Alpelisib (BYL719)
For research use only. Not for use in humans.
Catalog No.S2814
54 publications
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.
Purity & Quality Control
Choose Selective PI3K Inhibitors
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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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 |
| Smiles | CC1=C(SC(=N1)NC(=O)N2CCCC2C(N)=O)C3=CC(=NC=C3)C(C)(C)C(F)(F)F |
Bio Calculators
Molarity Calculator
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Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT03207529 | Recruiting | Drug: Alpelisib|Drug: Enzalutamide | Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Androgen Receptor Positive|Estrogen Receptor Negative|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Progesterone Receptor Negative|Progesterone Receptor Positive|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|PTEN Positive|Recurrent Breast Carcinoma|Refractory Breast Carcinoma|Triple-Negative Breast Carcinoma | M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Novartis|Astellas Pharma Global Development Inc. | June 7 2019 | Phase 1 |
| NCT02620839 | Recruiting | Drug: Alpelisib|Drug: Cisplatin | Solid Tumors | Pamela Munster|University of California San Francisco | December 1 2016 | Phase 1 |
| NCT02734615 | Recruiting | Drug: LSZ102|Drug: LEE011|Drug: BYL719 | Advanced or Metastatic ER+ Breast Cancer | Novartis Pharmaceuticals|Novartis | June 14 2016 | Phase 1 |
| NCT02550743 | Terminated | Drug: BYL719|Drug: Capecitabine|Radiation: Radiation | Rectal Cancer | howard safran|Brown University|Lifespan|Novartis Pharmaceuticals Corporation (Financial supporter) | June 3 2016 | Phase 1 |
| NCT02437318 | Active not recruiting | Drug: Fulvestrant|Drug: Alpelisib|Drug: Alpelisib placebo | Breast Cancer | Novartis Pharmaceuticals|Novartis | July 23 2015 | Phase 3 |
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.
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