Alpelisib (BYL719)

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) Structure
Alpelisib (BYL719) Chemical Properties
density 1.391
storage temp. Store at -20°C
solubility ≥22.07 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form White solid.
pka6.29±0.70(Predicted)
Safety Information
HS Code 29341000
MSDS Information
Alpelisib (BYL719) Usage And Synthesis
DescriptionBYL719 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.
DefinitionChEBI: (2S)-N1-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)-4-pyridinyl]-2-thiazolyl]pyrrolidine-1,2-dicarboxamide is a proline derivative.
targetPI3Kα
references1. 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.
BEZ235 (NVP-BEZ235, Dactolisib) 4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- D-ERYTHRO-SPHINGOSINE Glucagon Receptor Antagonist I Neratinib BI 2536 N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide hydrochloride Trametinib CAL-101 Tubastatin A hydrochloride Fluoxetine hydrochloride CX-4945 N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide MK-2206 2HCl BML-275 Selumetinib BKM120 (NVP-BKM120, Buparlisib) KU-55933

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