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首页-抗体药物偶连体和PROTACs-PROTAC-SR-1114
SR-1114

Chemical Structure : SR-1114

CAS No.: 2769141-82-2

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SR-1114 (SR1114)

货号: PC-72572Not For Human Use, Lab Use Only.

SR-1114 (SR1114) is a first-in-class ENL PROTAC degarder based on SR-0813 that binds to the E3 substrate adapter cereblon (CRBN), elicits rapid CRBN-dependent degradation of ENL with DC50 of 150 nM in MV4;11 cells.

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

    生物&药学活性

    SR-1114 (SR1114) is a first-in-class ENL degarder (PROTAC) based on SR-0813 that binds to the E3 substrate adapter cereblon (CRBN), elicits rapid CRBN-dependent degradation of ENL with DC50 of 150 nM in MV4;11 cells.
    After withdrawal of SR-1114 from cells, ENL is rapidly resynthesized within 24 h.
    ENL is also degraded by SR-1114 in MOLM-13 (DC50=311 nM) and OCI/AML-2 (DC50= 1.65 uM) cell lines.
    SR-1114 treatment resulted in the preferential suppression of multiple ENL target genes, including HOXA10, MYC, MYB, FLT3, ZEB2, and SATB1, closely replicating the transcriptional consequences of dTAG-mediated ENL degradation.
    The 16 h SR-1114 treatment (10 uM) also increased the abundance of the myeloid differentiation marker, CD11b, in agreement with the proposed role for ENL in preventing the terminal differentiation of AML cells.

    物理化学性质&存储条件

    分子量 830.87
    分子式 C39H42N8O11S
    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-Cyclobutyl-2-(3-((N-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)ethoxy)ethoxy)ethyl)sulfamoyl)amino)phenyl)imidazo[1,2-a]pyridine-6-carboxamide

    参考文献

    1. Garnar-Wortzel L, et al. ACS Cent Sci. 2021 May 26;7(5):815-830.

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