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WHI-P154
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
WHI-P154图片
CAS NO:211555-04-3
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
WHI-P154 是一种有效的 EGFR 抑制剂，也适度阻断 JAK3，IC50 分别为 4 nM 和 1.8 μM。
Cas No.211555-04-3
别名2-溴-4-(6,7-二甲氧基喹唑啉-4-基氨基)苯酚
化学名2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
Canonical SMILESCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)O)Br)OC
分子式C16H14BrN3O3
分子量376.2
溶解度≥ 125.6 mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

WHI-P154 is an inhibitor of JAK3 with IC50 value of 1.8μM [1].

In vitro kinase assays show that WHI-P154 is not a specific inhibitor. Besides JAK3, it also inhibits many other kinases, including EGFR, ABL, LCK, SRC and VEGFR. WHI-P154 inhibits EGFR with IC50 value of 4nM. The specificity of WHI-P154 has not been shown in cell-based assays either [1].

WHI-P154 shows cytotoxicity against the U373 human glioblastoma cell line in vitro. This antitumor activity can be enhanced by conjugation to EGF. WHI-P154 also shows antitumor activity in a SCID mouse xenograft model of human glioblastoma [2].

References:
[1] Changelian PS, Moshinsky D, Kuhn CF, Flanagan ME, Munchhof MJ, Harris TM, Whipple DA, Doty JL, Sun J, Kent CR, Magnuson KS, Perregaux DG, Sawyer PS, Kudlacz EM. The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7.
[2] Narla RK, Liu XP, Myers DE, Uckun FM. 4-(3'-Bromo-4'hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: a novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells. Clin Cancer Res. 1998 Jun;4(6):1405-14.