化学信息：
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化学名
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3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
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简称
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A83-01
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别名
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A 83-01, A-83-01, ALK5 Inhibitor IV
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中文名
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N/A
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化学式
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C25H19N5S
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分子量
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421.52
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CAS号
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909910-43-6
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO21mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入1.19ml DMSO，或者每4.22mg加入1ml DMSO，配制成10mM溶液。SF7917-10mM用DMSO配制。
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生物信息：
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产品描述
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A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5nM respectively).
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信号通路
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TGF-beta/Smad
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靶点
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ALK5
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－
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－
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－
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－
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IC50
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12nM
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－
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－
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－
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－
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体外研究
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A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation. Microarray analysis of HM-1 cells treated with TGF-β1 and/or A-83-01 revealed that A-83-01 efficiently inhibited transcriptional changes that are induced by TGF-β1. -83-01 treatment significantly increased these parameters within 24h that was positively related to pericyte coverage and tumor cell proliferation. Furthermore, apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging was decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure. Vascular function of the tumor improved by A-83-01treatment well assessed on post-Gd-L-enhanced MR images.
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体内研究
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The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3h post injection. A-83-01 induced 1.7-fold higher drug accumulation of F-SL in the tumor than liposome alone at 24h post injection.
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Furutani Y, Umemoto T, Murakami M. J Cell Biochem. 2011 Feb, 112(2), 614-24.
2. Yamamura S, Matsumura N, Mandai M. Int J Cancer. 2012 Jan 1, 130(1), 20-8.
3. Kawano K, Maitani Y. Yakugaku Zasshi. 2010 Dec, 130(12), 1679-85.
4. Taniguchi Y, Kawano K, Minowa T. Cancer Sci. 2010 Oct, 101(10), 2207-13.
包装清单：
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产品编号
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产品名称
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包装
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SF7917-10mM
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A83-01 (ALK5抑制剂)
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10mM×0.2ml
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SF7917-5mg
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A83-01 (ALK5抑制剂)
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5mg
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SF7917-25mg
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A83-01 (ALK5抑制剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品对人体有害，操作时请小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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