| Identification | Back Directory | [Name]
JAK3 INHIBITOR I | [CAS]
202475-60-3 | [Synonyms]
Janex 1
CS-2623
WHI-P131
WHI-P131, >98%
JANEX-1;WHI-P131
JAK3 INHIBITOR I
WHI-P131(Janex 1)
A JAK3 inhibitor
WHI-P131
WHIP-131;JANEX-1);WHIP131;JANEX1
4-(6,7-dimethoxyquinazolin-4-ylamino)phenol
Phenol, 4-[(6,7-dimethoxy-4-quinazolinyl)amino]-
4-(4'-HYDROXYPHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINE | [Molecular Formula]
C16H15N3O3 | [MDL Number]
MFCD01862614 | [MOL File]
202475-60-3.mol | [Molecular Weight]
297.31 |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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) Narla et al. (1998), Inhibition of human glioblastoma cell adhesion and invasion by 4-(4’-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3’-bromo-4’-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154); Mol. Clin. Cancer Res., 4 2463
2) Trieu et al. (2000), A specific inhibitor of janus kinase-3 increases survival in a transgenic mouse model of amyotrophic lateral sclerosis; Biochem. Biophys. Res. Commun., 267 22
3) Cetkovic-Cvrlje et al. (2003), Targeting JAK3 with JANEX-1 for prevention of autoimmune type 1 diabetes in NOD mice; Clin. Immunol., 106 213
4) Uckun et al. (2008), Anti-inflammatory activity profile of JANEX-1 in preclinical animal models; Bioorg. Med. Chem., 16 1287
5) Oh et al. (2013), Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice; Exp. Mol. Med., 45 e23 |
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| Company Name: |
China Langchem Inc.
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| Tel: |
0086-21-58956006 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList19141/0.htm |
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