Molecular Formula | C13H11N3O2 |
Molar Mass | 241.25 |
Solubility | 10 mM in DMSO |
Appearance | crystalline |
Color | brown |
Storage Condition | Store at +4°C |
In vitro study | In RKO and SW480 cells, SU9516 reduced cdk2-specific retinoblastoma protein pRB phosphorylation, increased caspase-3 activation, and altered the cell cycle. SU9516 also inhibits cell proliferation and induces apoptosis in cell lines. SU9516 kills leukemia cells by inhibiting RNA Pol II CTD phosphorylation, oxidative damage, and Mcl-1 transcriptional downregulation. In human T-cell leukemia Jurkat cells, SU9516 significantly enhanced the sensitivity to methotrexate. In addition, SU9516 also inhibits Aurora-A centrosome localization and subsequent centrosome expansion. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.145 ml | 20.726 ml | 41.452 ml |
5 mM | 0.829 ml | 4.145 ml | 8.29 ml |
10 mM | 0.415 ml | 2.073 ml | 4.145 ml |
5 mM | 0.083 ml | 0.415 ml | 0.829 ml |
biological activity | SU9516 is a 3-substituted indolinone CDK inhibitor for CDK2,CDK1, and CDK4 IC50 were 22 nM,40 nM, and 200 nM, respectively. SU9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM,40 nM, and 200 nM for CDK2,CDK1, and CDK4, respectively. |
Target | Value |
CDK2 () | 22 nM |
CDK1 | 40 nM |
CDK4 | 200 nM |