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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.

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CAS No.: 1990479-17-8
Formule: C₂₃H₃₃F₂N₅O₃S₂
Masse moléculaire:529.67

Stockage:

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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Activité biologique
- Description
- Cellular Effect
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

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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
Masse moléculaire 529.67
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

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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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Activité biologique
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Chemical Information
Pureté et documentation
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CRK12-IN-2

Voir tous les produits spécifiques à Isoform Parasite

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

CRK12-IN-2 Related Classifications

HY-143322 Related Classifications