WDR5-IN-5 (compound 41) (10 mg/kg; p.o.) shows high oral exposure (AUC0,inf=3984 h.ng/mL), long half-life of T1/2=1.3 h[1].
WDR5-IN-5 (3 mg/kg; i.v.) also shows low iv clearance (26 mL/min/kg). WDR5-IN-5 is well tolerated and shows no adverse effects in mice by both i.v. and p.o. dosing[1].
WDR5-IN-5 can be formulated as 0.6 and 1 mg/mL solutions in ethanol, tocopherol poly (ethylene glycol) succinate (TPGS), PEG400 and water (v/v/v/v, 5/5/30/60) for i.v. and p.o. dosing, respectively[1].
PK profile of WDR5-IN-5 in CD-1 Mice[1]
| Route | Dose (mg/kg) | CL (mL/min/kg) | AUC0,inf (h.ng/mL) | Vss (L/kg) | T1/2 (h) | F (%) |
| i.v. | 3 | 26 | 1951 | 1.6 | / | / |
| p.o. | 10 | 2083 | 3984 | / | 1.3 | 61 |
| Animal Model: | Male CD-1 mice[1] |
| Dosage: | 3 mg/kg i.v.; 10 mg/kg p.o. |
| Administration: | Intravenous injection or oral gavage |
| Result: | Showed high oral exposure (AUC0,inf=3984 h.ng/mL), long half-life of T1/2=1.3 h, and low iv clearance (26 mL/min/kg). |
