| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
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| Other Sizes |
| Targets |
TC-T 6000 targets equilibrative nucleoside transporter 4 (ENT4), a transporter involved in the cellular uptake of nucleosides and nucleoside analog drugs. By inhibiting ENT4, TC-T 6000 modulates nucleoside transport and has vasodilator activity. It inhibits hENT1 and hENT2 as well, but with lower potency. The compound is used for the study of cancer and cardiovascular injury.
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| ln Vitro |
In vitro, TC-T 6000 is a potent ENT4 inhibitor with an IC50 of 74.4 nM. It exhibits 20-fold and 80-fold selectivity for ENT4 over ENT2 and ENT1, respectively. The compound has vasodilator activity and is used to study nucleoside transport in cancer and cardiovascular disease.
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| ln Vivo |
In vivo, TC-T 6000 has vasodilator activity and is used for the study of cancer and cardiovascular injury. By inhibiting ENT4, the compound modulates nucleoside transport and may affect adenosine signaling and vascular function. Detailed in vivo data are available in research publications.
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| Enzyme Assay |
In vitro transporter assays for TC-T 6000 measure its inhibition of ENT4-mediated nucleoside uptake. Cells expressing ENT4 are incubated with radiolabeled nucleoside substrates and varying concentrations of the compound. Nucleoside uptake is measured by scintillation counting, and IC50 values are calculated from dose-response curves. An IC50 of 74.4 nM is determined for ENT4.
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| Cell Assay |
In vitro cell-based assays for TC-T 6000 use cells expressing ENT4, ENT1, or ENT2 to assess transporter inhibition. Cells are treated with serial dilutions of the compound, and nucleoside uptake is measured using radiolabeled substrates. Selectivity for ENT4 over ENT1 and ENT2 is determined by comparing IC50 values. Cell viability is assessed in parallel.
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| Animal Protocol |
In vivo animal models for TC-T 6000 include models of cancer and cardiovascular injury. The compound is administered via appropriate routes, and its effects on tumor growth, vascular function, and disease progression are evaluated. Pharmacodynamic studies measure ENT4 inhibition and nucleoside transport in target tissues.
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| ADME/Pharmacokinetics |
TC-T 6000 has a molecular formula of C26H48N8O2 and a molecular weight of 504.71 g/mol. It is also known as hENT4-IN-1 and TC-T6000. The compound has a purity of ≥98% and is soluble in DMSO at 10.09 mg/mL. It is stored as a powder at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
The toxicity profile of TC-T 6000 is characterized in preclinical safety studies. As an ENT4 inhibitor, the compound may affect nucleoside homeostasis and vascular function. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
TC-T 6000 (hENT4-IN-1) is a selective and potent inhibitor of human equilibrative nucleoside transporter 4 (ENT4) with an IC50 of 74.4 nM. It exhibits 20-fold and 80-fold selectivity for ENT4 over ENT2 and ENT1, respectively. TC-T 6000 has vasodilator activity and is used for the study of cancer and cardiovascular injury. It is also known as hENT4-IN-1 and is intended for laboratory research use only.
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| Molecular Formula |
C26H48N8O2
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|---|---|
| Molecular Weight |
504.72
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| Exact Mass |
504.39
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| CAS # |
949467-71-4
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| PubChem CID |
16757265
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
660.0±65.0 °C at 760 mmHg
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| Flash Point |
352.9±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.609
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| LogP |
4.45
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
36
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| Complexity |
524
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CN(CC(C)C)C1=NC(=NC2=C1N=C(N=C2N(CC(C)C)CC(C)C)NCCO)NCCO
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| InChi Key |
KIZLZYHFIWWKIL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H48N8O2/c1-17(2)13-33(14-18(3)4)23-21-22(30-25(31-23)27-9-11-35)24(32-26(29-21)28-10-12-36)34(15-19(5)6)16-20(7)8/h17-20,35-36H,9-16H2,1-8H3,(H,27,30,31)(H,28,29,32)
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| Chemical Name |
2-[[4,8-bis[bis(2-methylpropyl)amino]-2-(2-hydroxyethylamino)pyrimido[5,4-d]pyrimidin-6-yl]amino]ethanol
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| Synonyms |
TC-T6000; TCT 6000; TCT6000
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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 : ≥ 125 mg/mL (~247.67 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 | 1.9813 mL | 9.9065 mL | 19.8130 mL | |
| 5 mM | 0.3963 mL | 1.9813 mL | 3.9626 mL | |
| 10 mM | 0.1981 mL | 0.9906 mL | 1.9813 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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