| 应用 |
a novel pan-Cdk inhibitor inactive against 34 other kinases. |
| 产品介绍 |
PHA-793887是一种新型有效的CDK2，CDK5和CDK7抑制剂，IC50分别为8 nM， 5 nM 和10 nM，作用于CDK2， 5，和7比作用于CDK1， 4，和9选择性高6倍以上。 |
| 备注 |
PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. Phase 1. |
| 生化机理 |
PHA-793887 is a novel pan-Cdk inhibitor, including Cdk1, Cdk2, Cdk4, Cdk5, Cdk7, and Cdk9 with IC50’s in the 5 to 140 nM range. PHA-793887 is inactive against 34 other kinases representative of all kinase families, in particular c-abl, c-kit, lck, and TRKA with IC50>10 mM. PHA-793887 shows anti-proliferative activity against several solid tumor cell lines, with IC50<1 mM; in these cells, it is able to inhibit Rb phosphorylation and expression of S-phase cyclins, such as cyclin A. |
| 别名 |
PHA 793887;PHA793887; 3-甲基-N-[1,4,5,6-四氢-6,6-二甲基-5-[(1-甲基-4-哌啶基)甲酰基]吡咯并[3,4-c]吡唑-3-基]丁酰胺;PHA 793887;PHA793887;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 |
