Alpelisib - CAS 1217486-61-7
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Alpelisib
Catalog Number:
B0084-457654
Synonyms:
BYL-719; BYL719; BYL 719; Alpelisib;
CAS Number:
1217486-61-7
Description:
Alpelisib, also known as BLY719, is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BYL719 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.
COA:
Inquire
MSDS:
Inquire
Targets:
PI3K
Current Developer:
Novartis.
Catalog Number Size Price Stock Quantity
B0084-457654 100 mg $199 In stock
Bulk Inquiry
Chemical Structure
CAS 1217486-61-7 Alpelisib

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Reference Reading


1.Absorption, distribution, metabolism, and excretion of [(14)C]BYL719 (alpelisib) in healthy male volunteers.
James A1, Blumenstein L2, Glaenzel U3, Jin Y3, Demailly A3, Jakab A3, Hansen R2, Hazell K2, Mehta A4, Trandafir L5, Swart P3. Cancer Chemother Pharmacol. 2015 Oct;76(4):751-60. doi: 10.1007/s00280-015-2842-4. Epub 2015 Aug 8.
PURPOSE: To determine the pharmacokinetics of the p110α-selective inhibitor alpelisib (BYL719) in humans, to identify metabolites in plasma and excreta, and to characterize pathways of biotransformation.
2.A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-specific Inhibitor, with Letrozole in ER+/HER2-Negative Metastatic Breast Cancer.
Mayer IA1, Abramson V2, Formisano L3, Balko JM3, Estrada MV4, Sanders M5, Juric D6, Solit D7, Berger MF8, Won H8, Li Y9, Cantley LC10, Winer EP11, Arteaga CL3. Clin Cancer Res. 2016 Apr 28. pii: clincanres.0134.2016. [Epub ahead of print]
PURPOSE: Alpelisib, a selective oral inhibitor of the class I PI3K catalytic subunit p110α, has shown synergistic anti-tumor activity with endocrine therapy against ER+/PIK3CA mutated breast cancer cells. This phase Ib study evaluated alpelisib plus letrozole's safety, tolerability and preliminary activity in patients with metastatic ER+ breast cancer refractory to endocrine therapy.