Tetrac(Synonyms: Tetraiodothyroacetic acid; 3,3′,5,5′-Tetraiodothyroacetic acid)

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Tetrac (Synonyms: Tetraiodothyroacetic acid; 3,3′,5,5′-Tetraiodothyroacetic acid) 纯度: ≥95.0%

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(Synonyms: Tetraiodothyroacetic acid; 3,3

Tetrac Chemical Structure

CAS No. : 67-30-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
10 mg ￥500 In-stock
25 mg ￥1000 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

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[1][2].

体外研究
(In Vitro)

Tetrac (0.01-1 μM; 2-6 d) induces anti-proliferation in HT-29 and HCT116 cells with different K-RAS status[3].
Tetrac (0.1 μM; 30 min) inhibits activation of ERK1/2 in HT-29 and HCT116 cells[3].
Tetrac (0.1 μM; 24 h) inhibits expression of CCND1 and c-Myc, but promotes expression of CASP2 and THBS1[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

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[3]

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
(In Vivo)

Tetrac (35 μg; p.o. for 40 days) inhibits tumor inoculation, growth and integrin expression in mice[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wild-type male Balb/C mice aged 8 weeks are inoculated with 102B16F10 or B16LS9 cells[4]
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.

分子量

747.83

Formula

C14H8I4O4
CAS 号

67-30-1
中文名称

四碘甲状腺乙酸
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (133.72 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3372 mL 6.6860 mL 13.3720 mL
5 mM 0.2674 mL 1.3372 mL 2.6744 mL
10 mM 0.1337 mL 0.6686 mL 1.3372 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (3.34 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (3.34 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.34 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Schmohl KA, et, al. Tetrac as an anti-angiogenic agent in cancer. Endocr Relat Cancer. 2019 Jun 1; 26(6):R287-R304.

    [2]. Davis PJ, et, al. Nongenomic Actions of Thyroid Hormone: the Integrin Component. Physiol Rev. 2020 Jun 25.

    [3]. Chin YT, et, al. Tetrac and NDAT Induce Anti-proliferation via Integrin αvβ3 in Colorectal Cancers With Different K-RAS Status. Front Endocrinol (Lausanne). 2019 Mar 12; 10:130.

    [4]. Ashur-Fabian O, et, al. Tetrac Delayed the Onset of Ocular Melanoma in an Orthotopic Mouse Model. Front Endocrinol (Lausanne). 2019 Jan 8; 9:775.

    [5]. Rajabi M, et, al. Synthesis of new analogs of tetraiodothyroacetic acid (tetrac) as novel angiogenesis inhibitors for treatment of cancer. Bioorg Med Chem Lett. 2018 Apr 15;28(7):1223-1227.

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