PF 477736
Cat. No.：YN440005
CAS No. ：952021-60-2
规格
价格(RMB)
库存
| 产品名称: | PF 477736 |
| CAS No.: | 952021-60-2 |
| Chemical Name: | (αR)-amino-N-[5,6-dihydro-2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]-cyclohexaneacetamide |
| Synonyms: | PF 00477736 |
| 分子量: | 419.48 |
| 分子式: | C₂₂H₂₅N₇O₂ |
| SMILES: | O=C([C@@H](C1CCCCC1)N)NC2=CC3=C(C(C=NNC4=O)=C(N3)C5=CN(N=C5)C)C4=C2 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | PF 477736 (PF 00477736) 是一种有效，选择性和 ATP 竞争性的Chk1的抑制剂，Ki值为 0.49 nM。它也是Chk2抑制剂，Ki值为 47 nM。PF 477736 显示出对VEGFR2，Fms，Yes，Aurora-A，FGFR3，Flt3和Ret(IC50=8 (Ki)，10，14，23，23，25 和 39 nM) <100 倍的选择性。PF 477736 在体外和体内均可增强 Gemcitabine 的抗肿瘤活性。 |
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Blasina, A., Hallin, J., Chen, E., et al.Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1Mol. Cancer Ther.7(8),2394-2404(2008)
Zhang, C., Yan, Z., Painter, C.L., et al.PF-00477736 mediates checkpoint kinase 1 signaling pathway and potentiates docetaxel-induced efficacy in xenograftsClin. Cancer Res.15(14),4630-4640(2009)
Nguyen, T., Hawkins, E., Kolluri, A., et al.Synergism between bosutinib (SKI-606) and the Chk1 inhibitor (PF-00477736) in highly imatinib-resistant BCR-ABL+ leukemia cellsLeuk. Res.39,65-71(2015)
