Alpelisib | PI3K⍺ inhibitor

CAS:
 1217486-61-7
Catalog Number:
 10-4167

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5 mg$40.00
25 mg$125.00
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Alpelisib (1217486-61-7)  is a potent and selective (IC50s = 7.4 nM PI3Kα; 2.2 µM PI3Kß; 1.2 µM PI3KIδ; 50-fold selectivity against 442 tested kinases) PI3Kα inhibitor.1 Approved for use in the treatment of HR(+), HER2(-), PIK3CA-mutated breast cancer. Alpelisib has been used in combination with various chemotherapeutics to treat ovarian2, colorectal3, kidney4, bladder5, and head and neck6 cancers.

References/Citations:

  1. Furet et al. (2013), Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation; Bioorg. Med. Chem. Lett., 23 3741
  2. Thibault et al. (2025), PI3Kα-specific inhibitor BYL-719 synergizes with cisplatin in vitro in PIK3CA-mutated ovarian cancer cells; Sci. Rep., 15 6265
  3. Lim, et al. (2024), Phase 1b and pharmacokinetics study of alpelisib, a PIK3CA inhibitor, and capecitabine in patients with advanced solid tumors; Front. Oncol., 14 1390452
  4. Khalid et al. (2024), Dual inhibition of atypical PKC signaling and PI3K/Akt signaling dysregulates c-Myc to induce apoptosis in clear cell Renal Cell Carcinoma; Front. Oncol., 13 1213715
  5. Corral et al. (2023), Tumor and Stromal Cell Targeting with Nintedanib and Alpelisib Overcomes Intrinsic Bladder Cancer Resistance; Mol. Cancer Ther., 22 616
  6. Razak et al. (2023), A Phase 1b/2 Study of Alpelisib in Combination with Cetuximab in Patients with Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma; Target Oncol., 18 853
1217486-61-7, Alpelisib, Alpelisib supplier, BYL719, NVP-BYL719, PI3Kα inhibitor
CAS:
1217486-61-7
Catalog Number:
10-4167
Activity:
PI3Kα inhibitor
Chemical Names:
(2S)-1-N-[4-Methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridine-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
Alternate Name:
NVP-BYL719; BYL719
Molecular Weight:
441.47
Molecular Formula:

C19H22F3N5O2S

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee