TTT-28
Based on 1 Customer Validation
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1609138-51-3
- Formula: C31H31N3O6S
- Molecular Weight:573.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
1 μM
Compound: 28
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Inhibition of human wild type P-gp expressed in BacMam virus infected human HeLa cells assessed as calcein-AM accumulation after 10 mins by flow cytometry
Inhibition of human wild type P-gp expressed in BacMam virus infected human HeLa cells assessed as calcein-AM accumulation after 10 mins by flow cytometry
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[PMID: 24773054] |
TTT-28 (0-100 μM; 72 hours) reverses ABCB1-mediated MDR in drug selected SW620/Ad300 cells and transfected HEK293/ABCB1 cells; the IC50s of TTT-28 in CCD-18Co, SW620 and SW620/Ad300 cells are 213.4±11.0 μM, 89.4±3.9 μM and 92.0±5.0 μM, respectively[1]. TTT-28 (10 μM; 2 hours) raises the ABCB1-mediated MDR and increased the accumulation of [3H]-paclitaxel in ABCB1 overexpressing cells[1]. TTT-28 (10 μM; 0-72 hours) does not interfer with the expression level and localization of ABCB1, it results from blocking the efflux function of ABCB1[1]. TTT-28 (0-40 μM; 2 hours) interacts at the drug-substrate-binding site and actives the ATPase activity of ABCB1 in a concentration-dependent fashion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620 cells, SW620/Ad300 cells
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Concentration:0.1 μM, 1 μM, 10 μM, 100 μM
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Incubation Time:72 hours
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Result:Decreased the resistance fold of ABCB1 substrates (Paclitaxel, Doxorubicin, Vincristine) in SW620/Ad300 cells compared to SW620 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells
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Dosage:30 mg/kg
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Administration:Deliver orally; every 3rd day; 18 days
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Result:Lead to higher intratumoral accumulation of paclitaxel in tumors.
Chemical Information
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CAS No. 1609138-51-3
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Appearance Solid
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Molecular Weight 573.66
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Formula C31H31N3O6S
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Color White to off-white
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SMILES
O=C(N[C@@H](C(C)C)C1=NC(C(NC2=CC=CC=C2C(C3=CC=CC=C3)=O)=O)=CS1)C4=CC(OC)=C(OC)C(OC)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 250 mg/mL (435.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7432 mL | 8.7160 mL | 17.4319 mL | 43.5798 mL |
| 5 mM | 0.3486 mL | 1.7432 mL | 3.4864 mL | 8.7160 mL | |
| 10 mM | 0.1743 mL | 0.8716 mL | 1.7432 mL | 4.3580 mL | |
| 15 mM | 0.1162 mL | 0.5811 mL | 1.1621 mL | 2.9053 mL | |
| 20 mM | 0.0872 mL | 0.4358 mL | 0.8716 mL | 2.1790 mL | |
| 25 mM | 0.0697 mL | 0.3486 mL | 0.6973 mL | 1.7432 mL | |
| 30 mM | 0.0581 mL | 0.2905 mL | 0.5811 mL | 1.4527 mL | |
| 40 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0895 mL | |
| 50 mM | 0.0349 mL | 0.1743 mL | 0.3486 mL | 0.8716 mL | |
| 60 mM | 0.0291 mL | 0.1453 mL | 0.2905 mL | 0.7263 mL | |
| 80 mM | 0.0218 mL | 0.1089 mL | 0.2179 mL | 0.5447 mL | |
| 100 mM | 0.0174 mL | 0.0872 mL | 0.1743 mL | 0.4358 mL |
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