Tetrac

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.

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.

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.

——

Apoptosis

Apoptosis

Apoptosis | EGFR

——

——

67-30-1

747.83

C14H8I4O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (133.72 mM; 超声助溶 )

OC(=O)Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1

——

(-20℃)

With Ice Pack

≥ 2 years