ASN-002 is a orally available potent dual inhibitor of SYK (Spleen Tyrosine Kinase) and pan-JAK (Janus kinases) with IC50 values of 5-46 nM in biochemical assays. In mechanistic cell-based studies involving IgE and cytokine stimulations, ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. The compound showed anti-proliferative activity in a broad panel of human cancer cell lines including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solid and hematological tumor types. In a multiple myeloma (H929) xenograft model, ASN002 exhibited significant efficacy in inhibiting tumor growth (>95%). It also significantly delayed the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model.

KEYWORDS: ASN-002 | Supplier | SYK and JAK inhibitor | Gusacitinib | ASN002 | ASN 002 | CT-ASN002 | CAS [1425381-60-7] | B-Cell transformation | Spleen tyrosine kinase (Syk) | JAK | Inhibitor | Enzymes