Alpelisib (BYL719)

Catalog No.S2814 Batch:S281405

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Technical Data

Formula

C19H22F3N5O2S
Molecular Weight 441.47 CAS No. 1217486-61-7
Solubility (25°C)* In vitro DMSO 88 mg/mL (199.33 mM)
Ethanol 59 mg/mL (133.64 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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

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 (from reference)

Cell Assay:[2]
  • 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.
Animal Study:

[2]
  • Animal Models

    Female athymic nu/nu mice

  • Dosages

    40 mg/kg

  • Administration

    o.g.

Customer Product Validation

Data from [Data independently produced by Br J Haematol, 2014, 165(1), 89-101]

, , Mol Cancer Ther, 2017, 16(4):637-648

,

Selleck's Alpelisib (BYL719) has been cited by 198 publications

EML4-ALK fusions drive lung adeno-to-squamous transition through JAK-STAT activation [ J Exp Med, 2024, 221(3)e20232028] PubMed: 38284990
A p85 isoform switch enhances PI3K activation on endosomes by a MAP4- and PI3P-dependent mechanism [ Cell Rep, 2024, 43(5):114119] PubMed: 38630589
Integrated genomic and transcriptomic analysis reveals the activation of PI3K signaling pathway in HPV-independent cervical cancers [ Br J Cancer, 2024, 10.1038/s41416-023-02555-w] PubMed: 38253702
Integrative modeling uncovers p21-driven drug resistance and prioritizes therapies for PIK3CA-mutant breast cancer [ NPJ Precis Oncol, 2024, 8(1):20] PubMed: 38273040
Methyl vinyl ketone and its analogs covalently modify PI3K and alter physiological functions by inhibiting PI3K signaling [ J Biol Chem, 2024, 300(3):105679] PubMed: 38272219
Evolutionary states and trajectories characterized by distinct pathways stratify patients with ovarian high grade serous carcinoma [ Cancer Cell, 2023, 41(6):1103-1117.e12] PubMed: 37207655
Generation and multi-dimensional profiling of a childhood cancer cell line atlas defines new therapeutic opportunities [ Cancer Cell, 2023, 41(4):660-677.e7] PubMed: 37001527
Intact regulation of G1/S transition renders esophageal squamous cell carcinoma sensitive to PI3Kα inhibitors [ Signal Transduct Target Ther, 2023, 8(1):153] PubMed: 37041169
"Proteotranscriptomic analysis of advanced colorectal cancer patient derived organoids for drug sensitivity prediction" [ J Exp Clin Cancer Res, 2023, 42(1):8] PubMed: 36604765
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 42(20):1620-1633] PubMed: 37020035

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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