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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-LL-00071210
LL-00071210

Chemical Structure : LL-00071210

CAS No.: 1855080-61-3

LL-00071210 (LL00071210)

货号: PC-38789Not For Human Use, Lab Use Only.

LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.
    LL-00071210 demonstrated specific inhibitory action against PI3Kδ isoform with >100-fold selectivity over closely related PI3Kγ isoform.
    LL-00071210 potently inhibited IL2 (A), TNF-α (B) and IFN-γ (C) secretion from human PBMC's on stimulation with anti-CD3/CD28.
    LL-00071210 showed acceptable pharmacokinetic profile with good oral bioavailability in rodents.
    In rodent arthritis model, treatment with LL-00071210 led to dosedependent inhibition of disease severity, along with histopathological
    improvements in joint structure.
    LL-00071210 also demonstrated good combination potential with methotrexate at sub-therapeutic doses.

    物理化学性质&存储条件

    分子量 400.417
    分子式 C22H17FN6O
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (S)-4-amino-6-((1-(7-fluoro-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile

    参考文献

    1. Vijay Kanoje, et al. Eur J Pharmacol. 2022 May 27;175054.

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