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Alpelisib( BYL-719)

(CAS No:1217486-61-7)
Alpelisib (BYL719) 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.
CAS No:1217486-61-7
Molecular Weight(MW):441.47
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1217486-61-7
Molecular formula(MF) C19H22F3N5O2S
Molecular Weight(MW): 441.47
Alias
Solubility
In vitro DMSO 88 mg/mL (199.33 mM)
Ethanol 2 mg/mL (4.53 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
Biological Activity
Description Alpelisib (BYL719) 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.
Targets
PI3Kα [1]
(Cell-free assay)
5 nM
In vitro

BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Detroit562 Growth Inhibition Assay 0.1-100 μM 72 h IC50=1.10 μM 25550549
SNU-1076 Growth Inhibition Assay 0.1-100 μM 72 h IC50=6.82 μM 25550549
SNU-1066 Growth Inhibition Assay 0.1-100 μM 72 h IC50=1.13 μM 25550549
FaDu Growth Inhibition Assay 0.1-100 μM 72 h IC50=19.66 μM 25550549
SNU1041 Growth Inhibition Assay 0.1-100 μM 72 h IC50=20.65 μM 25550549
SCC25 Growth Inhibition Assay 0.1-100 μM 72 h IC50=49.30 μM 25550549
BON-1 Function Assay 1/10 μM 4 h inhibits PI3K (AKT Ser308) and mTORC1/2 activities 25026292
QGP-1 Function Assay 1/10 μM 4 h inhibits PI3K (AKT Ser308) and mTORC1/2 activities 25026292
MG-63 Growth Inhibition Assay IC50=6 μM, IC90=24 μM 24961790
HOS Growth Inhibition Assay IC50=15 μM, IC90=42 μM 24961790
MOS-J Growth Inhibition Assay IC50=10 μM, IC90=36 μM 24961790
POS-1 Growth Inhibition Assay IC50=8 μM, IC90=36 μM 24961790
92.1 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Mel270 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Omm1.3 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Omm1 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
C918 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Mel290 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
OPM2 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
OPM1 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
U266 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
MM1R Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
MM1S Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
H929 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
RPMI Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
SKBR3 Growth Inhibition Assay 33 μM 5 d inhibits 35% cell growth 23918797
MDA453 Growth Inhibition Assay 33 μM 5 d inhibits 38% cell growth 23918797
EFM192A Growth Inhibition Assay 33 μM 5 d inhibits 27% cell growth 23918797
AU565 Growth Inhibition Assay 33 μM 5 d inhibits 26% cell growth 23918797
MDA361 Growth Inhibition Assay 33 μM 5 d inhibits 44% cell growth 23918797
BT474 Growth Inhibition Assay 33 μM 5 d inhibits 16% cell growth 23918797
HCC202 Growth Inhibition Assay 33 μM 5 d inhibits 20% cell growth 23918797
KPL4 Growth Inhibition Assay 33 μM 5 d inhibits 58% cell growth 23918797
NCL-N87 Growth Inhibition Assay 33 μM 5 d inhibits 31% cell growth 23918797
UACC812 Growth Inhibition Assay 33 μM 5 d inhibits 27% cell growth 23918797
HCC2218 Growth Inhibition Assay 33 μM 5 d inhibits 15% cell growth 23918797
HCC1569 Growth Inhibition Assay 33 μM 5 d inhibits 5% cell growth 23918797
OE19 Growth Inhibition Assay 33 μM 5 d inhibits 23% cell growth 23918797
OE33 Growth Inhibition Assay 33 μM 5 d inhibits 23% cell growth 23918797
JIMT1 Growth Inhibition Assay 33 μM 5 d inhibits 9% cell growth 23918797
HCC1954 Growth Inhibition Assay 33 μM 5 d inhibits 29% cell growth 23918797
NUGC4 Growth Inhibition Assay 33 μM 5 d inhibits 14% cell growth 23918797
ZR-75-30 Growth Inhibition Assay 33 μM 5 d inhibits -15% cell growth 23918797

... Click to View More Cell Line Experimental Data

In vivo BYL719(>270 mg/d) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC in human. BYL719(270mg/d) shows first signs of clinical efficacy include 1 confirmed partial response in a patient with ER+ breast cancer, and significant PET responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17 evaluated patients. [1]