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Chemical Structure| 187739-60-2 Chemical Structure| 187739-60-2

Structure of Carboxyamidotriazole Orotate
CAS No.: 187739-60-2

Chemical Structure| 187739-60-2

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Carboxyamidotriazole Orotate is a nonvoltage-operated calcium channel and calcium channel-mediated signaling pathway signaling pathways inhibitors with anticancer, anti-inflammatory, and antiangiogenic effects.

Synonyms: L-651582 Orotate; CAI Orotate

4.5 *For Research Use Only !

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Product Details of Carboxyamidotriazole Orotate

CAS No. :187739-60-2
Formula : C22H16Cl3N7O6
M.W : 580.76
SMILES Code : 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
Synonyms :
L-651582 Orotate; CAI Orotate
MDL No. :MFCD22572756

Safety of Carboxyamidotriazole Orotate

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P264-P270-P301+P310+P330-P405-P501
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Description
Carboxyamidotriazole Orotate, the orotate salt of Carboxyamidotriazole (CAI), is recognized for its ability to inhibit signal transduction. It acts as a cytostatic blocker of nonvoltage-operated calcium channels and pathways dependent on these channels, showcasing antitumor, anti-inflammatory, and antiangiogenic properties[1].[2].
Target
  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
rat aortic rings 12 μg/mL 4 days as a positive control to evaluate anti-angiogenic properties Mol Cancer Ther. 2015 Oct;14(10):2228-37
CD8+T cells 10 μM 48 h To evaluate the effect of CAI on IFN-γ production in CD8+T cells, results showed that CAI significantly increased IFN-γ production. J Immunother Cancer. 2019 Sep 11;7(1):246
B16 melanoma cells 10 μM 24 h To evaluate the effect of CAI on the tumor-killing capability of CTLs, results showed that CAI enhanced the cytotoxic activity of CTLs. J Immunother Cancer. 2019 Sep 11;7(1):246
C26 cells 10 μM 48 h Measure intracellular ROS levels, results showed that CAI significantly increased ROS accumulation. Acta Pharm Sin B. 2022 Feb;12(2):759-773
HCT116 cells 10 μM 48 h Evaluate the effect of CAI on glucose uptake, results showed that CAI decreased 2-NBDG uptake. Acta Pharm Sin B. 2022 Feb;12(2):759-773

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/Ltj mice Sjögren's disease-like model Oral gavage 20 and 40 mg/kg Once daily for 16 weeks CAI augmented salivary secretion, decreased water intake and serum autoantibody levels, suppressed histological alterations and lymphocyte foci, and diminished inflammatory factors such as IL-1β and IL-6. It also blocked IκBα degradation and p65 nuclear translocation. Int J Med Sci. 2025 Apr 28;22(10):2362-2372
Lewis rats Adjuvant arthritis (AA) model Oral 10, 20, 40 mg/kg Once daily from day 12 to day 26 To evaluate the effects of CAI on arthritis index, body weight, joint destruction, and inflammatory cytokine levels in AA rats. CAI significantly decreased the arthritis index, improved body weight loss, reduced joint destruction, and lowered the levels of inflammatory cytokines (IL-1β, IL-6, IL-18, and TNF-α). Br J Pharmacol. 2015 Jul;172(13):3446-59
C57BL/6 mice B16 melanoma model Intragastric injection 20 mg/kg Once daily for 23 days To evaluate the effect of CAI on tumor growth, results showed that CAI significantly delayed tumor growth and prolonged the survival of tumor-bearing mice. J Immunother Cancer. 2019 Sep 11;7(1):246
BALB/c mice and nude mice Colorectal cancer xenograft model Intragastric injection 20 mg/kg Once daily for 28 days Evaluate the antitumor effect of CAI alone or in combination with GLS or GDH1 inhibitors, results showed that combination therapy significantly inhibited tumor growth and prolonged mouse survival. Acta Pharm Sin B. 2022 Feb;12(2):759-773

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.61mL

1.72mL

0.86mL

17.22mL

3.44mL

1.72mL

References

 

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