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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Farnesyl transferase (FTase)-Darlifarnib
Darlifarnib

Chemical Structure : Darlifarnib

CAS No.: 2939824-30-1

Darlifarnib (KO-2806, KO2806)

货号: PC-24121Not For Human Use, Lab Use Only.

Darlifarnib (KO-2806, KO2806) is a potent, specific farnesyltransferase (FTase) inhibitor with IC50 of 2.4 nM, while sparing activity of GGTase (IC50>1 uM).

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

    生物&药学活性

    Darlifarnib (KO-2806, KO2806) is a potent, specific farnesyltransferase (FTase) inhibitor with IC50 of 2.4 nM, while sparing activity of GGTase (IC50>1 uM).
    KO-2806 enhances adagrasib's inhibition of mTORC1 signaling by blocking RHEB farnesylation.
    KO-2806 deepens responses of NSCLC models to KRASG12C inhibition and inhibits mTORC1 in vivo.
    KO-2806 blocks rebound of mTOR signaling and deepens antitumor responses to mutant-selective and pan-RAS inhibitors in colorectal cancer.
    KO-2806 resensitizes refractory or relapsing NSCLC tumors to mutant-selective or pan-RAS inhibition.

    物理化学性质&存储条件

    分子量 468.52
    分子式 C29H20N6O
    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)-3-amino-3-(1-methyl-1H-imidazol-5-yl)-6-oxa-2(4,6)-quinolina-1,4(1,3)-dibenzenacyclohexaphane-22,44-dicarbonitrile

    参考文献

    1. Patent WO2024137751 A1.

    2. Patent WO2024233539 A1.

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