Drug intelligence / Profile preview

WHI-P131

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal
01

Overview

WHI-P131 is a **small molecule inhibitor** primarily targeting **Janus kinase 3 (JAK3)** and also exhibits **inhibitory activity against epidermal growth factor receptor (EGFR)**. It has been studied for its anticancer, chemopreventive, anti-inflammatory, and anti-diabetic properties. WHI-P131 has shown **prophylactic activity against UVB-induced carcinogenesis in vivo** and reduces parameters of inflammation and myocardial injury in animal models. In cell and animal studies, WHI-P131 induces apoptosis in JAK3-expressing leukemia cell lines, inhibits glioblastoma cell adhesion and invasion, prevents graft-versus-host disease (GVHD) without affecting graft-versus-leukemia (GVL) efficacy, and suppresses NF-κB mediated signaling, thereby reducing the production of nitric oxide and inducible nitric oxide synthase (iNOS), with possible benefit in diabetes prevention. Preclinical pharmacokinetic and safety studies in rodents and monkeys show broad tissue distribution, rapid absorption after intraperitoneal or oral administration, low oral bioavailability, and low acute toxicity[1][2][3][4][7][10].

Other names
4-[4'-hydroxyphenylamino]-6,7-dimethoxyquinazoline4-[6,7-dimethoxyquinazolin-4-ylamino]phenol hydrochloride
02

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