4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉

生物活性靶點(diǎn)體外研究體內(nèi)研究 用途與合成方法 MSDS 4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉價(jià)格(試劑級) 上下游產(chǎn)品信息

中文名稱	4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉
中文同義詞	4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉;化合物WHI-P97;2,6-二溴-4-((6,7-二甲氧基喹唑啉-4-基)氨基)苯酚;4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉;WHI-P97,JAK-3抑制劑
英文名稱	WHI-P97
英文同義詞	WHI-P 974-(3',5'-DibroMo-4-hydroxyphenyl)aMino-6,7-diMethoxyquinazoline;2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol;WHI-P-97;WHI P97;Phenol, 2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-;JAK3 Inhibitor I USP/EP/BP;WHI-P97;Janus kinase,JAK,airway,Inhibitor,WHIP97,eosinophil recruitment,WHI-P97,inhibit,ovalbumin challenge,WHI P97,ovalbumin-sensitized,WHI-P-97
CAS號	211555-05-4
分子式	C16H13Br2N3O3
分子量	455.1
EINECS號
相關(guān)類別	蛋白酪氨酸激酶;標(biāo)準(zhǔn)品
Mol文件	211555-05-4.mol
結(jié)構(gòu)式

4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉 性質(zhì)

4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉 用途與合成方法

生物活性

WHI-P97是一種有效的JAK-3抑制劑，Ki值為0.09 μM，在EGFR激酶抑制試驗(yàn)中IC50為2.5 μM。

靶點(diǎn)

體外研究

WHI-P97 inhibits 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/FcεRI crosslinking by >90% at low micromolar concentrations.WHI-P97 (30 μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells.

體內(nèi)研究

WHI-P97 is very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 μg/kg to 50 mg/kg, and LD     ₁₀    is not reached at a 50 mg/kg dose level when administered as a single i.p. or i.v. bolus dose.WHI-P97 (i.v. injection; 40 mg/kg; single dose) has an elimination half-life (t     _1/2    ) of 58.9 min and systemic clearance (CL) of 891 ml/h/kg in CD-1 mice and a t     _1/2    of 84.2 min and CL of 1513 ml/h/kg in BALB/c mice. The values for AUC and C     _max    are 107.3 μM and 296.7 μM, respectively, in CD-1 mice. And the IC     ₅₀    values are 58.4 μM and 212.7 μM, respectively, in BALB/c mice. The large volume of distribution are 322 ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice.WHI-P97 (intraperitoneal injection; 40 mg/kg; 24 days) prevents ovalbumin-sensitized mice the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion in mice. WHI-P97 inhibits the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion.

安全信息

MSDS信息

4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉 價(jià)格(試劑級)

4-(3',5'-二溴-4-羥基苯基)氨基-6,7-二甲氧基喹唑啉 上下游產(chǎn)品信息