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LC-1-40

Chemical Structure : LC-1-40

CAS No.:

LC-1-40 (NUDT1 degrader LC-1-40)

货号: PC-21992Not For Human Use, Lab Use Only.

LC-1-40 is a potent, specific NUDT1 (MTH1) degrader/PROTAC with DC50 of 0.97 nM in SHEP MYCN-ER cells, Dmax value of 96% at 50  nM.

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

    生物&药学活性

    LC-1-40 is a potent, specific NUDT1 (MTH1) degrader/PROTAC with DC50 of 0.97 nM in SHEP MYCN-ER cells, Dmax value of 96% at 50  nM.
    LC-1-40 induced a dose- and time-dependent NUDT1 degradation in SHEP MYCN-ER cells.
    LC-1-40 causes minimal changes in NUDT1 mRNA levels in Kelly and SF188 cells.
    LC-1-40 markedly increases 8-oxo-dG levels and selectively induces SHEP cell death upon 4-OHT induction of MYCN hyperactivation, elicits MYC(N)-driven synthetic lethality
    LC-1-40 (IP, 30 mg/kg) caused a remarkable intratumoral NUDT1 depletion within 1 h in patient-derived xenografts using MYCN-amplified T409 and MYCN-nonamplified T423 primary neuroblastoma tumors.
    LC-1-40 (30 mg/kg) selectively impeded the growth of MYCN-amplified T409 tumors.

    物理化学性质&存储条件

    分子量 844.97
    分子式 C49H48N8O6
    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

    N-cyclopropyl-6-(4-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidine-1-carbonyl)phenyl)-4-(phenylamino)quinoline-3-carboxamide

    参考文献

    1. Minhui Ye, et al. Nat Commun. 2024 Mar 16;15(1):2377.

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