research use only

Alpelisib (BYL719) PI3Kα inhibitor

Name: Alpelisib (BYL719)
Brand: Selleck Chemicals
SKU: S2814
Availability: InStock
Rating: 5 (243 reviews)

Cat.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. This compound is in Phase 2.

Chemical Structure

Molecular Weight: 441.47

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Akt mTOR AMPK GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK PI4K PIKfyve MELK
Related Products	LY294002 3-Methyladenine (3-MA) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin (SL-2052) Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	441.47	Formula	C₁₉H₂₂F₃N₅O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1217486-61-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (199.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.400mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL 88 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PI3Kα ^[1] (Cell-free assay) 5 nM
In vitro	Alpelisib (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]
In vivo	Alpelisib (BYL719) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents at doses exceeding 270 mg/d. It has a low clearance, a half-life of 8.5 h, and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying low inter-individual variability in Cmax and AUC in humans. At 270 mg/d, this compound shows first signs of clinical efficacy, including 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]
References	[1] http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/CT-01?rss=1 [2] https://pubmed.ncbi.nlm.nih.gov/34171264/

Applications

Methods	Biomarkers	PMID
Western blot	p-AKT(S473) / p-AKT(T308) p100β / p110α / p85 / p-ERBB3(Y1289) p-HER2 / IGF-1R pS6 (Ser235-236) PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD	25544637
Growth inhibition assay	Cell viability	27602501
Immunofluorescence	LC3	26637440

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):