1-(2-(2-(Dimethylamino)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-5-yl)urea
UNBS5162
CAS: 956590-23-1
Molecular Formula: C17H18N4O3
1-(2-(2-(Dimethylamino)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-5-yl)urea - Names and Identifiers
1-(2-(2-(Dimethylamino)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-5-yl)urea - Physico-chemical Properties
| Molecular Formula | C17H18N4O3 |
| Molar Mass | 326.35 |
| Density | 1.389±0.06 g/cm3(Predicted) |
| Boling Point | 526.4±35.0 °C(Predicted) |
| Solubility | DMSO: 21.5 mg/mL |
| pKa | 13.50±0.20(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| In vitro study | PC-3 cells were exposed to 1 μm UNBS5162 for 5 consecutive days. UNBS5162 can significantly reduce the expression of CXCL cytokines that promote angiogenesis. UNBS5162 has relatively weak anti-proliferative activity in vitro, with IC50 of 17.3 μm in PC-3, DU-145, U373-MG, Hs683, HCT-15, LoVo, MCF-7, A549 and Bx-PC-3 cells, respectively, 16 μm, 4.7 μm, 8.5 μm, 28.8 μm, 8.9 μm, 46.5 μm, 21.2 μm, 9.1 μm. 10 μm UNBS5162 significantly disrupts PC-3 tumor cell growth kinetics without inducing senescence; In DU-145 cells, UNBS5162 has reverse properties, this may depend on the p53 status and/or the degree of p16 expression of both cells. At a concentration of 1 μm, UNBS5162 did not induce such an antitumor effect. 10 μm UNBS5162 in PC-3 cells can increase the level of heterochromatin by increasing the number of histones-at least at the level of mRNA. In the experimental prostate cancer model, UNBS5162 can reduce the level of CXC chemokine ligands, such as CXCL1, CXCL5 and CXCL8, and has a good proliferation inhibition effect on the proliferation of tumor cells in vitro and in vivo. In SKOV3 ovarian cancer cells, it can inhibit cell proliferation, invasion and migration through PI3K/AKT signaling pathway, and promote cell apoptosis. |
| In vivo study | In a Human Orthotopic prostate cancer model, repeated administration of UNBS5162 significantly improved the survival cycle. The pharmacokinetics of UNBS5162 in female mice showed relatively low systemic exposure after oral administration of 80 mg/kg, Cmax = 510 ng/ml,AUC0-∞ = 886 ng · h/ml, its absolute bioavailability is only 3.84%. The volume of distribution and the total volume were 18.9 L/kg and 3.47 L/h/kg, respectively. After intravenous injection (tail) of 20 mg/kg UNBS5162, its half-life is about 3.8 hours, and its plasma concentration is maintained at 10 μm for about 30 minutes, maintain at 1 μm level for about 2 hours. |
1-(2-(2-(Dimethylamino)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-5-yl)urea - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.064 ml | 15.321 ml | 30.642 ml |
| 5 mM | 0.613 ml | 3.064 ml | 6.128 ml |
| 10 mM | 0.306 ml | 1.532 ml | 3.064 ml |
| 5 mM | 0.061 ml | 0.306 ml | 0.613 ml |
Last Update：2024-01-02 23:10:35
1-(2-(2-(Dimethylamino)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-5-yl)urea - Reference Information
| biological activity | UNBS5162 is an antagonist of CXCL chemokine expression in a range of human cancer cells including malignant gliomas (Hs683 and U373MG) cytotoxicity in colorectal cancer (HCT-15 and LoVo), breast cancer cells (MCF-7) with IC50 ranging from 0.5-5 μm. |
| Target | Value |
Last Update：2024-04-09 20:13:35
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Product Name: UNBS5162 Visit Supplier Webpage Request for quotation
CAS: 956590-23-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 956590-23-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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