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(2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide; BYL719; NVP-BYL719

Chemical

C19H22F3N5O2S

441.5

1217486-61-7

≥95%

Solid.

Soluble in DMSO or DMF.

Manufactured by SynKinase.

Target: PI3Kalpha | Kinase Group: Lipid Kinase | Substrate: LipidClick here for Original Manufacturer Product DatasheetOur product description may differ slightly from the original manufacturers product datasheet.

STUWGJZDJHPWGZ-LBPRGKRZSA-N

AMBIENT

+4°C

-20°C

Stable for at least 2 years after receipt when stored at -20°C.

No

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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

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)

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)

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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