AI-10-49
AI-10-49 is an inhibitor of the oncoprotein CBFβ-SMMHC targeting leukemia. It can effectively block the binding of CBFβ-SMMHC to the RUNX1 Runt domain, with a half-inhibitory concentration (IC50) of 0.26 μM, demonstrating high activity. The CBFβ-SMMHC fusion protein plays a pathogenic role in certain types of leukemia, such as acute myeloid leukemia. AI-10-49 is expected to inhibit the proliferation and survival of leukemia cells by interfering with its interaction with RUNX1.
| Storage | Store at -20°C |
| M.Wt | 660.52 |
| Cas No. | 1256094-72-0 |
| Formula | C30H22F6N6O5 |
| Solubility | ≥16.53mg/mL in DMSO |
| Chemical Name | 2,2'-(5,5'-((oxybis(ethane-2,1-diyl))bis(oxy))bis(pyridine-5,2-diyl))bis(5-(trifluoromethoxy)-1H-benzo[d]imidazole) |
| SDF | Download SDF |
| Canonical SMILES | FC(F)(F)OC1=CC2=C(C=C1)NC(C(C=C3)=NC=C3OCCOCCOC(C=C4)=CN=C4C5=NC6=CC(OC(F)(F)F)=CC=C6N5)=N2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
ME-1 (human leukemia cell lines) |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
6 h |
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Applications |
After 6 hours of treatment, AI-10-49 effectively dissociates RUNX1 from CBFb-SMMHC with 90% dissociation, by contrast, it has a mild effect on CBFb-RUNX1 association. The ChIP assays indicates that AI-10-49 treatment on ME-1 cells for 6 hours increases RUNX1 occupancy 8-, 2.2-, and 8-fold at the RUNX3, CSF1R, and CEBPA promoters. |
| Animal experiment [1]: | |
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Animal models |
Transplanted mice with Cbfb+/MYH11:Ras+/G12D leukemic cells |
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Dosage form |
200 mg/kg; 10 days |
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Applications |
Mice treated with AI-10-49 survives markedly longer (median latency = 61 days) and transient AI-10-49 treatment also reduces leukemia spreading in vivo. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Illendula A, Pulikkan JA, Zong H et.al A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice. Science. 2015 Feb 13;347(6223):779-84. | |
Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
