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  • PP121

    • PP-121
    货号: abs813316
    CAS号: 1092788-83-4
    分子式: C17H17N7
    分子量: 319.36
    产品说明书
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    货号-规格 货期 价格 数量
    abs813316-5mg 1-2周 ¥604.00
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    abs813316-10mg 1-2周 ¥920.00
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    abs813316-25mg 1-2周 ¥1842.00
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    abs813316-50mg 1-2周 ¥3018.00
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    产品描述
    描述

    PP121是一种作用于PDGFR, Hck, mTOR, VEGFR2, Src和Abl的多靶点抑制剂,IC50分别为2 nM, 8 nM, 10 nM, 12 nM, 14 nM和18 nM,也抑制DNA-PK,IC50为60 nM。PP-121在酪氨酸激酶和PI3Ks而不是丝-苏氨酸激酶保守的疏水性口袋中选择性相互作用。PP-121在Src处与Glu310形成氢键,有效取代催化赖氨酸的结构作用,且导致产生螺旋C的顺序和活性构象的稳定性。PP-121抑制一些 PI3Ks,包括p110α, DNA-PK 和mTOR,IC50分别为 52 nM, 60 nM 和 10 nM。

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    PP-121
    可溶性/溶解性
    Ethanol :2 mg/mL (6.26 mM)

    DMSO :60 mg/mL (187.9 mM)
    生物活性
    靶点
    PDGFR ,Hck,VEGFR,mTOR,Src,,
    In vitro(体外研究)
    PP-121 selectivity interacts within a hydrophobic pocket that is conserved between both tyrosine kinases and PI3Ks, not serine-threonine kinases. PP-121 makes a hydrogen bond to Glu310 in Src, effectively substituting for the structural role of the catalytic lysine and resulting in the ordering of helix C and stabilization of an active conformation. PP-121 also inhibits other PI3Ks including p110α and DNA-PK with IC50 of 52 nM and 60 nM, respectively. PP-121 potently and dose-dependently blocks the phosphorylation of Akt, p70S6K and S6 in two glioblastoma cell lines, U87 and LN229. PP-121 potently inhibits the proliferation of a subset of the tumor cell lines by direct inhibition of PI3Ks and mTOR. PP-121 induces a G0/G1 arrest in LN220, U87 and Seg1 cells. PP-121 also blocks tyrosine phosphorylation induced by v-Src in NIH3T3 cells transformed with v-Src(Thr338). PP-121 could restore actin stress fiber staining in NIH3T3 cells transformed with v-Src(Thr338). PP-121 at a low concentration of 40 nM inhibits Ret autophosphorylation in TT thyroid carcinoma cells that express the C634W oncogenic Ret mutant35. PP-121 inhibits cell proliferation with IC50 of 50 nM in TT thyroid carcinoma cells. PP-121 inhibits cell proliferating stimulated only with VEGF with IC50 of 41 nM in human umbilical vein endothelial cells (HUVECs). PP-121 directly inhibits Bcr-Abl induced tyrosine phosphorylation, resulting in drug-induced apoptosis in K562 cells and a combination of apoptosis and cell cycle arrest in Bcr-Abl expressing BaF3 cells.
    参考文献
    参考文献
    The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121.
    Peng Y,et al. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44. PMID:
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
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