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Chemical Structure : Alpelisib
CAS No.: 1217486-61-7
Catalog No.: PC-20590Not For Human Use, Lab Use Only.
Alpelisib (NVP-BYL719, BYL719) is ia potent, selective, and orally active PI3Kα inhibitor with IC50 of 5 nM, >50-fold selectivity over p110γ/p110δ/p110β.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $258 | In stock | |
| 100 mg | $698 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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Alpelisib (NVP-BYL719, BYL719) is ia potent, selective, and orally active PI3Kα inhibitor with IC50 of 5 nM, >50-fold selectivity over p110γ/p110δ/p110β.
Alpelisib (BYL719) potently inhibits PIK3CA somatic mutations (H1047R, E545K) with IC50 of 4 nM.
Alpelisib (BYL719) potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC50=74 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (>15-fold).
Alpelisib (BYL719) (0-50 uM) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 and MOS-J in a dose-dependent manner.
Alpelisib (BYL719) potently suppresses proliferation and PI3K signaling in human breast cancer cells harboring PIK3CA(H1047R) in combination with lapatinib.
Alpelisib (BYL719) inhibits growth factor-independent KRASG12D BM colony formation and sensitizes cells to a low dose of the MEK inhibitor MEK162.
| M.Wt | 441.47 | |
| Formula | C19H22F3N5O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-N1-(4-methyl-5-(2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)thiazol-2-yl)pyrrolidine-1,2-dicarboxamide |
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1. Furet P, et al. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8.
2. Gobin B, et al. Int J Cancer. 2015 Feb 15;136(4):784-96.
3. Fritsch C, et al. Mol Cancer Ther. 2014 May;13(5):1117-29.
4. Elkabets M, et al. Sci Transl Med. 2013 Jul 31;5(196):196ra99.
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