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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-Luxeptinib
Luxeptinib

Chemical Structure : Luxeptinib

CAS No.: 1616428-23-9

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Luxeptinib (CG-806, CG806)

货号: PC-72114Not For Human Use, Lab Use Only.

Luxeptinib (CG-806) is an orally bioavailable multikinase inhibitor with nanomolar potency against BTK, FLT3, TRK, STE/MAPK and Aurora kinase clusters.

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

    生物&药学活性

    Luxeptinib (CG-806) is an orally bioavailable multikinase inhibitor with nanomolar potency against BTK, FLT3, TRK, STE/MAPK and Aurora kinase clusters.
    Luxeptinib (CG-806) is cytotoxic to primary malignant cells obtained from patients with AML, ALL, and CLL at lower concentrations than other BTK and FLT3 inhibitors, and has activity in AML and lymphoma xenografts at concentrations attainable in patients.
    Luxeptinib inhibited the release of IL-1β, IL-6 and TNFα from THP-1 monocytes and macrophages at concentrations of 1 uM or above.
    Luxeptinib (CG-806) also inhibits the kinases p38MAPK, ERK1/2, SAPK/JNK and activation of transcription factor NF-κBp65 with a concentration profile similar to its inhibition of cytokine release.

    物理化学性质&存储条件

    分子量 495.438
    分子式 C25H17F4N5O2
    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

    Urea, N-[4-[2,3-dihydro-7-(5-methyl-1H-imidazol-2-yl)-1-oxo-1H-isoindol-4-yl]-3-fluorophenyl]-N'-(2,4,6-trifluorophenyl)-

    参考文献

    1. Zheng TJ, et al. Am J Physiol Cell Physiol. 2021 May 1;320(5):C902-C915.

    2. Sonowal H, et al. Biochem Pharmacol. 2022 Jan;195:114861.

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