CAS 211555-05-4|WHI-P97
| Common Name | WHI-P97 | ||
|---|---|---|---|
| CAS Number | 211555-05-4 | Molecular Weight | 455.10100 |
| Density | 1.785 | Boiling Point | / |
| Molecular Formula | C16H13Br2N3O3 | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol |
|---|---|
| Synonym | More Synonyms |
WHI-P97 BiologicalActivity
| 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. |
Chemical & Physical Properties
| Density | 1.785 |
|---|---|
| Molecular Formula | C16H13Br2N3O3 |
| Molecular Weight | 455.10100 |
| Exact Mass | 452.93200 |
| PSA | 76.50000 |
| LogP | 4.69420 |
| InChIKey | YVCXQRVVNQMZEI-UHFFFAOYSA-N |
| SMILES | COc1cc2ncnc(Nc3cc(Br)c(O)c(Br)c3)c2cc1OC |
| Storage condition | -20°C |
Synonyms
| whi-p97 |
| hms3265e23 |
