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Alpelisib (BYL719)

Alpelisib (BYL719)

Item no.	S2814-10000
Manufacturer	Selleckchem
CASRN	1217486-61-7
Amount	10 g
Quantity options	10mg 100mg 1g 10 g 10mM/1mL 20 mg 200 mg 5mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer
Type	Inhibitors
Specific against	other
Smiles	CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1217486-61-7'
Similar products	BYL719
Available
Manufacturer - Targets	PI3K
Storage Conditions	2 years -80 in solvent
Molecular Weight	441, 47
Clinical Trials	BYL719 is currently in Phase II clinical trial in adult patients with selected advanced solid tumors.
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]
Solubility (25C)	DMSO 88 mg/mL, Water <1 mg/mL, Ethanol 5 mg/mL
Information	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.
Chemical Name	1, 2-Pyrrolidinedicarboxamide, N1-[4-methyl-5-[2-(2, 2, 2-trifluoro-1, 1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-, (2S)-

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