Gusacitinib 是一种有效的Syk激酶和JAK激酶的双抑制剂，IC50值为 5 到 46 nM 之间，具有抗癌活性。

Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).

Gusacitinib (ASN-002) shows 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[1]. In mechanistic cell-based studies involving IgE and cytokine stimulations, Gusacitinib (ASN-002) strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively.

Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies[1]. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. In a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy in inhibiting tumor growth (>95%) and it also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model.

1425381-60-7

C24H28N8O2

460.53

ASN-002

DMSO:95mg/ml (206.28 Mm),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years