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ASN-002 (Gusacitinib)
Gusacitinib (ASN-002) is a clinical-stage, 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 (Refs 1, 2).
Catalog NO: CT-ASN002
Synonym: Gusacitinib, ASN002
CAS NO: 1425381-60-7
Mol. Formula: C24H28N8O2 • 0.8H2O
MW: 474.9
** in vivo Quality Material. 99.9% Purity, a recrystallized pale yellow powder, with a spot-on quantitative elemental analysis. Bulk (Grams). Prompt.