1609138-51-3

1609138-51-3 structure
1609138-51-3 structure
  • Name: TTT-28
  • Chemical Name: TTT-28
  • CAS Number: 1609138-51-3
  • Molecular Formula: C31H31N3O6S
  • Molecular Weight: 573.66
  • Catalog: Research Areas Cancer
  • Create Date: 2019-08-03 21:21:59
  • Modify Date: 2024-01-13 13:36:36
  • TTT-28 is a synthesized thiazole-valine peptidomimetic, 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].

Name TTT-28
Description TTT-28 is a synthesized thiazole-valine peptidomimetic, 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].
Related Catalog
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.
References

[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.

Molecular Formula C31H31N3O6S
Molecular Weight 573.66
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.