您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Derazantinib dihydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Derazantinib dihydrochloride
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。
Derazantinib dihydrochloride图片
CAS NO:1821329-75-2
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍

Derazantinib (formerly known as ARQ 087) is a novel, orally bioavailable, ATP competitive, small molecule, multi-kinase inhibitor with potent in vitro and in vivo activity against FGFR (fibroblast growth factor receptor) addicted cell lines and tumors with IC50s of 4.5, 1.8, and 4.5 nM for FGFR1-3 respectively in biochemical assay, IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3. In cells, ARQ 087 exhibited inhibition of FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK) as evidenced by the response to ARQ 087 treatment. Cell proliferation studies demonstrated ARQ 087 has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein showed a positive relationship between ARQ 087 induced G1 cell cycle arrest and subsequent induction of apoptosis. In addition, ARQ 087 was effective at inhibiting tumor growth in vivo in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions. ARQ 087 is currently being studied in a phase 1/2 clinical trial that includes a sub cohort for intrahepatic cholangiocarcinoma patients with confirmed FGFR2 gene fusions (NCT01752920).

纯度:≥98%

CAS:1821329-75-2