For research use only.
CAS No. 1217486-61-7
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.
Selleck's Alpelisib (BYL719) has been cited by 119 publications
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Choose Selective PI3K Inhibitors
|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.|
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. 
|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. |
|In vitro||DMSO||88 mg/mL (199.33 mM)|
|Ethanol||2 mg/mL (4.53 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* 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.
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||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
1.Please make sure the liquid is clear before adding the next solvent.
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Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04589650||Recruiting||Drug: Alpelisib|Drug: Placebo||PIK3CA-related Overgrowth Spectrum (PROS)||Novartis Pharmaceuticals|Novartis||April 19 2021||Phase 2|
|NCT04762979||Recruiting||Drug: Alpelisib|Drug: Fulvestrant|Drug: Aromatase inhibitor||Hormone Receptor Positive Breast Carcinoma|HER2-negative Breast Cancer|PIK3CA Mutant Metastatic Breast Cancer||Amanda Parkes|Novartis|University of Wisconsin Madison|Big Ten Cancer Research Consortium||February 12 2021||Phase 2|
|NCT04544189||Recruiting||Drug: Alpelisib|Drug: Fulvestrant|Drug: Placebo||Breast Neoplasms||Novartis Pharmaceuticals|Novartis||January 20 2021||Phase 2|
|NCT04524000||Recruiting||Drug: Alpelisib|Drug: Fulvestrant||Advanced Breast Cancer||Novartis Pharmaceuticals|Novartis||November 20 2020||Phase 2|
|NCT04300790||Recruiting||Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant||Breast Cancer||MedSIR|Novartis||October 23 2020||Phase 2|
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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