Name | NSC 663284 |
Synonyms | NSC 663284 CDC25 Phosphatase Inhibitor II, NSC 663284 5,8-Quinolinedione, 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]- |
CAS | 383907-43-5 |
Molecular Formula | C15H16ClN3O3 |
Molar Mass | 321.76 |
Density | 1.41±0.1 g/cm3(Predicted) |
Boling Point | 478.8±45.0 °C(Predicted) |
Solubility | DMSO: ≥150 mg/mL |
Appearance | solid |
Color | red |
pKa | 6.79±0.10(Predicted) |
Storage Condition | 2-8°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 1 month. |
Sensitive | Light Sensitive |
In vitro study | NSC 663284 (3-100μM; 48 hours) has a mean IC 50 value in the NCI 60 Cell human tumor panel of 1.5 ± 0.6 μM, has IC 50 values of 0.2 μM in human breast cancer MDA-MB-435 and MDA-N cells, has an IC 50 value of 1.7 μM in human breast MCF-7 cells in culture. NSC 663284 has relative IC 50 values for Cdc25B2 (IC 50 =0.21 μM) are 20- and 450-fold lower than for VHR (IC 50 =4.0 μM) or PTP1B (IC 50 >4.0 μM), respectively. |
In vivo study | NSC 663284 (intravenous injection; 2, 3, and 5mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single dose of 5 mg/kg, NSC 663284 is not detectable in plasma or tissues beyond 5 min. Following NSC 663284 treatment of tumor-bearing SCID mice, reduces glutathione concentrations in HT29 tumor are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys. |
Hazard Symbols | Xi - Irritant![]() |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.108 ml | 15.54 ml | 31.079 ml |
5 mM | 0.622 ml | 3.108 ml | 6.216 ml |
10 mM | 0.311 ml | 1.554 ml | 3.108 ml |
5 mM | 0.062 ml | 0.311 ml | 0.622 ml |
biological activity | NSC 663284 is a potent, cell-permeable and irreversible inhibitor of Cdc25 dual specificity, the IC50 of Cdc25B2 was 0.21 μm. NSC 663284 exhibited mixed competition kinetics with Cdc25A,Cdc25B2 and Cdc25C with Ki values of 29, 95 and 89 nM, respectively. NSC 663284 inhibits the activity of the NSD2 (IC50 of 170 nM) enzyme by interacting with the SET domain (Kd of 370 nM). |
Target | IC50: 0.21 μm (Cdc25B2) |