[CAS NO. 2863686-81-9] DRB18
PRODUCTS SPECIFICATIONS [2863686-81-9]
DESCRIPTION [2863686-81-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 382.88 |
| Molecular Formula | C22H23ClN2O2 |
| SMILES | ClC1=CC(NCC2=CC(O)=C(C)C=C2)=C(NCC3=CC=C(C)C(O)=C3)C=C1 |
Summary
DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity [1] .
IC50 & Target
GLUT [1]
In Vitro
DRB18 (0-10 μM; 30 min) reduces glucose uptake in GLUT1-4-expressed HEK293 cell lines in a dose-dependent manner with IC
50
s varying from ~ 900 nM to ~ 9 μM
[1]
.
DRB18 (5 and 10 μM; 72 hours) causes cell cycle arrest in the G1/S phase transition
[1]
.
DRB18 (5 and 10 μM; 72 hours) increases ROS levels in A549 cells
[1]
.
DRB18 (5 and 10 μM; 72 hours) reduces expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
| Cell Line: | GLUT1-4-expressed HEK293 cell lines [1] |
| Concentration: | 0-10 μM |
| Incubation Time: | 30 min |
| Result: | Reduced glucose uptake in these cell lines in a dose-dependent manner with IC 50 s varying from ~ 900 nM to ~ 9 μM. |
Cell Cycle Analysis
| Cell Line: | A549 [1] |
| Concentration: | 5 and 10 μM |
| Incubation Time: | 72 hours |
| Result: | Caused cell cycle arrest in the G1/S phase transition. |
Western Blot Analysis
| Cell Line: | A549 [1] |
| Concentration: | 5 and 10 μM |
| Incubation Time: | 72 hours |
| Result: | Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner. |
Western Blot Analysis
| Cell Line: | A549 [1] |
| Concentration: | 5 and 10 μM |
| Incubation Time: | 72 hours |
| Result: | Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner. |
In Vivo
DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43% [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male NU/J nude mice (3-4 weeks; tumor cell-injected) [1] |
| Dosage: | 10 mg/kg |
| Administration: | IP; thrice a week for 5 weeks |
| Result: | The tumors were 44% smaller by volume and 43% smaller by weight, also showed DRB18 decreased expression of GLUT1-4 (Fig. 5f) and reduced proliferative capacity within the xenografted tumor. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 130.59 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6118 mL | 13.0589 mL | 26.1178 mL |
| 5 mM | 0.5224 mL | 2.6118 mL | 5.2236 mL |
| 10 mM | 0.2612 mL | 1.3059 mL | 2.6118 mL |