67-30-1 2-(4-(4-羟基-3,5-二碘苯氧基)-3,5-二碘苯基)乙酸

危险性质：非危险化学品

• 生物活性 Tetrac (Tetraiodothyroacetic acid)，L-甲状腺素 (T4) 的天然衍生物，是甲状腺素整合素受体拮抗剂。Tetrac 阻断 T4 和 3,5,3'-triiodo-L-thyronine (T3) 在整联蛋白 αvβ3 上甲状腺激素的细胞表面受体处的作用。Tetra 具有抗血管生成和抗肿瘤活性。
• 体外研究 Tetrac (0.01-1 μM; 2-6 d) induces anti-proliferation in HT-29 and HCT116 cells with different K-RAS status. Tetrac (0.1 μM; 30 min) inhibits activation of ERK1/2 in HT-29 and HCT116 cells. Tetrac (0.1 μM; 24 h) inhibits expression of CCND1 and c-Myc , but promotes expression of CASP2 and THBS1 . Cell Proliferation Assay Cell Line: HT-29 and HCT116 cells Concentration: 0.01, 0.1, 1 μM Incubation Time: 0, 2, 4, 6 days Result: Induced anti-proliferation of K-RAS wild-type colorectal cancer cells. Western Blot Analysis Cell Line: HT-29 and HCT116 cells Concentration: 0.1 μM Incubation Time: 30 min Result: Inhibited constitutively activated ERK1/2, and this inhibition can remove by anti-integrin αvβ3 antibody pretreatment.
• 体内研究 Tetrac (35 μg; p.o. for 40 days) inhibits tumor inoculation, growth and integrin expression in mice. Animal Model: Wild-type male Balb/C mice aged 8 weeks are inoculated with 102B16F10 or B16LS9 cells Dosage: 35 μg per day Administration: P.o. (added to the drinking water) daily for 40 days Result: Delayed the onset of ocular melanoma. Reduced the S-100 and integrin staining level in the B16F10 mice model.

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