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编 号:F753829
分子式:C31H34F3N3O5
分子量:585.61
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生物活性:
TCMDC-135051 TFA is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 TFA prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 TFA has antiparasiticidal activity (EC50=320 nM).

体外研究:
TCMDC-135051 TFA shows potent activity against P. berghei sporozoites in a liver invasion and development assay 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 TFA 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.
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