Gusacitinib (ASN-002) (Synonyms: ASN-002) |
Catalog No.GC33041 |
구사시티닙(ASN-002)(ASN-002)은 5-46 nM의 IC50 값을 갖는 비장 티로신 키나제(SYK) 및 야누스 키나제(JAK)의 경구 활성 및 강력한 이중 억제제입니다. 구사시티닙(ASN-002)은 고형 및 혈액 종양 유형 모두에서 항암 활성을 가지고 있습니다.
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Cas No.: 1425381-60-7
Sample solution is provided at 25 µL, 10mM.
Gusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.
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 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 a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy in inhibiting tumor growth (>95%). It also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies[1].
[1]. Sanjeeva 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.
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