Drug intelligence / Profile preview

AT9283

Development stage
Phase 2
Lead developer
Astex Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

AT9283 is a small molecule, multi-targeted kinase inhibitor developed by Astex Therapeutics for the treatment of cancer. It acts primarily as an inhibitor of Aurora kinase A, Aurora kinase B, Janus kinase 2 (JAK2), BCR–ABL fusion protein, Janus kinase 3 (JAK3), and Fms-like tyrosine kinase 3 (FLT3). By inhibiting these kinases—especially Aurora A and B—it disrupts mitotic checkpoint control during cell division, leading to inhibition of cellular proliferation and induction of apoptosis in tumor cells that overexpress these targets. Preclinical studies have shown antitumor activity in various solid tumors and hematological malignancies such as leukemia and lymphoma. The drug was discovered using Astex’s fragment-based drug discovery platform[1][2][4][5].

Other names
1-cyclopropyl-3-(3-(5-morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea896466-04-9
02

Targets

JAK3 (Janus kinase 3)FLT3 (Fms related receptor tyrosine kinase 3)JAK2 (Janus kinase 2)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)AURKB (Aurora kinase B)AURKA (Aurora kinase A)

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