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。
生物活性 | Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is athyrointegrin receptorantagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone onintegrinαvβ3. 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 differentK-RASstatus[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 ofCCND1andc-Myc, but promotes expression ofCASP2andTHBS1[3].
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. |
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体内研究 (In Vivo) | Tetrac (35 μg; p.o. for 40 days) inhibits tumor inoculation, growth and integrin expression in mice[4].
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. |
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结构分类 | - Ketones, Aldehydes, Acids
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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 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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本网站选购。
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