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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MAP4K-BAY-405
BAY-405

Chemical Structure : BAY-405

CAS No.: 2442532-66-1

BAY-405 (BAY405)

货号: PC-49661Not For Human Use, Lab Use Only.

BAY-405 (BAY405) is a potent, selective MAP4K1 (HPK1) inhibitor with IC50 of 6 nM in binding competition assays.

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

    生物&药学活性

    BAY-405 (BAY405) is a potent, selective MAP4K1 (HPK1) inhibitor with IC50 of 6 nM in binding competition assays.
    BAY-405 inhibits SLP76 phosphorylation with submicromolar potency (IC50=0.63 uM) and shows good kinase selectivity.
    BAY-405 enhances T-cell immunity and overcomes the suppressive impact of PGE2, TGFβ and CD4+ T-regulatory cells.
    BAY-405 demonstrated single-agent efficacy in syngeneic EMT6 breast and B16-OVA melanoma mouse models, as well as benefits when combined with anti-PDL1 Ab in the B16-OVA model.

    物理化学性质&存储条件

    分子量 522.48
    分子式 C25H23F5N4O3
    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-(3,5-difluoro-4-((3-(1-(trifluoromethyl)cyclopropyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2,9-dioxa-4-azaspiro[5.5]undec-3-en-3-amine

    参考文献

    1. Leder, G. et al. Enhancement of anti-tumor T-cell immunity by means of an oral small molecule targeting the intracellular immune checkpoint MAP4K1. Cancer Res. 81 (Suppl. 13), Abstr. 1722 (2021).
    2. Mowat J, et al. J Med Chem. 2024 Sep 27. doi: 10.1021/acs.jmedchem.4c01325.

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