ChemicalBook > CAS DataBase List > JAK3 INHIBITOR I

JAK3 INHIBITOR I

Product Name: JAK3 INHIBITOR I
CAS No.: 202475-60-3
Chemical Name: JAK3 INHIBITOR I
Synonyms: CS-2623;Janex 1;WHI-P131;WHI-P131, >98%;JANEX-1 ，S5903;JAK3 INHIBITOR I;JANEX-1;WHI-P131;WHI-P131(Janex 1);JANEX-1, 10 mM in DMSO;A JAK3 inhibitor WHI-P131
CBNumber: CB7130537
Molecular Formula: C16H15N3O3
Formula Weight: 297.31
MOL File: 202475-60-3.mol

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JAK3 INHIBITOR I Property

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

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Safety

Hazard Codes: Xi
Risk Statements: 36/37/38
Safety Statements: 26-36
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: 420101
Product name: JAK3 Inhibitor I - CAS 202475-60-3 - Calbiochem
Packaging: 5MG
Price: $189
Updated: 2025/07/31

Cayman Chemical

Product number: 10011246
Product name: WHI-P131
Purity: ≥98%
Packaging: 1mg
Price: $31
Updated: 2024/03/01

Cayman Chemical

Product number: 10011246
Product name: WHI-P131
Purity: ≥98%
Packaging: 5mg
Price: $133
Updated: 2024/03/01

Cayman Chemical

Product number: 10011246
Product name: WHI-P131
Purity: ≥98%
Packaging: 10mg
Price: $234
Updated: 2024/03/01

Cayman Chemical

Product number: 10011246
Product name: WHI-P131
Purity: ≥98%
Packaging: 25mg
Price: $510
Updated: 2024/03/01

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JAK3 INHIBITOR I Chemical Properties,Usage,Production

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 (t_max) 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 C_max 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 I Preparation Products And Raw materials

Raw materials

Preparation Products

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JAK3 INHIBITOR I Suppliers

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View Lastest Price from JAK3 INHIBITOR I manufacturers

Career Henan Chemical Co

Product: 4-(4'-HYDROXYPHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINE 202475-60-3
Price: US $1.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 20kg
Release date: 2019-09-05

202475-60-3, JAK3 INHIBITOR IRelated Search:

Phenol, 3-[(6,7-diMethoxy-4-quinazolinyl)aMino]- Acetaminophen 2'-Hydroxyacetophenone Dihydroxybenzoic acid 2-HYDROXYACETOPHENONE 7-BROMO-1,2,3,4-TETRAHYDRO-QUINOLINE HYDROCHLORIDE WH-4-023 4-AMINO-3-CYANO-1,2,5,6-TETRAHYDROPYRIDINE 4-(3'-HYDROXYPHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINE, HCL JAK3 Inhibitor WHI-P97 JAK3 INHIBITOR II JAK3 INHIBITOR, NEGATIVE CONTROL JAK3 INHIBITOR I JAK3 INHIBITOR VI JAK3 INHIBITOR IV JAK2 INHIBITOR II JAK3 INHIBITOR V

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

WHIP-131;JANEX-1);WHIP131;JANEX1

CS-2623

WHI-P131, >98%

Phenol, 4-[(6,7-dimethoxy-4-quinazolinyl)amino]-

JANEX-1, 10 mM in DMSO

JANEX-1 ，S5903

202475-60-3

Non-Receptor Tyrosine Kinase Inhibitors

Kinase/Phosphatase Biology

Janus Kinase (JAK)

BioChemical

Cell Biology

Cell Signaling and Neuroscience

Inhibitors

Heterocycles, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals