CDK抑制剂(ROSCOVITINE)
Roscovitine (Seliciclib,CYC202)
CAS: 186692-46-6
Molecular Formula: C19H26N6O
CDK抑制剂(ROSCOVITINE) - Names and Identifiers
CDK抑制剂(ROSCOVITINE) - Physico-chemical Properties
| Molecular Formula | C19H26N6O |
| Molar Mass | 354.45 |
| Density | 1.3 |
| Melting Point | 106～107℃ |
| Boling Point | 577.5±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 10 mg/ml, with warming) or in Ethanol (up to 10 mg/ml). |
| Appearance | White to off-white solid |
| Color | White |
| pKa | 14.56±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| MDL | MFCD02266401 |
| Use | Roscovitine (Seliciclib,CYC202) is an effective and selective CDK inhibitor. When acting on Cdc2, CDK2 and CDK5, the IC50 is 0.65 μM, 0.7 μM and 0.16 μM, respectively, with little inhibitory effect on CDK4/6. Phase 2. |
| In vitro study | Roscovitine acts on cyclin-dependent kinases with high efficiency and high selectivity, with IC50 of 0.65 and 0.7 when acting on cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E and cdk5/p53, respectively, 0.7 and 0.16 μm. Nanomolar Roscovitine acts on starfish oocytes and sea urchin embryos, reversibly inhibits the transformation during the anterior middle period, and acts on the Xenopus laevis egg extract in vitro, inhibiting the activity of M-phase promoting factor and in vitro DNA synthesis, and inhibit the proliferation of mammalian cell lines, IC50 is 16 M. Roscovitine at concentrations of 7.5, 12.5, and 25 mM acted on mesangial cells resulting in a 25,50, and 100% decrease in CDK2 activity, respectively, in a dose-dependent manner. Recent studies have shown that Roscovitine acts on Dicostelium discoidosa to inhibit cdk5 kinase activity, cell proliferation, multicellular development, and cdk5 nuclear transport, without affecting cdk5 protein expression. |
| In vivo study | Roscovitine at a dose of 50 mg/kg significantly inhibited tumor growth in the Ewing's Sarcoma Family (ESFT) xenografts. Roscovitine acts on Nude Mice carrying MCF7 transplanted tumors to enhance the anticancer effect of anticancer Doxorubicin without increasing toxicity, and the mechanism is to arrest the cell cycle rather than cause apoptosis. |
CDK抑制剂(ROSCOVITINE) - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| HS Code | 29335990 |
CDK抑制剂(ROSCOVITINE) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.821 ml | 14.106 ml | 28.213 ml |
| 5 mM | 0.564 ml | 2.821 ml | 5.643 ml |
| 10 mM | 0.282 ml | 1.411 ml | 2.821 ml |
| 5 mM | 0.056 ml | 0.282 ml | 0.564 ml |
Last Update：2024-01-02 23:10:35
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