211555-05-4

211555-05-4 structure

Name: WHI-P97
Chemical Name: 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
CAS Number: 211555-05-4
Molecular Formula: C₁₆H₁₃Br₂N₃O₃
Molecular Weight: 455.10100
Catalog: Biochemical Inhibitor Protein tyrosine kinase
Create Date: 2019-01-01 20:33:19
Modify Date: 2024-01-14 15:43:15
WHI-P97 is a rationally designed potent inhibitor of JAK-3.IC50 value:Target: JAK3Treatment 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. 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.

Name	2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
Synonyms	whi-p97 hms3265e23

Description	WHI-P97 is a rationally designed potent inhibitor of JAK-3.IC50 value:Target: JAK3Treatment 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. 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.
Related Catalog	Research Areas >> Inflammation/Immunology
Target	JAK3:11 μM (IC50)
References	[1]. Ji KA, Yang MS, Jou I, Shong MH, Joe EH.Thrombin induces expression of cytokine-induced SH2 protein (CIS) in rat brain astrocytes: involvement of phospholipase A2, cyclooxygenase, and lipoxygenase.Glia. 2004 Nov 1;48(2):102-11. [2]. Wong WS, Leong KP.Tyrosine kinase inhibitors: a new approach for asthma.Biochim Biophys Acta. 2004 Mar 11;1697(1-2):53-69. [3]. Uckun FM, Sudbeck EA, Mao C, Ghosh S, Liu XP, Vassilev AO, Navara CS, Narla RK.Structure-based design of novel anticancer agents.Curr Cancer Drug Targets. 2001 May;1(1):59-71. [4]. Sudbeck EA, Liu XP, Narla RK, Mahajan S, Ghosh S, Mao C, Uckun FM.Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.Clin Cancer Res. 1999 Jun;5(6):1569-82.

Density	1.785
Molecular Formula	C₁₆H₁₃Br₂N₃O₃
Molecular Weight	455.10100
Exact Mass	452.93200
PSA	76.50000
LogP	4.69420
Storage condition	-20°C

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