PHA-793887
Cat. No.：YN270092
CAS No. ：718630-59-2
| 产品名称: | PHA-793887 |
| CAS No.: | 718630-59-2 |
| Chemical Name: | 3-methyl-N-[1,4,5,6-tetrahydro-6,6-dimethyl-5-[(1-methyl-4-piperidinyl)carbonyl]pyrrolo[3,4-c]pyrazol-3-yl]-butanamide |
| Synonyms: | PHA 793887,PHA793887 |
| 分子量: | 361.48 |
| 分子式: | C₁₉H₃₁N₅O₂ |
| SMILES: | CC(C)CC(NC1=NNC2=C1CN(C(C3CCN(C)CC3)=O)C2(C)C)=O |
| 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: | PHA-793887 是一种有效的，ATP 竞争性的CDK抑制剂，可抑制 Cdk2，Cdk1，Cdk4 和 Cdk9 的活性，IC50值分别为 8 nM，60 nM，62 nM 和 138 nM，同时可抑制糖原合酶激酶 3β (GSK-3β)，IC50值为 79 nM。 |
| IC50和靶点: | [{name:"Cdk5/p25:5 nM (IC50)"},{name: "cdk2/cyclin A:8 nM (IC50)"},{name: "CDK2/cyclinE:8 nM (IC50)"},{name: "CDK7/cyclin H:10 nM (IC50)"},{name: "Cdk1/cyclin B:60 nM (IC50)"},{name: "Cdk4/cyclin D1:62 nM (IC50)"},{name: "CDK9/cyclinT1:138 nM (IC50)"},{name: "GSK-3β:79 nM (IC50)"}] |
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| Solvent & Solubility: |
Brasca, M.G., Albanese, C., Alzani, R., et al.Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosingBioor. Med. Chem.18(5),1844-1853(2010)
Vargas, B., Giacobbi, N.S., Sanyal, A., et al.Inhibitors of signaling pathways that block reversal of HIV-1 latencyAntimicrob. Agents Chemother.63(2),e01744-01718(2019)
Alzani, R., Pedrini, O., Albanese, C., et al.Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia modelsExp. Hematol.38,259-269(2010)
