| Chemical Properties | Back Directory | [Boiling point ]
610.191±50.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.315±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [storage temp. ]
-10 to -25°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
10.178±0.10(predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Class I glucose transporters (GLUT1-4) inhibitor with greater anti-cancer efficacy than WZB117 (WZB-117) in cultures and in vivo.
DRB18 is a class I glucose transporters (GLUT1-4) inhibitor (glucose uptake IC50 = 2.6/8.8/4.5/0.9 μM using HEK293 GLUT1/2/3/4 transfectants) th at exhibits greater anti-cancer efficacy than WZB117 (WZB-117) in cultures (IC50 <10 μM in 51 of 60 cancer cultures tested vs. only 17 from the same 60 cultures when using WZB117) and suppresses A549 xenografts-derived tumor growth in mice in vivo (44% reduction with 10 mg/kg i.p. 3x per wk for 5 wks) by altering the abundance of metabolites in glucose-related pathways. | [in vivo]
DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43%[1]. | 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. |
| [References]
[1] Shriwas P, Roberts D, Li Y, et al. A small-molecule pan-class I glucose transporter inhibitor reduces cancer cell proliferation in vitro and tumor growth in vivo by targeting glucose-based metabolism. Cancer Metab. 2021;9(1):14. Published 2021 Mar 26. DOI:10.1186/s40170-021-00248-7 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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