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202475-60-3

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202475-60-3 Usage

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.

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

Check Digit Verification of cas no

The CAS Registry Mumber 202475-60-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,0,2,4,7 and 5 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 202475-60:
(8*2)+(7*0)+(6*2)+(5*4)+(4*7)+(3*5)+(2*6)+(1*0)=103
103 % 10 = 3
So 202475-60-3 is a valid CAS Registry Number.

202475-60-3SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name Janex 1

1.2 Other means of identification

Product number -
Other names 1-Amino-4-<4-hydroxy-anilino>-anthrachinon-2-sulfonsaeure

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:202475-60-3 SDS

202475-60-3Relevant articles and documents

QUINAZOLINE DERIVATIVES AS ECTONUCLEOTIDE PYROPHOSPHATASE PHOSPHODIESTERASE 1 INHIBITORS

-

Paragraph 0195; 0229, (2020/07/15)

The present disclosure provides certain quinazoline compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

4-(4′-hydroxyphenyl) amino-6,7-dimethoxyquinazoline to prevent development of colorectal cancer

-

, (2008/06/13)

The present invention is directed to a method of preventing the development or recurrence of colorectal cancer in a mammal comprising administering to the mammal, an effective cancer preventative amount of 4-(4′-hydroxyphenyl)-amino-6,7-dimethoxyquinazoli

Treatment of atherosclerosis in apolipoprotein E-deficient mice with 4- (3'-bromobenzoyl)-6,7-dimethoxyquinazoline (WHI-P164), a potent inhibitor of triglyceride synthesis

Trieu, Vuong N.,Liu, Xing-Ping,Chen, Chun-Lin,Uckun, Fatih M.

, p. 179 - 188 (2007/10/03)

We identified a novel organic compound, 4-(3'-bromobenzoyl)-6,7- dimethoxyquinazoline (compound WHI-P164), as a potent inhibitor of triglyceride (TG) synthesis. In an in vitro model of lipid synthesis, WHI- P164 (but not any one of the three structurally similar control dimethoxyquinazoline compounds) inhibited the accumulation of TG-rich intracellular lipid droplets in Caco-2 human intestinal cells in a concentration-dependent fashion. WHI-P164 caused no acute toxicity associated with morbidity or mortality in mice when administered at dose levels ranging from 0.5 to 80 mg/kg. In pharmacokinetic studies in mice, WHI-P164 was rapidly eliminated from plasma with a terminal elimination half-life of 26.1 ± 1.3 min after intraperitoneal administration and 33.3 ± 11.3 min after intravenous administration. Treatment with 40 mg/kg WHI-P164 (but not one of three structurally similar control dimethoxyquinazoline compounds) administered intraperitoneally once daily for 7 consecutive treatment days blocked the in vivo hepatic TG synthesis in both apoE-deficient and wild-type C57B1/6 mice. In apoE-deficient mice maintained on a high-fat/high- cholesterol Western diet, WHI-P164 substantially reduced the lipid accumulation in the liver after 7 days of treatment and the lipid accumulation in the aorta after 1 month of treatment. Our results in apoE- deficient mice show that lipid accumulation in hepatocytes and foam cells are related events, and inhibiting TG synthesis with WHI-P164 offers an effective means to treat atherosclerosis.

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