Anticancer agent 164 

CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer^[1][2].

CML-IN-1 (compound 7) exhibits the least cellular toxicity and better biological activity in cellular assays (K562, IC₅₀: 0.038 μM)^[1].
CML-IN-1 (compound 4) significantly inhibits HCT116 cell proliferation with IC₅₀ values of 8.04 ± 0.94 µM after 48 h and 5.52 ± 0.42 µM after 72 h, respectively^[2].
CML-IN-1 (compound 4) inhibits colony formation, migration, and invasion of HCT116 cells in a dose-dependent manner, as well as inducing cell apoptosis and arresting the cell cycle in the G2/M phase^[2].
CML-IN-1 (compound 4) inhibits the activation of the MEK/ERK signaling in HCT116 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

540.58

C₂₁H₂₃F₃N₈O₂S₂

2235393-30-1

O=C(NC1=CC=C(C(F)(F)F)C=C1)NC2=NN=C(SC3=NC=NC(NCCCN4CCOCC4)=C3)S2

Room temperature in continental US; may vary elsewhere.

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

• [1]. Li W, et al. Design and synthesis of novel 1-phenyl-3-(5-(pyrimidin-4-ylthio)-1,3,4-thiadiazol- 2-yl)urea derivatives with potent anti-CML activity throughout PI3K/AKT signaling pathway. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1831-1835.  [Content Brief]

  [2]. Li W, et al. A novel 4-(1,3,4-thiadiazole-2-ylthio)pyrimidine derivative inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer. Acta Pharm. 2023 Sep 14;73(3):489-502.  [Content Brief]