JAK3 Inhibitor I
WHI-P97
CAS: 211555-05-4
Molecular Formula: C16H13Br2N3O3
JAK3 Inhibitor I - Names and Identifiers
| Name | WHI-P97 |
| Synonyms | WHI-P97 WHI P97 WHI-P-97 JAK3 Inhibitor I 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 |
| CAS | 211555-05-4 |
JAK3 Inhibitor I - Physico-chemical Properties
| Molecular Formula | C16H13Br2N3O3 |
| Molar Mass | 455.1 |
| Density | 1.785 |
| Boling Point | 470.9±45.0 °C(Predicted) |
| pKa | 7.05±0.36(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | 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 study | 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 i.p. or i.v. bolus dose.WHI-P97 (i.v. 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 a t 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 airway 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. |
JAK3 Inhibitor I - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.197 ml | 10.986 ml | 21.973 ml |
| 5 mM | 0.439 ml | 2.197 ml | 4.395 ml |
| 10 mM | 0.22 ml | 1.099 ml | 2.197 ml |
| 5 mM | 0.044 ml | 0.22 ml | 0.439 ml |
Last Update：2024-01-02 23:10:35
JAK3 Inhibitor I - Reference Information
| biological activity | WHI-P97 is an effective JAK-3 inhibitor with a Ki value of 0.09 μM and IC50 of 2.5 μM in EGFR kinase inhibition test. |
| target | TargetValue JAK3 () |
| Target | Value |
| in vitro study | 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 study | 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 I. p. or I. v. bolus dose.WHI-P97 (I. v. 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 a t 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 μ m and 296.7 μ m, respectively, in CD-1 mICE. And the IC 50 values are 58.4 μ m and 212.7 μ m, 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 airway 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. |
| 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. |
Last Update：2024-04-09 02:00:03
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Product Name: WHI-P97 Visit Supplier Webpage Request for quotationCAS: 211555-05-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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