Carboxyamidotriazole Orotate(Synonyms: L-651582 Orotate; CAI Orotate)

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Carboxyamidotriazole Orotate (Synonyms: L-651582 Orotate; CAI Orotate) 纯度: 99.89%

Carboxyamidotriazole Orotate (L-651582 Orotate)，是一种口服生物有效的信号转导抑制剂Carboxyamidotriazole (CAI) 的 orotate 盐形式。Carboxyamidotriazole Orotate 是一种非电压性钙通道 (nonvoltage-operated calcium channels) 和钙通道介导的信号通路 (calcium channel-mediated signaling pathways) 的细胞抑制剂，具有抗癌，抗炎活性和抗血管生成作用。

Carboxyamidotriazole Orotate(Synonyms: L-651582 Orotate; CAI Orotate)

Carboxyamidotriazole Orotate Chemical Structure

CAS No. : 187739-60-2

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生物活性

Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects[1][2].

体外研究
(In Vitro)

Carboxyamidotriazole Orotate (0.1-10 µM; 24-96 hours) inhibits cell proliferation of LAMA84R and K562R cell lines[1].
Carboxyamidotriazole Orotate inhibits the phosphorylation of a selected target of Bcr-Abl kinase. Tyrosine phosphorylation of CrkL is reduced by 5 µM Carboxyamidotriazole Orotate treatment[1].

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 Viability Assay[1]

Cell Line: LAMA84R and K562R cell lines
Concentration: 0.1, 1, 5, 10 µM
Incubation Time: 24, 48, 72, 96 hours
Result: Showed a 50% growth reduction of the chronic myelogenous leukaemia (CML) lines with 5 µM CTO at 96 h time point.

Western Blot Analysis[1]

Cell Line: LAMA84R and K562R cell lines
Concentration: 0.1, 1, 5 µM
Incubation Time: 72 and 96 hours
Result: A dose-dependent inhibition of both total and phosphorylated Bcr-Abl levels.

体内研究
(In Vivo)

Carboxyamidotriazole Orotate (342, 513 mg/kg; i.p.; Q1D×5 for two rounds) displays antitumor activity on CML xenografts[1].

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: Male NOD/SCID mice four-to-five week old[1]
Dosage: 342, 513 mg/kg
Administration: i.p.; Q1D×5 for two rounds
Result: Increase survival.

Clinical Trial

分子量

580.76

Formula

C22H16Cl3N7O6
CAS 号

187739-60-2
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (8.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7219 mL 8.6094 mL 17.2188 mL
5 mM 0.3444 mL 1.7219 mL 3.4438 mL
10 mM — — —

*

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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Corrado C, et al. Carboxyamidotriazole-orotate inhibits the growth of imatinib-resistant chronic myeloid leukaemia cells and modulates exosomes-stimulated angiogenesis. PLoS One. 2012;7(8):e42310.

    [2]. Hussain MM, et al. Phase II trial of carboxyamidotriazole in patients with relapsed epithelial ovarian cancer. J Clin Oncol. 2003 Dec 1;21(23):4356-63.

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