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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-DSF-102
DSF-102

Chemical Structure : DSF-102

CAS No.: 197585-01-6

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DSF-102 (DSF102)

货号: PC-49235Not For Human Use, Lab Use Only.

DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of 13.2 uM.

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

    生物&药学活性

    DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of 13.2 uM.
    DSF-102 demonstrated a strong inhibitory effect on AKT signaling at 50 uM in A549 cells, A549 cells showed EGFR accumulation on the membrane and in the perinuclear region from early to later time of stimulation.
    DSF-102 (50 µM) promoted the formation of numerous clustered vesicles expressing EEA1 (Early Endosome Antigen 1) and increased the expression of LAMP1 (Lysosomal-Associated Membrane Protein 1).
    DSF-102 showed cytotoxic effects against human triple negative breast MDA-MB-231 and human colon HCT-15 cancer cells ( KRAS mutation at codon 13), overexpressing EGFR, with IC50 of 41.3 uM and 12.8 uM, respectively.

    物理化学性质&存储条件

    分子量 335.24
    分子式 C15H8F3N3O3
    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

    (E)-5-nitro-3-((3-(trifluoromethyl)phenyl)imino)indolin-2-one

    参考文献

    1. Rosa Di Liddo, et al. Cancers (Basel). 2022 Jul 27;14(15):3647.

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