1. Anti-infection
  2. Parasite
  3. 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.

For research use only. We do not sell to patients.

CRK12-IN-2 Chemical Structure

CRK12-IN-2 Chemical Structure

CAS No. : 1990479-17-8

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Description

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].

Cellular Effect
Cell Line Type Value Description References
L6 EC50
3600 nM
Compound: 2
Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 69 hrs by resazurin dye based fluorescence analysis
Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 69 hrs by resazurin dye based fluorescence analysis
[PMID: 35303411]
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

529.67

Formula

C23H33F2N5O3S2

CAS No.
SMILES

CC(CS(=O)(N[C@H]1CC[C@@H](CC1)NC2=NC(N)=C(S2)C(C3=C(C=C(C=C3F)CN(C)C)F)=O)=O)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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CRK12-IN-2 Related Classifications

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CRK12-IN-2
Cat. No.:
HY-143322
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