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Alpelisib

SYN-1230-M001 1 mg INQ
SYN-1230-M005 5 mg INQ
SYN-1230-M010 10 mg INQ
SYN-1230-M050 50 mg INQ
SYN-1230-M100 100 mg INQ
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Product Data
Synonyms (2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide; BYL719; NVP-BYL719
Properties
Formula C19H22F3N5O2S
MW 441.5
CAS 1217486-61-7
Purity ≥95%
Appearance Solid.
Solubility Soluble in DMSO or DMF.
Origin Manufactured by SynKinase.
Other Product Data Target: PI3Kalpha | Kinase Group: Lipid Kinase | Substrate: Lipid

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key STUWGJZDJHPWGZ-LBPRGKRZSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.

Product Description

Selective PI3Kα inhibitor with IC50 of 5nM. Has minimal effect on other PI3K isoforms. Exhibits favorable pharmacokinetics and excellent oral bioavailability in animal models. In xenografts using nude mice, it showed dose-dependent effects of tumour inhibition. In a phase Ib study, it showed synergistic anti-tumor activity with endocrine therapy against ER+/PIK3CA mutated breast cancer cells.

Product References

  1. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation: P. Furet, et al.; Bioorg. Med. Chem. Lett. 23, 3741 (2013)
  2. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials: C. Fritsch, et al.; Mol. Cancer Ther. 13, 1117 (2014)
  3. A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-specific Inhibitor, with Letrozole in ER+/HER2-Negative Metastatic Breast Cancer: I.A. Mayer, et al.; Clin. Cancer Res. (Epub ahead of print) (2016)
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