Carboxyamidotriazole Orotate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Carboxyamidotriazororotate 是一种非电压驱动的钙通道和钙通道介导的信号通路的细胞抑制抑制剂。

Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.(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.(In Vivo):Carboxyamidotriazole Orotate (342, 513 mg/kg; i.p.; Q1D×5 for two rounds) displays antitumor activity on CML xenografts.

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.

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.

L-651582 Orotate | CAI Orotate

GPCR/G Protein

Calcium Channel

Calcium Channel

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187739-60-2

580.76

C22H16Cl3N7O6

>98% (HPLC)

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

O=C(C(NC1=O)=CC(N1)=O)O.O=C(C2=C(N)N(CC3=CC(Cl)=C(C(C4=CC=C(Cl)C=C4)=O)C(Cl)=C3)N=N2)N

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(-20℃)

With Ice Pack

≥ 2 years