化合物WHI-P97 HCl T4657L

Product Introduction
Bioactivity


英文名: WHI-P97 HCl 211555-05-4(free base)

描述: WHI-P97 HCl 211555-05-4(free base) 是一种有效的选择性 JAK-3 抑制剂。 WHI-P97 在模型研究中估计 Ki 值为 0.09 microM，在 EGFR 激酶抑制试验中测得的 IC50 值为 2.5 microM。 WHI-P97以浓度依赖性方式有效抑制EGFR 阳性人癌细胞的体外侵袭性。

体外活性: WHI-P97 is a potent inhibitor of Janus kinase (JAK)-3.?Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations.?WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.Therapeutic WHI-P97 concentrations, which inhibit mast cell leukotriene synthesis in vitro, could easily be achieved in vivo after the i.v. or i.p. administration of a single nontoxic 40 mg/kg bolus dose of WHI-P97.

体内活性: WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose.??WHI-P97 showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels.?Treatment of ovalbumin-sensitized mice with WHI-P97 prevented the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion.?Furthermore, WHI-P97 inhibited the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.91 mg/mL (10 mM)


关键字: WHI-P97 HCl 211555-05-4(free base) | WHI P97 HCl 211555 05 4(free base) | WHI-P-97 HCl 211555-05-4(free base) | WHIP97 HCl 211555054(free base)

相关产品: Pacritinib | RGB-286638 free base | Abrocitinib | Brevilin A | ITK inhibitor 2 | Delgocitinib | JBJ-02-112-05 | CEP-33779 | GDC-0214 | JAK3-IN-6

相关库: Anti-Prostate Cancer Compound Library | Anti-Cancer Compound Library | Angiogenesis related Compound Library | Anti-Lung Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Stem Cell Differentiation Compound Library | Reprogramming Compound Library | Bioactive Compound Library

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