Alpelisib (BYL719)

Catalog No.S2814 Batch:S281404

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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 2 mg/mL (4.53 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 221 publications

AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6] PubMed: 39385030
A class I PI3K signalling network regulates primary cilia disassembly in normal physiology and disease [ Nat Commun, 2024, 15(1):7181] PubMed: 39168978
Combined inhibition of KRASG12C and mTORC1 kinase is synergistic in non-small cell lung cancer [ Nat Commun, 2024, 15(1):6076] PubMed: 39025835
EML4-ALK fusions drive lung adeno-to-squamous transition through JAK-STAT activation [ J Exp Med, 2024, 221(3)e20232028] PubMed: 38284990
Arachidonic acid released by PIK3CA mutant tumor cells triggers malignant transformation of colonic epithelium by inducing chromatin remodeling [ Cell Rep Med, 2024, S2666-3791(24)00179-4] PubMed: 38614093
PI3K/mTOR inhibition induces tumour microenvironment remodelling and sensitises pS6high uterine leiomyosarcoma to PD-1 blockade [ Clin Transl Med, 2024, 14(5):e1655] PubMed: 38711203
PI3K/mTOR inhibition induces tumour microenvironment remodelling and sensitises pS6high uterine leiomyosarcoma to PD-1 blockade [ Clin Transl Med, 2024, 14(5):e1655] PubMed: 38711203
Combined inhibition of CDK4/6 and AKT is highly effective against the luminal androgen receptor (LAR) subtype of triple negative breast cancer [ Cancer Lett, 2024, 604:217219] PubMed: 39244005
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

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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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