AZD-1480产品描述：AZD-1480 是一种新颖的
JAK2 的ATP竞争性抑制剂，
IC50 值为 < 0.4 nM。
AZD-1480产品描述：AZD-1480 is a novel ATP-competitive
JAK2 inhibitor with
IC50 of < 0.4 nM, selectively against JAK3 ａnd Tyk2, ａnd to a smaller extent against JAK1.IC50 & Target: IC50: < 0.4 nM (JAK2)
In Vitro: AZD1480 (5μM) induces G2/M arrest ａnd cell death by inhibiting Aurora kinases
[1]. AZD1480 is a potent JAK2 inhibitor that can suppress growth, survival, as well as FGFR3 ａnd STAT3 signaling ａnd downstream targets including Cyclin D2 in human multiple myeloma cells. At low micromolar concentrations, AZD1480 blocks cell proliferation ａnd induces apoptosis of myeloma cell lines
[2]. AZD1480 effectively blocks constitutive ａnd stimulus-induced JAK1, JAK2, ａnd STAT-3 phosphorylation in both human ａnd murine glioma cells, ａnd leads to a decrease in cell proliferation ａnd induction of apoptosis
[3]. AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase, ａnd that it is capable of inhibiting STAT3 phosphorylation ａnd tumor growth in a STAT3-dependent manner. AZD1480 inhibits tumor angiogenesis ａnd metastasis in part by affecting the tumor microenvironment
[4].
In Vivo: AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors ａnd multiple myeloma
[1]. In vivo, AZD1480 inhibits the growth of subcutaneous tumors ａnd increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors
[3]. AZD1480 blocks lung infiltration of myeloid cells ａnd formation of pulmonary metastases in both mouse syngeneic experimental ａnd spontaneous metastatic models. Furthermore, AZD1480 reduces angiogenesis ａnd metastasis in a human xenograft tumor model
[4]. AZD1480 suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity
[5].
研究领域：
GPCR/G Protein靶点：
Adrenergic Receptor相关产品：
Isoprenaline hydrochloride |
Norepinephrine bitartrate monohydrate |
(R)-(-)-Phenylephrine hydrochloride |
ICI 118,551 hydrochloride |
Propranolol hydrochloride |
L-Epinephrine |
Ivabradine hydrochloride |
Clonidine hydrochloride |
Salmeterol xinafoate |
Phentolamine mesylate |
Yohimbine Hydrochloride |
Perphenazine |
Silodosin |
Vilanterol trifenatate |
Atipamezole hydrochloride |
Alternative_Names:AZD1480;AZD 1480
MWt:348.77
Formula:C14H14ClFN8
SMILES:ClC1=C(N=C(N=C1)N[C@@H](C)C2=NC=C(C=N2)F)NC3=NNC(C)=C3
Research_Area:Cancer
公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、；MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足*新的科研需求；数千种产品在上海有充足备货，24-48小时内送达客户；大量产品提供免费试用装；已为全球多个知名企业、院校构建各种定制型化合物库。网址：www.medchemexpress.cn
地址:上海市浦东新区蔡伦路720号2号楼4层
原创作者：MedChemExpress
