CRK12-IN-2

Cat. No.: HY-143322: FAQs
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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

CAS No. : 1990479-17-8

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Description

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
C_lb (mL/min/kg)	15±5
V_dss (L/kg)	2.3±0.6
half-life (h)	4±2
AUC_0-∞(ng·min/mL)	140000±40000	500000±30000
C_max (ng/mL)		1700±800
T_max (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.

1990479-17-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

CRK12-IN-2 Related Classifications

Infection

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CRK12-IN-21990479-17-8ParasitetrypanosomiasisTrypanosoma congolenseTrypanosoma vivaxcattlemiceInhibitorinhibitorinhibit

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