| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
GLUT[1]
The primary targets of DRB18 are glucose transporters (GLUTs), including GLUT1, GLUT2, GLUT3, and GLUT4. GLUTs are membrane proteins that facilitate the uptake of glucose into cells. DRB18 is a pan-GLUT inhibitor that inhibits glucose uptake in cells expressing these transporters. By inhibiting glucose uptake, DRB18 disrupts cellular energy metabolism. |
|---|---|
| ln Vitro |
With an IC50 range from approximately 900 nM to approximately 9 μM, DRB18 (0-10 μM; 30 min) decreases glucose absorption in the HEK293 cell line expressing GLUT1-4 in a dose-dependent manner [1]. Cell cycle arrest is caused by DRB18 (5 and 10 μM; 72 hours) at the G1/S phase transition [1]. In A549 cells, DRB18 (5 and 10 μM; 72 hours) raises ROS levels [1]. In A549 cells, DRB18 (5 and 10 μM; 72 hours) dose-dependently decreases the expression of glycosylated GLUT1 and GLUT2-4 [1].
DRB18 is a potent pan-GLUT inhibitor that inhibits glucose uptake in HEK293 cells expressing GLUT1, GLUT2, GLUT3, or GLUT4 with IC50 values of 2.6, 8.8, 4.5, and 0.9 µM, respectively. It alters the abundance of metabolites in glucose-related pathways and changes energy-related metabolism in A549 cells. DRB18 can eventually lead to G1/S phase arrest, increased oxidative stress, and necrotic cell death. It exhibits antitumor activity. |
| ln Vivo |
For five weeks, DRB18 (10 mg/kg; intraperitoneal injection; three times per week) reduced tumor weight and volume by 43% and 44%, respectively[1].
In vivo, DRB18 exhibits antitumor activity. By inhibiting glucose uptake and disrupting cellular energy metabolism, it can inhibit tumor growth and proliferation. Its efficacy would be assessed in animal models of cancer, with endpoints including tumor growth inhibition, analysis of glucose metabolism, and assessment of cell death pathways. |
| Enzyme Assay |
In vitro binding and enzyme activity assays for DRB18 typically involve measuring its ability to inhibit glucose uptake. Glucose uptake assays are performed using HEK293 cells expressing GLUT1, GLUT2, GLUT3, or GLUT4. Cells are incubated with radiolabeled glucose or a fluorescent glucose analog in the presence of increasing concentrations of DRB18, and the inhibition of glucose uptake is measured. The reported IC50 values are 2.6, 8.8, 4.5, and 0.9 µM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively.
|
| Cell Assay |
Cell Proliferation Assay
Cell Types: GLUT1-4-expressed HEK293 cell lines[1] Tested Tested Concentrations: 0-10 μM Incubation Duration: 30 min Experimental Results: diminished glucose uptake in these cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM. Cell Cycle Analysis Cell Types: A549[1] Tested Tested Concentrations: 5 and 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Caused cell cycle arrest in the G1/S phase transition. Western Blot Analysis Cell Types: A549[1] Tested Tested Concentrations: 5 and 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: diminished expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner. Western Blot Analysis Cell Types: A549[1] Tested Tested Concentrations: 5 and 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: diminished expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner. Cellular assays for DRB18 involve treating cancer cell lines (such as A549 cells) with the compound and measuring its effects on glucose metabolism, cell cycle progression, and cell death. Readouts include changes in metabolite levels in glucose-related pathways, G1/S phase arrest, increased oxidative stress, and necrotic cell death. The compound's antitumor activity is assessed by measuring cell viability and proliferation. |
| Animal Protocol |
Animal/Disease Models: Male NU/J nude mice (3-4 weeks; tumor cell-injected)[1]
Doses: 10 mg/kg Route of Administration: IP; thrice a week for 5 weeks Experimental Results: The tumors were 44% smaller by volume and 43% smaller by weight, also demonstrated DRB18 diminished expression of GLUT1-4 (Fig. 5f) and decreased proliferative capacity within the xenografted tumor. In vivo efficacy of DRB18 would be evaluated in mouse xenograft models of cancer. The compound could be administered orally or via injection. Efficacy endpoints would include tumor growth inhibition, analysis of glucose metabolism in tumor tissue, and assessment of cell death pathways. |
| ADME/Pharmacokinetics |
DRB18 has a molecular weight of 382.88 and a molecular formula of C22H23ClN2O2. It is a potent pan-inhibitor of glucose transporters (GLUTs). DRB18 inhibits glucose uptake in HEK293 cells expressing GLUT1, GLUT2, GLUT3, or GLUT4 with IC50 values of 2.6, 8.8, 4.5, and 0.9 µM, respectively. It exhibits antitumor activity and is supplied with a purity of 99.54%. The compound is for research use only and is not intended for human therapeutic use.
|
| Toxicity/Toxicokinetics |
No specific toxicity data is available for DRB18 in the provided literature. As a research compound, its safety profile would be an important consideration for in vivo applications. Potential toxicities could be related to its effects on glucose metabolism in normal tissues. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications. The compound is for research use only and is not intended for human therapeutic use.
|
| References | |
| Additional Infomation |
DRB18 is a potent pan-inhibitor of glucose transporters (GLUTs). It inhibits glucose uptake in HEK293 cells expressing GLUT1, GLUT2, GLUT3, or GLUT4 with IC50 values of 2.6, 8.8, 4.5, and 0.9 µM, respectively. DRB18 alters energy-related metabolism in A549 cells, leading to G1/S phase arrest, increased oxidative stress, and necrotic cell death. It exhibits antitumor activity. DRB18 has a molecular formula of C22H23ClN2O2 and a molecular weight of 382.88.
|
| Molecular Formula |
C22H23CLN2O2
|
|---|---|
| Molecular Weight |
382.883224725723
|
| Exact Mass |
382.144
|
| CAS # |
2863686-81-9
|
| PubChem CID |
154824629
|
| Appearance |
White to yellow solid powder
|
| LogP |
5.5
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
452
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(C=C(C=C1)CNC2=C(C=C(C=C2)Cl)NCC3=CC(=C(C=C3)C)O)O
|
| InChi Key |
WNTAQMQIZGJASL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H23ClN2O2/c1-14-3-5-16(9-21(14)26)12-24-19-8-7-18(23)11-20(19)25-13-17-6-4-15(2)22(27)10-17/h3-11,24-27H,12-13H2,1-2H3
|
| Chemical Name |
5-[[4-chloro-2-[(3-hydroxy-4-methylphenyl)methylamino]anilino]methyl]-2-methylphenol
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 50 mg/mL (130.59 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
