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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-ERAS-5024
ERAS-5024

Chemical Structure : ERAS-5024

CAS No.:

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ERAS-5024 (ERAS5024)

货号: PC-21263Not For Human Use, Lab Use Only.

ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.

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

    生物&药学活性

    ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.
    ERAS-5024 displays >100-fold cellular selectivity against WT KRAS.
    ERAS-5024 demonstrates potent in vitro anti-proliferative activities in a panel of cell lines harboring G12D mutation (AsPC-1, IC50=3.5 nM).
    ERAS-5024 is 3-fold more potent than MRTX1133 in the in vitro three-dimensional Cell-Titer Glo (3D CTG) assay with the AsPC-1 cell line, demonstrates more potent in vivo activity than MRTX1133.
    ERAS-5024 at 3 and 10 mg/kg inhibited tumor growth by 51% and 77%, respectively, in the KRAS G12D mutant pancreatic ductal adenocarcinoma (PDAC) xenograft model AsPC-1.

    物理化学性质&存储条件

    分子量 672.69
    分子式 C33H30F6N6OS
    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

    (4S)-4-(4-(8-azabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-6-(trifluoromethyl)quinazolin-7-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile

    参考文献

    1. Cheng H, et al. ACS Med Chem Lett. 2023 Sep 18;14(10):1351-1357.

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