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SynKinase
Alpelisib
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | (2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide; BYL719; NVP-BYL719 |
| Product Type | Chemical |
| Properties | |
| Formula | C19H22F3N5O2S |
| MW | 441.5 |
| CAS | 1217486-61-7 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO or DMF. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data | Target: PI3Kalpha | Kinase Group: Lipid Kinase | Substrate: Lipid |
| InChi Key | STUWGJZDJHPWGZ-LBPRGKRZSA-N |
| 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. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
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
- 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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