Uses
AI-10-49 is an inhibitor of leukemic oncoprotein CBFβ-SMHHC. AI-10-49 inhibits the binding of CBFβ-SMMHCto the RUNX1 Runt domain with IC50 value of 0.26 μM. AI-10-49 can be used for the research of leukemia[1].
in vivo
AI-10-49 (200 mg/kg; per day) delays leukemia progression in mice[1].
| Animal Model: | Mice (Cbfb+/MYH11:Ras+/G12D leukemic cells)[1] |
| Dosage: | 200 mg/kg |
| Administration: | per day |
| Result: | Reduced leukemia expansion in vivo and survived significantly long. |
References
[1] Anuradha Illendula, 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. DOI:
10.1126/science.aaa0314
