货号	规格	价格	上海	北京	珠海	重庆	武汉
S83287-5mg	≥98%	￥640.00 S83287-5mg ￥640.00 3-5天	0 货期：3-5天	-	-	-	-
S83287-10mg	≥98%	￥1110.00 S83287-10mg ￥1110.00 3-5天	0 货期：3-5天	-	-	-	-
S83287-50mg	≥98%	￥3670.00 S83287-50mg ￥3670.00 3-5天	0 货期：3-5天	-	-	-	-
S83287-100mg	≥98%	￥5870.00 S83287-100mg ￥5870.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

AT7519 (AT7519M) TFA as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

靶点：

CDK9/Cyclin T:10 nM (IC50);CDK5/p35:13 nM (IC50);cdk2/cyclin A:47 nM (IC50);Cdk4/cyclin D1:100 nM (IC50);cdk6/cyclin D3:170 nM (IC50);Cdk1/cyclin B:210 nM (IC50);CDK7/Cyclin H/MAT1:2400 nM (IC50);GSK3β:89 nM (IC50);Others

体外研究：

AT7519 (0-4 μM) TFA results in dose-dependent cytotoxicity with IC50s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 TFA overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) TFA induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) TFA inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells. AT7519 (250 nM) TFA inhibits cell cycle progression in human tumor cell lines. AT7519 TFA also induces apoptosis of human tumor cell lines. AT7519 (100-700 nM) TFA induces apoptosis in leukemia cell lines. AT7519TFA also inhibits transcription in human tumor cell lines. Furthermore, AT7519 TFA inhibits RNA polymerase II and reduces antiapoptotic protein levels

体内研究：

AT7519 TFA inhibits tumor growth in a human MM xenograft mouse model. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) TFA also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice

参考文献：

1. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36. 2. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009 Feb;8(2):324-32. 3. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.015 ml	10.075 ml	20.15 ml
5 mM	0.403 ml	2.015 ml	4.03 ml
10 mM	0.202 ml	1.008 ml	2.015 ml
50 mM	0.04 ml	0.202 ml	0.403 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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AT7519 (trifluoroacetate)