CRK12-IN-2

CRK12-IN-2 (compound 2) is an inhibitor of CRK12. CRK12-IN-2 shows potency against Trypanosoma congolense and Trypanosoma vivax with EC50 values of 3.2 and 0.08 nM. CRK12-IN-2 can be used for the research of animal trypanosomiasis[1].

Research Areas >> Infection

CRK12-IN-2 (10 mg/kg; s.c. once daily for 4 days) effectively cures mice with T. congolense- and T. vivax-infection[1]. 1.19Pharmacokinetic Properties of CRK12-IN-2 in Cattle[1]. Cattle IV 2 mg/kg Cattle IM 10 mg/kg Clb (mL/min/kg) 15±5 Vdss (L/kg) 2.3±0.6 half-life (h) 4±2 AUC0-∞(ng·min/mL) 140000±40000 500000±30000 Cmax (ng/mL) 1700±800 Tmax (h) 1.3±0.6 F (%) 73±6 Animal Model: Mice with T. congolense and T. vivax infection[1] Dosage: 10 mg/kg Administration: Subcutaneous injection; 10 mg/kg once daily; for 4 days Result: Fully cured both T. congolense- and T. vivax-infected mice for 4 days at a dose of 10 mg/kg.

[1]. Smith A, et al. Repositioning of a Diaminothiazole Series Confirmed to Target the Cyclin-Dependent Kinase CRK12 for Use in the Treatment of African Animal Trypanosomiasis. J Med Chem. 2022 Apr 14;65(7):5606-5624.