| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
TTT-28 (0-100 μM; 72 hours) reverses ABCB1-mediated MDR in drug-selected SW620/Ad300 cells and transfected HEK293/ABCB1 cells; TTT-28 in CCD-18Co, SW620, and SW620/Ad300 cells The IC50 values in 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) promotes ABCB1-mediated MDR and increases [3H]-paclitaxel accumulation in ABCB1-overexpressing cells [1]. TTT-28 (10 μM; 0-72 hours) does not interfere with the expression level and localization of ABCB1 and is created by blocking the efflux function of ABCB1 [1]. TTT-28 (0-40 μM; 2 hours) binds at the drug-substrate binding site and increases the ATPase activity of ABCB1 in a concentration-dependent manner [1].
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| ln Vivo |
Because TTT-28 (oral; 30 mg/kg; every 3 days; 18 days) inhibits the efflux function of ABCB1, it increases the anticancer activity of paclitaxel by inhibiting the growth of SW620/Ad300 tumors and promoting apoptosis[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SW620 cells, SW620/Ad300 cells Tested Concentrations: 0.1 μM, 1 μM, 10 μM, 100 μM Incubation Duration: 72 hrs (hours) Experimental Results: ABCB1 substrate (paclitaxel, doxorubicin, vincristine) The fold resistance of SW620/Ad300 cells was diminished compared with SW620 cells. |
| Animal Protocol |
Animal/Disease Models: 5-10 weeks old male athymic NCR (nu/nu) nude mice ABCB1 overexpression SW620/Ad300 cell tumor xenograft model
Doses: 30mg/kg Route of Administration: oral; Route of Administration: oral. Once every three days; 18-day Experimental Results: Causes increased intratumoral accumulation of paclitaxel in the tumor. |
| References |
| Molecular Formula |
C31H31N3O6S
|
|---|---|
| Molecular Weight |
573.659346818924
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| Exact Mass |
573.193
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| CAS # |
1609138-51-3
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| PubChem CID |
86765226
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| Appearance |
White to off-white solid powder
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| LogP |
6.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
41
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| Complexity |
870
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S1C=C(C(NC2=CC=CC=C2C(C2C=CC=CC=2)=O)=O)N=C1[C@H](C(C)C)NC(C1C=C(C(=C(C=1)OC)OC)OC)=O
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| InChi Key |
VUSXKXGCZNKQFS-SANMLTNESA-N
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| InChi Code |
InChI=1S/C31H31N3O6S/c1-18(2)26(34-29(36)20-15-24(38-3)28(40-5)25(16-20)39-4)31-33-23(17-41-31)30(37)32-22-14-10-9-13-21(22)27(35)19-11-7-6-8-12-19/h6-18,26H,1-5H3,(H,32,37)(H,34,36)/t26-/m0/s1
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| Chemical Name |
N-(2-benzoylphenyl)-2-[(1S)-2-methyl-1-[(3,4,5-trimethoxybenzoyl)amino]propyl]-1,3-thiazole-4-carboxamide
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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 : ~250 mg/mL (~435.80 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 | 1.7432 mL | 8.7160 mL | 17.4319 mL | |
| 5 mM | 0.3486 mL | 1.7432 mL | 3.4864 mL | |
| 10 mM | 0.1743 mL | 0.8716 mL | 1.7432 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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