Alpelisib (BYL719)

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Purity: >97%

Keywords

Alpelisib BYL719 1217486-61-7

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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 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

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AKT(S473) / p-AKT(T308); p100β / p110α / p85 / p-ERBB3(Y1289); p-HER2 / IGF-1R; pS6 (Ser235-236); PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD;	25544637 27048245 27604488
Growth inhibition assay	Cell viability;	27602501
Immunofluorescence	LC3;	26637440

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]

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