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.
Product information
CAS Number: 187739-60-2
Molecular Weight: 580.76
Formula: C22H16Cl3N7O6
Synonym:
L-651582 Orotate
CAI Orotate
Chemical Name: 2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid; 5-amino-1-{[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl}-1H-1,2,3-triazole-4-carboxamide
Smiles: NC(=O)C1N=NN(CC2=CC(Cl)=C(C(Cl)=C2)C(=O)C2C=CC(Cl)=CC=2)C=1N.OC(=O)C1=CC(=O)NC(=O)N1
InChiKey: MNWOBDDXRRBONM-UHFFFAOYSA-N
InChi: InChI=1S/C17H12Cl3N5O2.C5H4N2O4/c18-10-3-1-9(2-4-10)15(26)13-11(19)5-8(6-12(13)20)7-25-16(21)14(17(22)27)23-24-25;8-3-1-2(4(9)10)6-5(11)7-3/h1-6H,7,21H2,(H2,22,27);1H,(H,9,10)(H2,6,7,8,11)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 5 mg/mL (8.61 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
References:
- Corrado C, et al. Carboxyamidotriazole-orotate inhibits the growth of imatinib-resistant chronic myeloid leukaemia cells and modulates exosomes-stimulated angiogenesis. PLoS One. 2012;7(8):e42310.
- Hussain MM, et al. Phase II trial of carboxyamidotriazole in patients with relapsed epithelial ovarian cancer. J Clin Oncol. 2003 Dec 1;21(23):4356-63.
Products are for research use only. Not for human use.
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