Carboxyamidotriazole Orotate|187739-60-2|(L-651582 Orotate; CAI Orotate)-陌孚医药/Medlife

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

目录号: PL04589 纯度: ≥99%

CAS No. :187739-60-2

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中文名称	Carboxyamidotriazole Orotate
英文名称	Carboxyamidotriazole Orotate
英文别名	Carboxiamidotriazol orotate;SB17292;5-Amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]triazole-4-carboxamide;2,4-dioxo-1H-pyrimi;Carboxyamidotriazole (Orotate);L-651582 (Orotate);CAI (Orotate);Carboxyamidotriazole Orotate;L-651582 Orotate;CAI Orotate;OCSMDRBVJRAMCI-UHFFFAOYSA-N;CARBOXYAMIDOTRIAZOLE OROTATE
Cas No.	187739-60-2
分子式	C₂₂H₁₆Cl₃N₇O₆
分子量	580.76
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

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.

性状

Solid

体外研究(In Vitro)

Carboxyamidotriazole Orotate (0.1-10 μM; 24-96 hours) inhibits cell proliferation of LAMA84R and K562R cell lines.
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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male NOD/SCID

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 5 mg/mL (8.61 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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