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Art. -Nr.: HY-101511

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TTT-28

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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.

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Reinheit: 99.87%
CAS. Nr.: 1609138-51-3
Formel: C₃₁H₃₁N₃O₆S
Molecular Weight:573.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TTT-28 Chemical Structure

CAS. Nr.: 1609138-51-3

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	1 μM Compound: 28	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	[PMID: 24773054]

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

SW620 cells, SW620/Ad300 cells
Concentration:

0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:

72 hours
Result:

Decreased the resistance fold of ABCB1 substrates (Paclitaxel, Doxorubicin, Vincristine) in SW620/Ad300 cells compared to SW620 cells.

In Vivo

TTT-28 (deliver orally; 30 mg/kg; every 3 rd day; 18 days) potentiates the anticancer activity of paclitaxel due to its inhibitory effect on the efflux function of ABCB1, it enhances the inhibitory effect of paclitaxel on the growth of SW620/Ad300 tumor and promoted apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells
Dosage:

30 mg/kg
Administration:

Deliver orally; every 3rd day; 18 days
Result:

Lead to higher intratumoral accumulation of paclitaxel in tumors.

Chemical Information

CAS. Nr. 1609138-51-3
Appearance Solid
Molecular Weight 573.66
Formel C₃₁H₃₁N₃O₆S
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang YJ, et al. Thiazole-valine peptidomimetic (TTT-28) antagonizes multidrug resistance in vitro and in vivo by selectively inhibiting the efflux activity of ABCB1. Sci Rep. 2017 Feb 9;7:42106. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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TTT-28

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Lipid Metabolism Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TTT-28

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Lipid Metabolism Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TTT-28 Related Classifications

HY-101511 Related Classifications