BYL719

BYL719 is an inhibitor of phosphoinositide 3-kinase alpha (PI3Kalpha, IC50s = 4.6, 4, and 4.8 nM for wild-type, E545K mutant, and H1047R mutant PI3K, respectively). It is selective for PI3Kalpha over PI3Kbeta, PI3Kdelta, PI3Kgamma, and PI4Kbeta (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 PI3Kalpha-dependent Rat1-myr-p110alpha 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.Formal Name: (2S)-N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide. CAS Number: 1217486-61-7. Synonyms: Alpelisib, NVP-BYL719. Molecular Formula: C19H22F3N5O2S. Formula Weight: 441.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 317 nm. SMILES: CC(C)(C(F)(F)F)C1=NC=CC(C2=C(C)N=C(NC(N3[C@H](C(N)=O)CCC3)=O)S2)=C1. InChi Code: InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1. InChi Key: STUWGJZDJHPWGZ-LBPRGKRZSA-N.