1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. Carboxyamidotriazole Orotate

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

Cat. No.: HY-16125
Handling Instructions

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.

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Carboxyamidotriazole Orotate Chemical Structure

Carboxyamidotriazole Orotate Chemical Structure

CAS No. : 187739-60-2

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Description

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].

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].

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.
In Vivo

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

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.
Molecular Weight

580.76

Formula

C₂₂H₁₆Cl₃N₇O₆

CAS No.

187739-60-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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 --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

CarboxyamidotriazoleL-651582CAIL651582L 651582Calcium ChannelCa2+ channelsCa channelsovariancancertoxicitychronicmyelogenousleukaemiaBcr/AblInhibitorinhibitorinhibit

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Carboxyamidotriazole Orotate
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