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Crolibulin is a small molecule tubulin polymerization inhibitor. Microtubulin inhibitor Crolibulin (EPC2407) binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of tubulin into microtubules, which may result in cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. Crolibulin also disrupts tumor neovascularization, which may result in a reduction in tumor blood flow and tumor hypoxia and ischemic necrosis.
| 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.
| Molecular Weight | 417.26 |
| Formula | C18H17BrN4O3 |
| CAS Number | 1000852-17-4 |
| Purity | >98% |
| Solubility | DMSO: ≥ 90 mg/mL (Need warming and ultrasonic) |
| Storage | at -20°C |
[3] Patil SA, et al. Future Med Chem. Chromenes: potential new chemotherapeutic agents for cancer.
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