- 英文名称
- 2-(4-(4-Hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl)acetic acid
- 分子式
- C14H8I4O4
- 分子量
- 747.83
- 中文别名
- 3,3',5,5'-四碘甲腺-乙酸（储存“-20℃，避光”；运输“干冰”）; 5-diiodophenoxy)-3; Thyroacetic acid,3,3',5,5'-tetraiodo; 3,5-Diiodo-4-(4-hydroxy-3,5-diiodophenoxy)benzeneacetic acid; Tetrac; MFCD00055932; [4-(4-hydroxy-3; 4-(4-Hydroxy-3,5-diiodophenoxy)-3,5-diiodophenylacetic acid; Benzeneacetic acid,3,5-diiodo-4-(4-hydroxy-3,5-diiodophenoxy); 3,3',5,5'-TETRAIODOTHYROACETIC ACID; Tetraiodothyroacetic acid; Acide 3,5,3',5'-tetraiodothyroacetique [French]; 5-diiodophenyl] acetic acid; EINECS 200-649-1
- 用途
- - 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.
