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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
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].
体内研究
When administered intraperitoneally at doses of 342 and 513 mg/kg on a once-daily schedule for two cycles, Carboxyamidotriazole Orotate exhibits significant antitumor activity in CML xenograft models[1].
体外研究
Carboxyamidotriazole Orotate curbs the proliferation of LAMA84R and K562R cell lines within a concentration range of 0.1-10 µM over 24-96 hours[1].
Carboxyamidotriazole Orotate also impedes the phosphorylation of CrkL, a target of Bcr-Abl kinase, with a significant reduction observed upon treatment with 5 µM of Carboxyamidotriazole Orotate[1].
Carboxyamidotriazole Orotate 细胞实验
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
Carboxyamidotriazole Orotate 动物实验
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.
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