Identification | Back Directory | [Name]
JAK3 Inhibitor I | [CAS]
211555-05-4 | [Synonyms]
WHI-P-97;WHI P97 JAK3 Inhibitor I USP/EP/BP 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol Phenol, 2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]- WHI-P 974-(3',5'-DibroMo-4-hydroxyphenyl)aMino-6,7-diMethoxyquinazoline | [Molecular Formula]
C16H13Br2N3O3 | [MDL Number]
MFCD02683947 | [MOL File]
211555-05-4.mol | [Molecular Weight]
455.1 |
Chemical Properties | Back Directory | [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) | [color ]
White to gray |
Hazard Information | Back Directory | [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 td> | 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]
Target | Value | JAK3 () | table>
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Tags:211555-05-4
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