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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	Activity Description	PMID
Detroit562	Growth Inhibition Assay	0.1-100 Î¼M	72 h	IC50=1.10 Î¼M	25550549
SNU-1076	Growth Inhibition Assay	0.1-100 Î¼M	72 h	IC50=6.82 Î¼M	25550549
SNU-1066	Growth Inhibition Assay	0.1-100 Î¼M	72 h	IC50=1.13 Î¼M	25550549
FaDu	Growth Inhibition Assay	0.1-100 Î¼M	72 h	IC50=19.66 Î¼M	25550549
SNU1041	Growth Inhibition Assay	0.1-100 Î¼M	72 h	IC50=20.65 Î¼M	25550549
SCC25	Growth Inhibition Assay	0.1-100 Î¼M	72 h	IC50=49.30 Î¼M	25550549
BON-1	Function Assay	1/10 Î¼M	4 h	inhibits PI3K (AKT Ser308) and mTORC1/2 activities	25026292
QGP-1	Function Assay	1/10 Î¼M	4 h	inhibits PI3K (AKT Ser308) and mTORC1/2 activities	25026292
MG-63	Growth Inhibition Assay			IC50=6 Î¼Mï¼ IC90=24 Î¼M	24961790
HOS	Growth Inhibition Assay			IC50=15 Î¼Mï¼ IC90=42 Î¼M	24961790
MOS-J	Growth Inhibition Assay			IC50=10 Î¼Mï¼ IC90=36 Î¼M	24961790
POS-1	Growth Inhibition Assay			IC50=8 Î¼Mï¼ IC90=36 Î¼M	24961790
92.1	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 Î¼M	24563540
Mel270	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 Î¼M	24563540
Omm1.3	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 Î¼M	24563540
Omm1	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 Î¼M	24563540
C918	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 Î¼M	24563540
Mel290	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 Î¼M	24563540
OPM2	Growth Inhibition Assay	0.5-2.5 Î¼M	48 h	inhibits cell growth in a dose-dependent manner	24405121
OPM1	Growth Inhibition Assay	0.5-2.5 Î¼M	48 h	inhibits cell growth in a dose-dependent manner	24405121
U266	Growth Inhibition Assay	0.5-2.5 Î¼M	48 h	inhibits cell growth in a dose-dependent manner	24405121
MM1R	Growth Inhibition Assay	0.5-2.5 Î¼M	48 h	inhibits cell growth in a dose-dependent manner	24405121
MM1S	Growth Inhibition Assay	0.5-2.5 Î¼M	48 h	inhibits cell growth in a dose-dependent manner	24405121
H929	Growth Inhibition Assay	0.5-2.5 Î¼M	48 h	inhibits cell growth in a dose-dependent manner	24405121
RPMI	Growth Inhibition Assay	0.5-2.5 Î¼M	48 h	inhibits cell growth in a dose-dependent manner	24405121
SKBR3	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 35ï¼ cell growth	23918797
MDA453	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 38ï¼ cell growth	23918797
EFM192A	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 27ï¼ cell growth	23918797
AU565	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 26ï¼ cell growth	23918797
MDA361	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 44ï¼ cell growth	23918797
BT474	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 16ï¼ cell growth	23918797
HCC202	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 20ï¼ cell growth	23918797
KPL4	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 58ï¼ cell growth	23918797
NCL-N87	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 31ï¼ cell growth	23918797
UACC812	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 27ï¼ cell growth	23918797
HCC2218	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 15ï¼ cell growth	23918797
HCC1569	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 5ï¼ cell growth	23918797
OE19	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 23ï¼ cell growth	23918797
OE33	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 23ï¼ cell growth	23918797
JIMT1	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 9ï¼ cell growth	23918797
HCC1954	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 29ï¼ cell growth	23918797
NUGC4	Growth Inhibition Assay	33 Î¼M	5 d	inhibits 14ï¼ cell growth	23918797
ZR-75-30	Growth Inhibition Assay	33 Î¼M	5 d	inhibits -15ï¼ 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]