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| Alpelisib (BYL719) Basic information |
| Product Name: | Alpelisib (BYL719) | | Synonyms: | (2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide;BYL-719;BYL-719 /BYL719;Alpelisib;BLV-719;(S)-N1-(4-Methyl-5-(2-(1,1,1-trifluoro-2-Methylpropan-2-yl)pyridin-4-yl)thiazol-2-yl)pyrrolidine-1,2-dicarboxaMide;ALPELISIB;BYL-719; BYL 719;CS-614 | | CAS: | 1217486-61-7 | | MF: | C19H22F3N5O2S | | MW: | 441.47 | | EINECS: | | Product Categories: | Inhibitors;Akt;PI3K/Akt/mTOR;mTOR;PI3K;Api;API | | Mol File: | 1217486-61-7.mol |
| Alpelisib (BYL719) Chemical Properties |
| density | 1.391 | | solubility | ≥22.07 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | White solid. | | pka | 6.29±0.70(Predicted) |
| Alpelisib (BYL719) Usage And Synthesis |
| Description | BYL719 is an inhibitor of phosphoinositide 3-kinase α (PI3Kα; IC50s = 4.6, 4, and 4.8 nM for wild-type, E545K mutant, and H1047R mutant PI3K, respectively). It is selective for PI3Kα over PI3Kβ, PI3Kδ, PI3Kγ, and PI4Kβ (IC50s = 1,156, 290, 250, and 581 nM, respectively), as well as VPS34, mTOR, DNA-PK, and ATR (IC50s = >9,100 nM for all). BYL719 (12.5, 25, and 50 mg/kg) reduces tumor volume in a PI3Kα-dependent Rat1-myr-p110α mouse xenograft model. It also reduces tumor burden in THP-1 acute myeloid leukemia (AML) and MCF-7 breast cancer mouse xenograft models. Formulations containing BYL719 have been used in the treatment of advanced or metastatic breast cancer. | | Uses | (2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide is a newly developed phosphatidylinositol-3-kinase (PI3K) inhibitor and a mTOR inhibit
or for the treatment of proliferative diseases. | | Uses | (2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide is a newly developed phosphatidylinositol-3-kinase (PI3K) inhibitor and a mTOR inhibitor for the treatment of proliferative diseases. | | references | 1. furet p, guagnano v, fairhurst ra et al. discovery of nvp-byl719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. bioorg med chem lett 2013; 23: 3741-3748. 2. azab f, vali s, abraham j et al. pi3kca plays a major role in multiple myeloma and its inhibition with byl719 decreases proliferation, synergizes with other therapies and overcomes stroma-induced resistance. br j haematol 2014; 165: 89-101. 3. juric d, argiles g, burris h et al. phase i study of byl719, an alpha-specific pi3k inhibitor, in patients with pik3ca mutant advanced solid tumors: preliminary efficacy and safety in patients with pik3ca mutant er-positive (er+) metastatic breast cancer (mbc). cancer res 2012; 72: p6-10. |
| Alpelisib (BYL719) Preparation Products And Raw materials |
| Raw materials | Acetamide,N-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]--->4-Methyl-2-(1,1,1-trifluoro-2-Methylpropan-2-yl)pyridine-->4-broMo-2-(1,1,1-trifluoro-2-Methylpropan-2-yl)pyridine-->4-methyl-2-(2,2,2-trifluoro-1-methyl-1-trimethylsilanyloxy-ethyl)pyridine-->1,1,1-trifluoro-2-(4-methylpyridin-2-yl)propan-2-ol-->1,1,1-trifluoro-2-(4-methylpyridin-2-yl)propan-2-yl methanesulfonate-->N-(4-Methyl-5-(2-(1,1,1-trifluoro-2-Methylpropan-2-yl)pyridin-4-yl)thiazol-2-yl)-1H-iMidazole-1-carboxaMide-->phenyl 4-methyl-5-(2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)thiazol-2-ylcarbamate-->L-Prolinamide-->1-(2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)propan-2-one-->2-Acetyl-4-methylpyridine-->2,4-Lutidine |
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