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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Discoidin Domain Receptor (DDR)-KI-301690
KI-301690

Chemical Structure : KI-301690

CAS No.: 2757924-20-0

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KI-301690 (KI 301690)

货号: PC-49385Not For Human Use, Lab Use Only.

KI-301690 (KI 301690) is a novel potent, specific DDR1 inhibitor, synergized with gemcitabine to suppress the growth of pancreatic cancer cells.

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

    生物&药学活性

    KI-301690 (KI 301690) is a novel potent, specific DDR1 inhibitor, synergized with gemcitabine to suppress the growth of pancreatic cancer cells.
    KI-301690 displayed the strongest binding affinity for DDR1 (percent of control [POC] = 9) through a panel of 50 oncogenic kinases at 1 uM.
    KI-301690 inhibited p-DDR1 expression in a dose dependent manner in pancreatic cancer cells.
    KI-301690 (1-20 uM) decreased proliferative ability in PANC-1 cells in a dose and time-dependent manner.
    KI-301690 effectively inhibited expressions of major ECM components by binding collagen, increased gemcitabine sensitivity when used in combination.
    KI-301690 effectively blocked DDR1/PYK2/FAK signaling in pancreatic cancer cells combined with gemcitabine.
    KI-301690 (30 mg/kg) and gemcitabine (3 mg/kg) for 45 days displays antitumor effects in a pancreatic cancer xenograft model, effectively decreased the expression of p-DDR, p-PYK2, and p-FAK.

    物理化学性质&存储条件

    分子量 459.554
    分子式 C25H29N7O2
    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

    9-(2-aminobenzyl)-2-((4-(2-(piperidin-1-yl)ethoxy)phenyl)amino)-7,9-dihydro-8H-purin-8-one

    参考文献

    1. Ko S, et al. Am J Cancer Res. 2022 Sep 15;12(9):4326-4342.

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