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  • DC Chemicals Limited
  • China
  • Product Name: AI-10-49
  • Price: $1100.0/250mg $2100.0/1g $600.0/100mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

1256094-72-0

1256094-72-0 structure
1256094-72-0 structure
  • Name: AI-10-49
  • Chemical Name: 2,2'-[Oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[6-(trifluoromethoxy)-1H-benzimidazole]
  • CAS Number: 1256094-72-0
  • Molecular Formula: C30H22F6N6O5
  • Molecular Weight: 660.523
  • Catalog: Research Areas Cancer
  • Create Date: 2018-11-30 15:53:33
  • Modify Date: 2024-01-11 10:43:31
  • AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.IC50 value: 0.26 uM [1]Target: CBFβ-SMMHC/RUNX1 interaction inhibitorAI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics,and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers.

Name 2,2'-[Oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[6-(trifluoromethoxy)-1H-benzimidazole]
Synonyms AI-10-49
1H-Benzimidazole, 2,2'-[oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[5-(trifluoromethoxy)-
2,2'-[Oxybis(2,1-ethanediyloxy-5,2-pyridinediyl)]bis[5-(trifluoromethoxy)-1H-benzimidazole]
Description AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.IC50 value: 0.26 uM [1]Target: CBFβ-SMMHC/RUNX1 interaction inhibitorAI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics,and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers.
Related Catalog
References

[1]. Illendula A, et al. Chemical biology. A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice. Science. 2015 Feb 13;347(6223):779-84.

Density 1.5±0.1 g/cm3
Boiling Point 790.3±70.0 °C at 760 mmHg
Molecular Formula C30H22F6N6O5
Molecular Weight 660.523
Flash Point 431.8±35.7 °C
Exact Mass 660.155579
PSA 129.29000
LogP 7.00
Vapour Pressure 0.0±2.8 mmHg at 25°C
Index of Refraction 1.611
Storage condition -20℃