TCMDC-135051

CAS No. 2413716-15-9

TCMDC-135051( —— )

Catalog No. M33139 CAS No. 2413716-15-9

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 188 In Stock
5MG 186 In Stock
10MG 320 In Stock
25MG 506 In Stock
50MG 644 In Stock
100MG 887 In Stock
200MG Get Quote In Stock
500MG 1795 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    TCMDC-135051
  • Note
    Research use only, not for human use.
  • Brief 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.
  • Description
    TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM).
  • In Vitro
    TCMDC-135051 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 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.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2413716-15-9
  • Formula Weight
    471.59
  • Molecular Formula
    C29H33N3O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (530.12 mM; Ultrasonic )
  • SMILES
    CCN(CC)Cc1ccc(OC)c(c1)-c1cc2c(ccnc2[nH]1)-c1ccc(C(O)=O)c(c1)C(C)C
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Alam MM, et al. Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target. Science. 2019 Aug 30;365(6456). pii: eaau1682.?
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