InformationAlpelisib (BYL719) is a potent and selectivePI3Kαinhibitor withIC50of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.In vitroBYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway.In vivoBYL719(>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.Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C19H22F3N5O2S Molecular Weight: 441.47
- UPC:
- 12352005
- Condition:
- New
- Availability:
- 2 weeks
- Weight:
- 0.85 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- A408653-1ml
- CAS:
- 1217486-61-7
- Product Size:
- 1ml
