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CAS No.: 1446712-19-1

Synonyms: SNG-1153

SNG1153, a derivate of icaritin, is a modulator of ER-α36 and an inducer of phosphorylation of β-catenin.

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400-920-2911

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描述Estrogen receptor variant ERα36 is highly deregulated in human cancers. SNG1153 is a synthetic compound derived from icaritin that targets abnormal ERα36 activity, inhibits cell proliferation, and induces apoptosis of BCR-ABL⁺ leukemic cells. SNG-1153 inhibited the proliferation of chronic myeloid leukemia cell line K562 with an IC50 value of 4.9 μM. The addition of SNG-1153 (2.5 μM) in imatinib-resistant K562 (K562IMR) cells significantly increased the frequency of Annexin V⁺ cells after 48 h of exposure to imatinib. The phosphorylation of BCR-ABL on tyrosine residue 177 was reduced to a lesser extent in K562IMR cells by a combination of SNG-1153 plus imatinib compared to the group treated with imatinib alone. SNG-1153 alone at a dose of 5 μM significantly disrupted the BCR-ABL-GRB2 interaction in BCR-ABL-T315I cells. In a human cell engrafted mouse model of leukemia, oral administration with dasatinib (15 mg/kg) plus SNG-1153 (37.5 mg/kg) once a day for two weeks decreased the intensity of bioluminescent signals compared to vehicle- or SNG-1153-treated groups^[3]. SNG-1153 was also shown to inhibit the growth of lung cancer stem cells and induce β-catenin phosphorylation at concentrations of 5 and 10 μM, respectively^[4].
作用机制SNG-1153 is a hydrolytic derivate of icaritin from Epimedium. It targets abnormal ERα36 activity and acts as an anti-tumor agent against human lung cancer^[4].
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