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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-HM5023507
HM5023507

Chemical Structure : HM5023507

CAS No.: 1549766-06-4

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HM5023507 (HM 5023507)

货号: PC-38687Not For Human Use, Lab Use Only.

HM5023507 is a potemt, selective, orally active dual PI3Kδ/γ inhibitor with IC50 of 4 nM and 5 nM for p110γ and p110δ, respectively.

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

    生物&药学活性

    HM5023507 is a potemt, selective, orally active dual PI3Kδ/γ inhibitor with IC50 of 4 nM and 5 nM for p110γ and p110δ, respectively.
    HM5023507 displays 100‐fold selectivity against PI3Kα and PI3Kβ in recombinant enzymatic assays and in primary human immune cells with an exquisite selectivity against other targets.
    HM5023507 attenuated anti‐CD3/anti‐CD28‐induced human T cell activation, with a better potency in the blockade of IL‐2 production than in proliferation response, with IC50 values of 9 and 120 nM, respectively.
    HM5023507 reduces T cell differentiation into different effector cell types including Th1, Th2, Th17, and Treg cells with mean IC50 values of 48, 18, 63, and 130 nM, respectively.
    HM5023507 inhibited anti‐IgM‐induced activation as measured by upregulation of CD69 and IL‐6 production from purified human B cells (IC50<10 nM), also attenuated B cell activation in rat whole blood with an average IC50 of 44 nM.
    HM5023507 (3 mg/kg, p.o.) attenuates B cell activation and CXCL1 induced neutrophil influx in female Wistar rats.

    物理化学性质&存储条件

    分子量 435.872
    分子式 C21H18ClN7O2
    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

    (S)-2-(1-(5-acetyl-2-aminopyrimidin-4-yl)azetidin-2-yl)-5-chloro-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4(3H)-one

    参考文献

    1. Yu Cai, et al. Pharmacol Res Perspect. 2020 Feb; 8(1): e00559.

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