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TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $79 | In Stock | In Stock | |
| 5 mg | $196 | In Stock | In Stock | |
| 10 mg | $337 | In Stock | In Stock | |
| 25 mg | $533 | In Stock | In Stock | |
| 50 mg | $693 | In Stock | In Stock | |
| 100 mg | $954 | In Stock | In Stock | |
| 500 mg | $1,930 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $198 | In Stock | In Stock |
| Description | TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector. |
| In vitro | In a liver invasion and development assay, TCMDC-135051 shows potent activity against P. berghei sporozoites in which the compound shows a pEC50 value of 6.17 (EC50=0.40 μM). The kinase assays using recombinant PvCLK3 (P. vivax) and PbCLK3 (P. berghei) show that TCMDC-135051 has near-equipotent inhibition at these two orthologs, with pIC50 values of 7.47 (IC50=0.033 μM) and 7.86 (IC50=0.013 μM), respectively[1]. |
| Molecular Weight | 471.59 |
| Formula | C29H33N3O3 |
| Cas No. | 2413716-15-9 |
| Smiles | CCN(CC)Cc1ccc(OC)c(c1)-c1cc2c(ccnc2[nH]1)-c1ccc(C(O)=O)c(c1)C(C)C |
| Relative Density. | 1.173 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 225 mg/mL (477.11 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.6 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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