Comparison

Alpelisib (BYL719) European Partner

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
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)-

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 10 g
Available: In stock
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