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AI-10-49 effectively dissociated RUNX1 from CBFβ-SMMHC. AI-10-49 has enhanced inhibitory activity on ME-1 cell growth (IC50 = 0.6 mM). AI-10-49 showed negligible activity (IC50 > 25 μM) in normal human bone marrow cells. In a panel of 11 human leukemia cell lines, ME-1 cells were the only cell line highly sensitive to AI-10-49.
In vivo: vehicle-treatedmice succumbed to leukemia with a median latency of 33.5 days, whereas AI-10-49-treated mice survived significantly longer (median latency = 61 days; P = 2.7 × 10-6).
In mice transplanted with Cbfb+/MYH11;Nras+/G12D leukemic cells, AI-10-49 (200 mg/kg, i.p.) reduces leukemia expansion.
| Molecular Weight | 660.52 |
| Formula | C30H22F6N6O5 |
| CAS Number | 1256094-72-0 |
| Solubility (25°C) | DMSO 100 mg/mL Ethanol 100 mg/mL warmed |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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