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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Src-iHCK-37
iHCK-37

Chemical Structure : iHCK-37

CAS No.: 516478-09-4

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iHCK-37 (ASN05260065)

货号: PC-72678Not For Human Use, Lab Use Only.

iHCK-37 (ASN05260065) is a potent and selective Hck inhibitor with Ki of 0.22 uM.

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

    生物&药学活性

    iHCK-37 (ASN05260065) is a potent and selective Hck inhibitor with Ki of 0.22 uM.
    iHCK-37 displays high selectivity against a panel of kinases including other Src family members (Blk, Fgr, Fyn, cSRC, Lck, Lyn, Syk, and Yes), tyrosine kinases (Abl and Abl-T315I), as well as some kinases important for HIV1 (CDK9, FAK, Itk, JAK3, Ron).
    iHCK-37 has anti-neoplastic activity in leukemia cells without altering apoptosis and survival rate of normal cells.
    iHCK-37 demonstrates additive effects against leukemia cells combined with 5-Azacytidine or Cytarabine, reduces the activation of oncogenic pathways, MAPK/ERK and PI3K/AKT, leading to reduction of ERK and AKT phosphorylation, and increases BAX and decreased BCL-XL protein expression.
    iHCK-37 exhibits antiproliferative activity profile against the human leukemia cell line KU-812 (IC50=66.5 uM).
    iHCK-37 also blocks HIV-1 replication with EC50 of 12.9 uM.

    物理化学性质&存储条件

    分子量 544.73
    分子式 C30H32N4O2S2
    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-[2-(4-Morpholinyl)phenyl]-2-[[5,6,7,8-tetrahydro-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]thio]acetamide

    参考文献

    1. Roversi FM, et al. Biochim Biophys Acta Mol Basis Dis. 2017 Feb;1863(2):450-461.

    2. Roversi FM, et al. Cancer Immunol Immunother. 2022 Jan 18.

    3. Cristina Tintori, et al. ChemMedChem. 2013 Aug;8(8):1353-60.

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