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Gusacitinib(ASN-002)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gusacitinib(ASN-002)图片
规格:98%
分子量:460.53
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Gusacitinib(ASN-002)是一种有效的、SYK激酶和JAK激酶的双抑制剂,其IC50值为5-46nM。
货号:ajcx12870
CAS:1425381-60-7
分子式:C24H28N8O2
分子量:460.53
溶解度:DMSO : 100 mg/mL (217.14 mM)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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.