2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β; exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R).ETP-46321, has been pro?led and shown to be a potent PI3K a and d inhibitor, highly selective versus mTOR and 288 representative kinases. The compound demonstrated a good pharmacokinetic profile in mice and was selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-Ras G12V oncogenic mutation, showing significant tumor growth inhibition (ca. 51%), and reduction of the tumor metabolic activity as measured by PET techniques.
