| 產(chǎn)品描述： | AT7519 Hydrochloride is 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. |
| 靶點(diǎn)： |
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);Apoptosis;?GSK-3;?CDK |
| 體內(nèi)研究： |
AT7519 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.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice |
| 參考文獻(xiàn)： |
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. 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： |
DMSO : ≥ 300 mg/mL (716.49 mM) H2O : 8.33 mg/mL (19.89 mM; Need ultrasonic) |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.388 ml |
11.941 ml |
23.883 ml |
| 5 mM |
0.478 ml |
2.388 ml |
4.777 ml |
| 10 mM |
0.239 ml |
1.194 ml |
2.388 ml |
| 50 mM |
0.048 ml |
0.239 ml |
0.478 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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