JAK3 INHIBITOR I
JAK3 INHIBITOR I Basic information
- Product Name:
- JAK3 INHIBITOR I
- Synonyms:
-
- 4-(4'-HYDROXYPHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINE
- JAK3 INHIBITOR I
- WHI-P131
- Janex 1
- A JAK3 inhibitor WHI-P131
- 4-(6,7-dimethoxyquinazolin-4-ylamino)phenol
- WHI-P131(Janex 1)
- JANEX-1;WHI-P131
- CAS:
- 202475-60-3
- MF:
- C16H15N3O3
- MW:
- 297.31
- Product Categories:
-
- Inhibitors
- Heterocycles, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals
- Mol File:
- 202475-60-3.mol
JAK3 INHIBITOR I Chemical Properties
- Boiling point:
- 468.1±40.0 °C(Predicted)
- Density
- 1.336±0.06 g/cm3(Predicted)
- storage temp.
- Keep in dark place,Inert atmosphere,2-8°C
- solubility
- DMSO: 18 mg/mL, soluble
- form
- solid
- pka
- 10.06±0.26(Predicted)
- color
- yellow
- Stability:
- Stable for 2 years from date of purchase as supplied. Protect from moisture. Solutions in DMSO may be stored at -20°C for up to 2 months.
- InChI
- InChI=1S/C16H15N3O3/c1-21-14-7-12-13(8-15(14)22-2)17-9-18-16(12)19-10-3-5-11(20)6-4-10/h3-9,20H,1-2H3,(H,17,18,19)
- InChIKey
- HOZUXBLMYUPGPZ-UHFFFAOYSA-N
- SMILES
- C1(O)=CC=C(NC2=C3C(=NC=N2)C=C(OC)C(OC)=C3)C=C1
JAK3 INHIBITOR I Usage And Synthesis
Description
WHI-P131 (202475-60-3) is a JAK3 inhibitor.?Inhibits human glioblastoma cell adhesion and invasion.1 Increases survival in a mouse ALS model.2 Delays or prevents autoimmune type 1 diabetes in NOD mice.3 Exhibits potent anti-inflammatory activity in mouse models of peritonitis, colitis, cellulitis and systemic inflammatory response syndrome.4 Displays protective effects against myocardial ischemia and reperfusion injury in mouse models.5
Uses
Janex 1 is a Janus tyrosine kinase 3 (JAK3) inhibitor. Inhibition of JAK3 has been shown to exhibit protective action against the development of T1D in non-obese diabetic (NOD) mice. Janex 1 has been shown to suppresses proliferation of short-term cultured NOD CD4+ T cells through induction of apoptosis, while promoting survival of a particular population of long-term cultured cells. It ameliorates the expression of TNF-α-induced cell adhesion molecules and improves myocardial vascular permeability.
in vivo
JANEX-1 is administered at doses ranging from 5 to 100 mg/kg. Evaluation of CPK activity revealed a dose-response curve with an effective dose 50 (ED50) value of 7.44 mg/kg. Mice receiving JANEX-1 displayed significantly reduced CPK and LDH levels. In addition, the infarct size of JANEX-1-treated mice (30.16±2.79%) is significantly decreased when compared with I/R-operated mice (65.64±3.76%)[2]. JANEX-1 (WHI-P131) is absorbed rapidly, and the time to reach the maximum plasma JANEX-1 concentration (tmax) is 24.7±1.7 min. JANEX-1 is rapidly eliminated with an elimination half-life of 45.6±5.5 min. Although the predicted maximum plasma JANEX-1 concentration is 10.5 ± 0.8 μM, which is only half of the Cmax following i.v. administration of the same bolus dose, the i.p. bioavailability is 94.6% and the systemic exposure levels (i.e., AUC) are very similar to those observed after i.v. injection (17.1±2.2 μM h versus 18.1±1.2 μM h)[3].
IC 50
JAK3: 78 μM (IC50)
References
[1] R K NARLA. Inhibition of human glioblastoma cell adhesion and invasion by 4-(4’-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3’-bromo-4’-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154).[J]. Clinical Cancer Research, 1998, 4 10: 2463-2471.
[2] VUONG N. TRIEU . A Specific Inhibitor of Janus Kinase-3 Increases Survival in a Transgenic Mouse Model of Amyotrophic Lateral Sclerosis[J]. Biochemical and biophysical research communications, 2000, 267 1: Pages 22-25. DOI:10.1006/bbrc.1999.1905
[3] MARINA CETKOVIC-CVRLJE . Targeting JAK3 with JANEX-1 for prevention of autoimmune type 1 diabetes in NOD mice[J]. Clinical immunology, 2003, 106 3: Pages 213-225. DOI:10.1016/s1521-6616(02)00049-9
[4] FATIH M. UCKUN . Anti-inflammatory activity profile of JANEX-1 in preclinical animal models[J]. Bioorganic & Medicinal Chemistry, 2008, 16 3: Pages 1287-1298. DOI:10.1016/j.bmc.2007.10.066
[5] YOUNG-BIN OH. Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice[J]. Experimental and Molecular Medicine, 2013, 45 5: e23-e23. DOI:10.1038/emm.2013.43
JAK3 INHIBITOR ISupplier
- Tel
- 17317130613
- 3358272972@qq.com
- Tel
- 18210857532; 18210857532
- jkinfo@jkchemical.com
- Tel
- 0086-21-58956006
- Tel
- 021-58950125
- info@chemexpress.com
- Tel
- 400-6206333 13167063860
- anhua.mao@aladdin-e.com
JAK3 INHIBITOR I(202475-60-3)Related Product Information
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