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Cat. No.: HY-143322

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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.

CAS No.: 1990479-17-8
Formula: C₂₃H₃₃F₂N₅O₃S₂
Molecular Weight:529.67

Storage:

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

Data Sheet (272 KB)

CRK12-IN-2 Chemical Structure

CAS No.: 1990479-17-8

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Biological Activity
- Description
- Cellular Effect
- In Vivo
Chemical Information
Purity & Documentation
References
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Classifications
Bioz

Biological Activity

Description

All Parasite Isoforms :

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
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.

Chemical Information

CAS No. 1990479-17-8
Molecular Weight 529.67
Formula C₂₃H₃₃F₂N₅O₃S₂
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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CRK12-IN-2

All Parasite Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

CRK12-IN-2 Related Classifications

HY-143322 Related Classifications