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 Purity: 98.98%
COA 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.

For research use only. We do not sell to patients.

Carboxyamidotriazole Orotate Chemical Structure

Carboxyamidotriazole Orotate Chemical Structure

CAS No. : 187739-60-2

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Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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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].

MedChemExpress (MCE) 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.
In Vivo

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

MedChemExpress (MCE) 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
Molecular Weight

580.76

Formula

C22H16Cl3N7O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

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

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (8.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.32%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7219 mL 8.6094 mL 17.2188 mL 43.0470 mL
5 mM 0.3444 mL 1.7219 mL 3.4438 mL 8.6094 mL
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Carboxyamidotriazole Orotate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Carboxyamidotriazole Orotate
Cat. No.:
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