Tirbanibulin (KX2-391) is a synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase signaling inhibitor with an IC50 of average 72 nM. Tirbanibulin (KX2-391) has potential antineoplastic activity. Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase. In addition, Tirbanibulin (KX2-391) also inhibits microtubule polymerization. Preclinical studies have suggested that KX2-391 is able to prevent the proliferation and metastasis of prostate cancer cell lines in mouse xenografts.
| Molecular Weight | 431.53 |
| Formula | C26H29N3O3 |
| CAS Number | 897016-82-9 |
| Solubility (25°C) | DMSO 50 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.
[1] Anna H Dlott, et al. Tirbanibulin: Topical Treatment for Actinic Keratosis
[2] No authors listed. Am J Health Syst Pharm. Tirbanibulin
[3] Anthony Markham, et al. Tirbanibulin: First Approval
[4] Andrew Blauvelt, et al. Phase 3 Trials of Tirbanibulin Ointment for Actinic Keratosis
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