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| | WHI-P97 Basic information |
| Product Name: | WHI-P97 | | Synonyms: | WHI-P 974-(3',5'-DibroMo-4-hydroxyphenyl)aMino-6,7-diMethoxyquinazoline;2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol;JAK3 Inhibitor I USP/EP/BP;Phenol, 2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-;WHI-P-97;WHI P97;WHI-P97;Janus kinase,JAK,airway,Inhibitor,WHIP97,eosinophil recruitment,WHI-P97,inhibit,ovalbumin challenge,WHI P97,ovalbumin-sensitized,WHI-P-97 | | CAS: | 211555-05-4 | | MF: | C16H13Br2N3O3 | | MW: | 455.1 | | EINECS: | | | Product Categories: | | | Mol File: | 211555-05-4.mol |  |
| | WHI-P97 Chemical Properties |
| Boiling point | 470.9±45.0 °C(Predicted) | | density | 1.785 | | storage temp. | Store at -20°C | | solubility | DMSO : 5.88 mg/mL (12.92 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) | | form | Powder | | pka | 7.05±0.36(Predicted) |
| | WHI-P97 Usage And Synthesis |
| Definition | ChEBI: 2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol is a member of quinazolines. | | Biological Activity | WHI-P97 is a potent JAK-3 inhibitor with Ki of 0.09 μM and IC50 of 2.5 μM in EGFR kinase inhibition assay. | | in vitro | 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. | | in vivo | 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 ip or iv bolus dose. WHI-P97 (iv 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 at 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 airwa y lumen after the ovalbumin challenge in a dose-dependent fashion. | Animal Model: | BALB/c mouse model of allergic asthma | | Dosage: | 40 mg/kg | | Administration: | intraperitoneal injection; 24 days | | Result: | Showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels. | | | target | |
| | WHI-P97 Preparation Products And Raw materials |
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