1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. TTT-28

TTT-28 

Cat. No.: HY-101511
Handling Instructions

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.

TTT-28 Chemical Structure

TTT-28 Chemical Structure

CAS No. : 1609138-51-3

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Description

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[1].

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].

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].

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.
Molecular Weight

573.66

Formula

C₃₁H₃₁N₃O₆S

CAS No.

1609138-51-3

SMILES

O=C(N[[email protected]@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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Please store the product under the recommended conditions in the Certificate of Analysis.

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