Carboxyamidotriazole Orotate (Synonyms:L-651582 Orotate; CAI Orotate)
目录号 : KM11579 CAS No. : 187739-60-2 纯度 : 98%

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。

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5mg
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10mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

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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.

体外研究

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.

Cell Viability Assay

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

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

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

Animal Model: Male NOD/SCID mice four-to-five week old
Dosage: 342, 513 mg/kg
Administration: i.p.; Q1D×5 for two rounds
Result: Increase survival.
分子式
C22H18Cl3N7O6
分子量
580.76
CAS号
187739-60-2
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。-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。

临床试验
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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