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Formula | C19H22F3N5O2S |
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Molecular Weight | 441.47 | CAS No. | 1217486-61-7 | ||||
Solubility (25°C)* | In vitro | DMSO | 88 mg/mL (199.33 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <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.) |
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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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] |
Cell Assay:[2] |
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Animal Study: |
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Data from [Data independently produced by Br J Haematol, 2014, 165(1), 89-101]
, , Mol Cancer Ther, 2017, 16(4):637-648
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.