Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
Other Sizes |
|
Purity: =97.97%
Carboxyamidotriazole (RFE-007; L-651582; NSC-609974; CAI) is a novel and potent inhibitor of both cAMP-phosphodiesterases and GMP-phosphodiesterases with anti-tumor and anti-inflammatory activity. Also an inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways.
References | |
---|---|
Additional Infomation |
Carboxyamidotriazole has been used in trials studying the treatment of Lymphoma, Lung Cancer, Breast Cancer, Kidney Cancer, and Ovarian Cancer, among others.
Carboxyamidotriazole is an orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2+ channels, blocking both Ca2+ influx into cells and Ca2+ release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion and metastasis. (NCI04) |
Molecular Formula |
C17H12CL3N5O2
|
---|---|
Molecular Weight |
424.67
|
Exact Mass |
423.006
|
CAS # |
99519-84-3
|
Related CAS # |
Carboxyamidotriazole Orotate;187739-60-2
|
PubChem CID |
108144
|
Appearance |
White to off-white solid powder
|
Density |
1.65g/cm3
|
Boiling Point |
685.5ºC at 760 mmHg
|
Flash Point |
368.3ºC
|
Index of Refraction |
1.73
|
LogP |
4.48
|
Hydrogen Bond Donor Count |
2
|
Hydrogen Bond Acceptor Count |
5
|
Rotatable Bond Count |
5
|
Heavy Atom Count |
27
|
Complexity |
549
|
Defined Atom Stereocenter Count |
0
|
InChi Key |
WNRZHQBJSXRYJK-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C17H12Cl3N5O2/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/h1-6H,7,21H2,(H2,22,27)
|
Chemical Name |
5-amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]triazole-4-carboxamide
|
Synonyms |
RFE007L651582NSC609974RFE-007L-651582NSC-609974NSC 609974 RFE 007 CAI
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~100 mg/mL (~235.48 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3548 mL | 11.7738 mL | 23.5477 mL | |
5 mM | 0.4710 mL | 2.3548 mL | 4.7095 mL | |
10 mM | 0.2355 mL | 1.1774 mL | 2.3548 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.