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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-PF-06651600 malonate
PF-06651600 malonate

Chemical Structure : PF-06651600 malonate

CAS No.: 2140301-97-7

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PF-06651600 malonate (Ritlecitinib, PF06651600 malonate)

货号: PC-62334Not For Human Use, Lab Use Only.

PF-06651600 malonate (Ritlecitinib) is a novel potent, selective JAK3 inhibitor with IC50 of 0.346 nM, displays >1,000-fold selectivity over JAK1 and JAK2.

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

    生物&药学活性

    PF-06651600 malonate (Ritlecitinib) is a novel potent, selective JAK3 inhibitor with IC50 of 0.346 nM, displays >1,000-fold selectivity over JAK1 and JAK2.
    PF-06651600 inhibits Th1 and Th17 cell differentiation and function, reduces disease pathology in rat adjuvant-induced arthritis as well as in mouse experimental autoimmune encephalomyelitis models.
    PF-06651600 selectively targets γc cytokine pathways while preserving JAK1-dependent anti-inflammatory signaling such as the IL-10 suppressive functions following LPS treatment in macrophages and the suppression of TNFα and IL-1β production in IL-27-primed macrophages.

    物理化学性质&存储条件

    分子量 389.412
    分子式 C18H23N5O5
    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

    1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one malonate

    参考文献

    1. Telliez JB, et al. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451.

    2. Thorarensen A, et al. J Med Chem. 2017 Mar 9;60(5):1971-1993.

    3. Robinette ML, et al. Mucosal Immunol. 2017 May 17. doi: 10.1038/mi.2017.38.

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