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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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