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Background Information:
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).
Reference:
1. N. S. Rao, et al, ASN002: A Potent Dual SYK/JAK Inhibitor Currently in a Phase I/II Study Shows Strong Antitumor Activity in Preclinical Studies, Blood 2015 vol. 126 no. 23 4009.
2. S. Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.
APIM050083: ASN-002 (GUSACITINIB)
CAS No.: 1425381-60-7.
Molecular Formula: C24H28N8O2 • 0.8H2O.
Molecular Weight: 474.9.
Purity: >99.5% by HPLC (at 214 and 254 nm).
QC: HPLC, MS, NMR, and Quantitative Elemental analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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