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| Targets |
GLUT inhibitor-1 targets glucose transporters GLUT1 and GLUT3. These transporters are responsible for the uptake of glucose into cells. Inhibition of GLUT1 and GLUT3 deprives cancer cells of glucose, an essential nutrient for their growth and survival. The compound has IC50 values of 242 nM for GLUT1 and 179 nM for GLUT3.
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| ln Vitro |
In vitro, GLUT inhibitor-1 is a potent inhibitor of GLUT1 and GLUT3 with IC50s of 242 nM and 179 nM, respectively. It is used to study the role of glucose transporters in cancer and autoimmune diseases. The compound shows potent inhibition of glucose uptake in cells expressing these transporters.
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| ln Vivo |
Summary of pharmacokinetic data of GLUT inhibitor-1 (compound 15b; 30 mg/kg) in mice and rats [1]. Parameters Mouse Rat Oral Cmax (ng/mL) 2525 1675 Oral AUC (ng/mL) 5890 6813 CL (mL/min/kg) 40 37 Vdss (L/Kg) 1.70 4.51 t1/2 (h) 0.785 2.59 F (% ) 45.4 49.4 B/Pb 0.05 b: Solubility evaluated in PBS buffer solution.
In vivo, GLUT inhibitor-1 is orally active and has been studied in pharmacokinetic studies in mice and rats. At 30 mg/kg, the oral Cmax is 2525 ng/mL in mice and 1675 ng/mL in rats; the oral AUC is 5890 ng/mL in mice and 6813 ng/mL in rats. The oral bioavailability is 45.4% in mice and 49.4% in rats. |
| Enzyme Assay |
The in vitro transporter inhibition assay for GLUT inhibitor-1 involves measuring glucose uptake in cells expressing GLUT1 or GLUT3 in the presence of the compound. The IC50 values are determined by quantifying the reduction in glucose uptake. Radiolabeled or fluorescent glucose analogs are used as substrates.
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| Cell Assay |
In vitro cell-based assays for GLUT inhibitor-1 involve treating cancer cells with the compound and assessing cell viability, glucose uptake, and metabolic changes. The compound’s effects on cell proliferation and survival are evaluated in the context of glucose deprivation.
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| Animal Protocol |
In vivo animal studies for GLUT inhibitor-1 involve pharmacokinetic studies in mice and rats. Efficacy studies would involve xenograft mouse models of cancer or autoimmune disease models, where the compound would be administered orally and disease progression monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GLUT inhibitor-1 have been reported in mice and rats. At 30 mg/kg oral dose, the Cmax is 2525 ng/mL (mouse) and 1675 ng/mL (rat); AUC is 5890 (mouse) and 6813 (rat) ng/mL; CL is 40 (mouse) and 37 (rat) mL/min/kg; Vdss is 1.70 (mouse) and 4.51 (rat) L/kg; t1/2 is 0.785 (mouse) and 2.59 (rat) h; oral bioavailability is 45.4% (mouse) and 49.4% (rat).
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| Toxicity/Toxicokinetics |
No specific toxicity data for GLUT inhibitor-1 are available in the provided literature. The compound is for research use only.
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| References | |
| Additional Infomation |
GLUT inhibitor-1 is a potent, orally active inhibitor of GLUT1 and GLUT3. It has IC50s of 242 nM and 179 nM, respectively. It is being studied for cancer and autoimmune diseases. It is for research use only. Its CAS number is 2421141-40-2.
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| Molecular Formula |
C32H35N7O2
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| Molecular Weight |
549.67
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| Exact Mass |
549.285
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| CAS # |
2421141-40-2
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| PubChem CID |
156020834
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
41
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| Complexity |
889
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NC1(C)CC1)(=O)COC1=CC=CC(C2=NC(NC3=CC=C(C4=CNN=C4)C=C3)=C3CN(C4CCC4)CCC3=N2)=C1
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| InChi Key |
IXZVJTRRPOHKJF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H35N7O2/c1-32(13-14-32)38-29(40)20-41-26-7-2-4-22(16-26)30-36-28-12-15-39(25-5-3-6-25)19-27(28)31(37-30)35-24-10-8-21(9-11-24)23-17-33-34-18-23/h2,4,7-11,16-18,25H,3,5-6,12-15,19-20H2,1H3,(H,33,34)(H,38,40)(H,35,36,37)
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| Chemical Name |
2-[3-[6-cyclobutyl-4-[4-(1H-pyrazol-4-yl)anilino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-2-yl]phenoxy]-N-(1-methylcyclopropyl)acetamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~181.93 mM)
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| 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 | 1.8193 mL | 9.0964 mL | 18.1927 mL | |
| 5 mM | 0.3639 mL | 1.8193 mL | 3.6385 mL | |
| 10 mM | 0.1819 mL | 0.9096 mL | 1.8193 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.
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