WHI-P97
- CAS NO.:211555-05-4
- Empirical Formula: C16H13Br2N3O3
- Molecular Weight: 455.1
- MDL number: MFCD02683947
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:11
What is WHI-P97?
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. |
Properties of WHI-P97
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 |
Safety information for WHI-P97
Computed Descriptors for WHI-P97
New Products
Tubulysin I Tubulysin D 2,2-diethoxyethanethioamide 4,4-DIFLUOROPIPERIDINE 4-(Benzyloxy)-3-bromophenylacetic Acid 4-CYANO-TETRAHYDROPYRAN-4-CARBOXYLIC ACID 2-(azetidin-3-ylidene)acetonitrile (hydrochloride) 4-IODOTETRAHYDRO-2H-PYRAN 4-FLUOROPIPERIDINE Imeglimin Hydrochloride IH Fuel shell (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Calcium Sodium Phosphosilicate IH 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile (R)-(3-(3-fluoro-4- thiomorpholinophenyl)-2- oxooxazolidin-4-yl) methyl methanesulfonate methyl 3-fluoro-4- thiomorpholino phenylcarbamate Flame Retardant Zinc Borate Magnesium Trisilicate Lubiprostone Latanoprostene Bunod 7-Methoxyquinoline-4-carboxylic acid 1H-Imidazole-4-carbonitrile 7-Methoxyquinoline-4-carbonitrileRelated products of tetrahydrofuran
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