A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice

BYL719 – 10 mg

Brand:
Cayman
CAS:
1217486-61-7
Storage:
-20
UN-No:
Non-Hazardous - /

BYL719 is a selective inhibitor of phosphoinositide 3-kinase α (PI3Kα) that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM).{28003,28002} It is less effective against PI3K isoforms β, γ, and δ (IC50s = 1,156, 250, and 290 nM) as well as a range of related kinases.{28003} BYL719 is effective in vivo, as it dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice.{28003} Effectiveness against wild type and mutant PI3Kα-dependent tumors may be augmented by combination therapy with inhibitors of other kinases.{28000,28004,28001} Combination therapy may be necessary, as loss of downstream pathway components can confer clinical resistance to BYL719.{28331}  

 

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Description

A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors

Formal name: (2S)-N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide

Synonyms:  Alpelisib|NVP-BYL719

Molecular weight: 441.5

CAS: 1217486-61-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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