Growth Inhibition Assay 33 μM 5 d inhibits 44％ cell growth 23918797
BT474 Growth Inhibition Assay 33 μM 5 d inhibits 16％ cell growth 23918797
HCC202 Growth Inhibition Assay 33 μM 5 d inhibits 20％ cell growth 23918797
KPL4 Growth Inhibition Assay 33 μM 5 d inhibits 58％ cell growth 23918797
NCL-N87 Growth Inhibition Assay 33 μM 5 d inhibits 31％ cell growth 23918797
UACC812 Growth Inhibition Assay 33 μM 5 d inhibits 27％ cell growth 23918797
HCC2218 Growth Inhibition Assay 33 μM 5 d inhibits 15％ cell growth 23918797
HCC1569 Growth Inhibition Assay 33 μM 5 d inhibits 5％ cell growth 23918797
OE19 Growth Inhibition Assay 33 μM 5 d inhibits 23％ cell growth 23918797
OE33 Growth Inhibition Assay 33 μM 5 d inhibits 23％ cell growth 23918797
JIMT1 Growth Inhibition Assay 33 μM 5 d inhibits 9％ cell growth 23918797
HCC1954 Growth Inhibition Assay 33 μM 5 d inhibits 29％ cell growth 23918797
NUGC4 Growth Inhibition Assay 33 μM 5 d inhibits 14％ cell growth 23918797
ZR-75-30 Growth Inhibition Assay 33 μM 5 d inhibits -15％ cell growth 23918797
Rat1 P110alpha inhibition assay IC50 = 0.074 μM 26164189
Rat1 PI3Kalpha inhibition assay IC50 = 0.074 μM 26206504
Rat1 P110alpha inhibition assay IC50 = 0.074 μM 23726034
Rat1 P110delta inhibition assay IC50 = 1.2 μM 26164189
Rat1 PI3Kgamma inhibition assay IC50 = 1.2 μM 26206504
Rat1 P110delta inhibition assay IC50 = 1.2 μM 23726034
Rat1 P110beta inhibition assay IC50 = 2.2 μM 26164189
Rat1 PI3Kbeta inhibition assay IC50 = 2.2 μM 26206504
Rat1 P110alpha inhibition assay IC50 = 2.2 μM 23726034
Click to View More Cell Line Experimental Data

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
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 Research Cell lines CW2 cells
Concentrations 500 nM
Incubation Time 72 h
Method

Cells were treated with increasing concentrations of alpelisib (0–1000 nM) for 72 h. Cell viability was quantified using the CyQuant assay.
Experimental Result Images Methods Biomarkers Images PMID
Western blot PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD pS6 (Ser235-236) p-HER2 / IGF-1R p100β / p110α / p85 / p-ERBB3(Y1289) p-AKT(S473) / p-AKT(T308) 27604488
Growth inhibition assay Cell viability 27602501
Immunofluorescence LC3 26637440
In Vivo
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]
Animal Research Animal Models Female athymic nu/nu mice
Dosages 40 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05948943 Recruiting
Lymphatic Malformations
Novartis Pharmaceuticals|Novartis
 November 24 2023 Phase 2|Phase 3
NCT05660083 Recruiting
HER2-negative Breast Cancer|Metastatic Breast Cancer|Metaplastic Breast Carcinoma|TNBC - Triple-Negative Breast Cancer
The Methodist Hospital Research Institute|Novartis Pharmaceuticals
 January 12 2023 Phase 2
NCT05508906 Recruiting
Metastatic Breast Cancer|Advanced Breast Cancer|HR-positive Breast Cancer|HER2-negative Breast Cancer
Olema Pharmaceuticals Inc.|Novartis
 August 31 2022 Phase 1
NCT05230810 Recruiting
HER2-positive Metastatic Breast Cancer
Criterium Inc.|Novartis|Seagen Inc.
 August 25 2022 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 441.47 Formula

C19H22F3N5O2S
CAS No. 1217486-61-7 SDF Download Alpelisib (BYL719) SDF
Smiles CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (199.33 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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