| Identification | Back Directory | [Name]
1-Propanesulfonamide, N-[trans-4-[[4-amino-5-[4-[(dimethylamino)methyl]-2,6-difluorobenzoyl]-2-thiazolyl]amino]cyclohexyl]-2-methyl- | [CAS]
1990479-17-8 | [Synonyms]
CRK12-IN-2
1-Propanesulfonamide, N-[trans-4-[[4-amino-5-[4-[(dimethylamino)methyl]-2,6-difluorobenzoyl]-2-thiazolyl]amino]cyclohexyl]-2-methyl- | [Molecular Formula]
C23H33F2N5O3S2 | [MOL File]
1990479-17-8.mol | [Molecular Weight]
529.67 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
CRK12-IN-2 (10 mg/kg; s.c. once daily for 4 days) effectively cures mice with T. congolense- and T. vivax-infection[1].
1.19 Pharmacokinetic 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. |
| [References]
[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. DOI:10.1021/acs.jmedchem.1c02104 |
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