SCH 727965
Dinaciclib (SCH727965)
CAS: 779353-01-4
Molecular Formula: C21H28N6O2
SCH 727965 - Names and Identifiers
SCH 727965 - Physico-chemical Properties
| Molecular Formula | C21H28N6O2 |
| Molar Mass | 396.49 |
| Density | 1.33 |
| Melting Point | >78oC (dec.) |
| Solubility | Chloroform (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Light Beige |
| pKa | 15.15±0.10(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| Stability | Hygroscopic |
| In vitro study | The effects of Dinaciclib on CDK1 and CDK9 were comparable, but the effects on CDK2 and CDK5 were 12 and 14-fold stronger, respectively. Dinaciclib acts on A2780 cells, effectively inhibits DNA replication, inhibits DNA uptake by dThd, with an IC50 of 4 nM. At concentrations greater than 6.25 nM, Dinaciclib strongly inhibited phosphorylation of Rb at the Ser 807/811 site. Complete inhibition of Rb phosphorylation was associated with apoptosis, expressed by the presence of p85 PARP cleavage products in cells treated with Dinaciclib at concentrations greater than 6.25 nM. Dinaciclib effectively acts on a broad spectrum of human tumor cell lines. Addition of Dinaciclib during hydroxyurea treatment also inhibited γ-H2AX accumulation in a dose-dependent manner. Dinaciclib inhibits the proliferation of malignant melanoma cells and induces large-scale apoptosis of malignant melanoma cells. Dinaciclib induces apoptosis in several osteosarcoma cell lines, including anti-Doxorubicin and Dasatinib cells. Dinaciclib reduces RNAP II phosphorylation at serine 2 and also reduces CDK inhibitor p27 |
| In vivo study | Daily intraperitoneal administration of Dinaciclib at doses of 8, 16, 32, and 48 mg/kg for 10 days resulted in tumor suppression of 70%, 89%, 96%, and, respectively. Dinaciclib MED (minimum effective dose) is approximately less than 8 mg/kg. The drug resistance of Dinaciclib was good, and the highest weight loss was 5% in the highest dose treatment group. Dinaciclib has anti-cancer activity in vivo in a dose-dependent manner, treating at a dose level below the MTD (the highest tolerated dose), almost completely inhibiting tumor growth. Dinaciclib acts on mice and has a short plasma half-life. |
SCH 727965 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.522 ml | 12.611 ml | 25.221 ml |
| 5 mM | 0.504 ml | 2.522 ml | 5.044 ml |
| 10 mM | 0.252 ml | 1.261 ml | 2.522 ml |
| 5 mM | 0.05 ml | 0.252 ml | 0.504 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Dinaciclib (SCH727965) Visit Supplier Webpage Request for quotationCAS: 779353-01-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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