IMB5046 is a microtubule inhibitor that has antitumor activity, overcoming multidrug-resistance. IMB5046 was cytotoxic with an IC50 range of 37 to 426 nM against multiple tumor cell lines, including some that were resistant to colchicine, vincristine and paclitaxel. IMB5046 was also active against human lung tumor xenografts. IMB5046 was found to bind to tubulin at the colchicine site, but with a different binding mode. IMB5046 inhibited tubulin polymerization, and induced G2/M arrest.
| Molecular Weight | 388.44 |
| Formula | C19H20N2O5S |
| CAS Number | 1001571-08-9 |
| Solubility (25°C) | DMSO: 20 mg/mL |
| 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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