Molecular Formula | C18H13N3OS2 |
Molar Mass | 351.45 |
Density | 1.41 |
Boling Point | 569.1±60.0 °C(Predicted) |
Solubility | DMSO: ≥ 47 mg/mL |
Appearance | powder |
Color | white to light brown |
pKa | 3.99±0.10(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
In vitro study | RO-3306 inhibition of CDK1/cyclin B1,CDK1/cyclin A,CDK2/cyclin E, and CDK4/cyclin D activity, Ki 35 nM,110 nM,340 nM, and> 2000 nM. Treatment of HCT116,SW480, and HeLa cells with RO-3306 for 20 hours resulted in complete cell cycle arrest at G2/M phase. The proliferation of HCT116 and SW480 was effectively blocked by RO-3306. RO-3306 appears to have a stronger pro-apoptotic effect in cancer cells (HCT116 and SW480) than in non-tumorigenic cells (MCF 10A and MCF 12A). RO-3306 of the 10 μm concentration effectively prevented oocyte maturation. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.845 ml | 14.227 ml | 28.454 ml |
5 mM | 0.569 ml | 2.845 ml | 5.691 ml |
10 mM | 0.285 ml | 1.423 ml | 2.845 ml |
5 mM | 0.057 ml | 0.285 ml | 0.569 ml |
biological activity | RO-3306 is a competitive selective CDK1 inhibitor of ATP, Ki is 20 nM, and the selectivity is 15 times that of other human kinases. RO-3306 can enhance p53-mediated Bax activation and mitochondrial apoptosis. |
target | TargetValue CDK1 (Cell-Free Assay) 20 nM(Ki) PKCδ (Cell-Free Assay) 318 nM(Ki) SGK (Cell-Free Assay) 497 nM(Ki) ERK (Cell-Free Assay) 1980 nM(Ki) |
Target | Value |
CDK1 (Cell-free assay) | 20 nM(Ki) |
PKCδ (Cell-free assay) | 318 nM(Ki) |
SGK (Cell-free assay) | 497 nM(Ki) |
ERK (Cell-free assay) | 1980 nM(Ki) |
in vitro study | RO-3306 inhibit CDK1/cyclin B1,CDK1/cyclin A,CDK2/cyclin E, and CDK4/cyclin D activities, Ki is 35 nM,110 nM,340 nM, respectively, and> 2000 nM. HCT116,SW480, and HeLa cells treated with RO-3306 for 20 hours resulted in complete cell cycle arrest in G2/M phase. The proliferation of HCT116 and SW480 was effectively blocked by RO-3306. RO-3306 appeared to have a stronger pro-apoptotic effect in cancer cells (HCT116 and SW480) than in non-tumorigenic cells (MCF 10A and MCF 12A). RO-3306 at a concentration of 10 μM effectively prevented oocyte maturation. |