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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-YLIU-5-162-1
YLIU-5-162-1

Chemical Structure : YLIU-5-162-1

CAS No.: 2417685-83-5

YLIU-5-162-1

货号: PC-20901Not For Human Use, Lab Use Only.

YLIU-4-105-1 is a novel type II JAK2 inhibitor, binds to JAK2 kinase domain (JH1), show potential for overcoming acquired resistance to ruxolitinib.

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

    生物&药学活性

    YLIU-4-105-1 is a novel type II JAK2 inhibitor, binds to JAK2 kinase domain (JH1), show potential for overcoming acquired resistance to ruxolitinib.
    YLIU-4-105-1 shows pure JAK2 selectivity, inhibits pSTAT1 (Y701) and in some cases pERK1/2 (T202/Y204) to varying extents, but does not inhibit pAKT (T308).
    YLIU-4-105-1 is more potent against JAK2 V617F-dependent SET2 cells.
    YLIU-4-105-1 (50 mg/kg or 75 mg/kg, IP daily) shows abdominal ascites, intraabdominal drug precipitate, and dilated loops of bowel on rhEPO-induced polycythemia mouse model.

    物理化学性质&存储条件

    分子量 605.67
    分子式 C32H34F3N7O2
    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-(2-(cyclopropanecarboxamido)imidazo[1,2-b]pyridazin-6-yl)-N-(3-((4-ethylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-4-methylbenzamide

    参考文献

    1. Matthew L Arwood, et al. Cell Chem Biol. 2023 Jun 15;30(6):618-631.e12.

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