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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-AB801
AB801

Chemical Structure : AB801

CAS No.: 3024588-48-2

AB801 (Ligritinib, AB-801)

货号: PC-24678Not For Human Use, Lab Use Only.

Ligritinib (AB801) is a highly potent, selective, and orally bioavailable AXL kinase inhibitor with biochemical IC50 of 1.8 nM, and cellular pALX IC50 of 68 nM in ELISA assays.

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

    生物&药学活性

    Ligritinib (AB801) is a highly potent, selective, and orally bioavailable AXL kinase inhibitor with biochemical IC50 of 1.8 nM, and cellular pALX IC50 of 68 nM in ELISA assays.
    AB801 showed extremely high levels of selectivity against MERTK and TYRO3, and only one kinase (DRAK1) showing a <100-fold selectivity ratio against AXL against the human kinome.
    30 mg/kg AB801 in combination with sunitinib exhibited a statistically significant reduction in tumor volume in human 786-O clear-cell renal cell carcinoma (ccRCC) xenograft model

    物理化学性质&存储条件

    分子量 528.66
    分子式 C33H32N6O
    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

    6-[(7S)-3-[3-[5-(3-Methylpyridin-2-yl)pyridin-2-yl]-1H-pyrazolo[3,4-b]pyridin-5-yl]-6,7,8,9-tetrahydro-5H-benzo[7]annulen-7-yl]-3-oxa-6-azabicyclo[3.1.1]heptane

    参考文献

    1. Miles DH, et al. J Med Chem. 2025 May 23. doi: 10.1021/acs.jmedchem.5c00239.

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