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Alpelisib (BYL719)

Alpelisib (BYL719)

Manufacturer	Selleckchem
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer
Type	Inhibitors
Specific against	other
Amount	20 mg
Item no.	S2814-20
Targets	PI3K
CASRN	1217486-61-7
eClass 6.1	30220300
eClass 9.0	32160605
Available
Chemical Name	1, 2-Pyrrolidinedicarboxamide, N1-[4-methyl-5-[2-(2, 2, 2-trifluoro-1, 1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-, (2S)-
Clinical Trials	BYL719 is currently in Phase II clinical trial in adult patients with selected advanced solid tumors.
Description	BYL719 strongly and selectively inhibits the PI3Kalpha.
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]
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]
Molecular Weight (MW)	441, 47
Picture ChemicalStructure Description	BYL719 Chemical Structure
Solubility (25C)	DMSO 88 mg/mL, Water <1 mg/mL, Ethanol 5 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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Amount: 20 mg

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Delivery expected until 5/16/2024