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BYL-719

CAT: 0013-GTR19164284-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19164284-01Size:1 g
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Description
Alpelisib (BYL-719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2. (In Vitro) :Alpelisib (BYL-719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50s~4 nM) . Alpelisib potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC50=74±15 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (≥15-fold compared with PI3Kα) .Alpelisib (BYL-719, 0-50 μM; 72 hours) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 and MOS-J in a dose-dependent manner.Alpelisib (BYL-719) significantly alters the distribution of cell cycle phases. Alpelisib (BYL-719, 25 μM; 18 hours) induces a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell lines. (In Vivo) :Alpelisib (BYL-719) (12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice; oral administration; daily) significantly reduces tumor volumes and deposition of ectopic bone matrix.Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv) .
CAS Number
1217486-61-7
Product Name Alternative
Alpelisib
Purity
>98% (HPLC)
Solubility
Ethanol: 2 mg/mL (4.53 mM) ; DMSO: 88 mg/mL (199.33 mM)
Smiles
O=C (N1[C@H] (C (N) =O) CCC1) NC2=NC (C) =C (C3=CC (C (C) (C) C (F) (F) F) =NC=C3) S2
Molecular Formula
C19H22F3N5O2S
Molecular Weight
441.47
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(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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