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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-R992
R992

Chemical Structure : R992

CAS No.: 2171523-99-0

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R992 (R-992)

货号: PC-49565Not For Human Use, Lab Use Only.

R992 (MERTK inhibitor) is a novel potent, selective and orally bioavailable inhibitor of Mer tyrosine kinase (MerTK) with IC50 of 18 nM in ADP-Glo assays.

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

    生物&药学活性

    R992 (MERTK inhibitor) is a novel potent, selective and orally bioavailable inhibitor of Mer tyrosine kinase (MerTK) with IC50 of 18 nM in ADP-Glo assays.
    R992 exhibits seven to eight-fold selectivity over AXL and TYRO3 in biochemical assays.
    R992 docked in MERTK and the H-bonds R992 forms with three residues in the ATP pocket (MET-647, PRO-672, and ASP-741).
    R992 blocks MERTK phosphorylation in HUVEC with EC50 of 32 nM, effectively blocks MERTK phosphorylation in human and murine cells.
    R992 (60 mg/kg, orally 2x/day) dose-dependently increases bone nodule formation and increases osteoblast differentiation markers Alpl, SP7, and Runx2.
    Treatment with R992 of osteoblasttumor cultures could decrease F-actin content, stress fiber formation, and promoted osteoblast spreading.
    R992 inhibits multiple myeloma tumor progression and bone disease in U266 myeloma mouse models.
    R992 inhibits tumor progression and cancer-induced bone loss in breast- and lung cancer bone metastasis in the lung- and breast cancer models.

    物理化学性质&存储条件

    分子量 478.641
    分子式 C27H38N6O2
    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

    3-(butylamino)-5-((1r,4r)-4-hydroxycyclohexyl)-8-((4-methylpiperazin-1-yl)methyl)pyrimido[4,5-c]isoquinolin-6(5H)-one

    参考文献

    1. Engelmann J, et al. Nat Commun. 2022 Dec 12;13(1):7689.

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