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DRB18

Catalog No. T22317   CAS 2863686-81-9

DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1/S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].

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DRB18 Chemical Structure
DRB18, CAS 2863686-81-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 96.00
5 mg In stock $ 239.00
10 mg In stock $ 378.00
25 mg In stock $ 763.00
50 mg In stock $ 1,230.00
100 mg In stock $ 1,650.00
500 mg In stock $ 3,290.00
1 mL * 10 mM (in DMSO) In stock $ 263.00
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Purity: 98.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1/S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].
In vitro DRB18 (0-10 μM; 30 min) demonstrably decreases glucose absorption in a dose-dependent manner within HEK293 cells expressing GLUT1-4, with inhibitory concentration (IC50) values ranging approximately from 900 nM to 9 μM [1]. Additionally, at concentrations of 5 and 10 μM over 72 hours, DRB18 induces cell cycle arrest at the G1/S phase transition and elevates reactive oxygen species (ROS) levels in A549 cells [1]. Concurrently, it diminishes the expression of the glycosylated forms of GLUT1 and GLUT2-4 in A549 cells, following a dose-responsive relationship [1]. These findings were derived from cell proliferation assays on HEK293 cell lines, and cell cycle as well as western blot analyses on A549 cell lines, underscoring DRB18's multifaceted biochemical impacts.
In vivo DRB18 administered at a dosage of 10 mg/kg intraperitoneally (IP) three times a week for five weeks significantly reduced tumor volume and weight by 44% and 43%, respectively, in male NU/J nude mice aged 3-4 weeks with injected tumor cells. This treatment also resulted in decreased expression of GLUT1-4 and reduced proliferative capacity within the xenografted tumor.
Molecular Weight 382.88
Formula C22H23ClN2O2
CAS No. 2863686-81-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (117.5 mM), Sonification and heating to 60℃ are recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library Anti-Cancer Metabolism Compound Library

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Keywords

DRB18 2863686-81-9 Metabolism transporter DRB 18 DRB-18 inhibitor inhibit

 

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