Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Fadrozole (CGS 16949A) is a highly potent and selective nonsteroidal aromatase inhibitor (IC50 of 6.4 nM) with potential antineoplastic activity. Aromatase, a member of the cytochrome P-450 superfamily, is found in many tissues; overexpression has been linked to the development of preneoplastic and neoplastic changes in breast tissue. Check for active clinical trials or closed clinical trials using this agent. Fadrozole specifically inhibits aromatase, blocking the aromatization of androstenedione and testosterone into estrone and estradiol, respectively, the final step in estrogen biosynthesis; the reduction in estrogen levels may inhibit growth in estrogen-dependent cancers.
ln Vitro |
With an IC50 of 6.4 nM, fadrozole hydroHClide is a very effective and specific nonsteroidal aromatase inhibitor. With an IC50 of 0.03 μM, fadrozole hydrochloride suppresses the synthesis of estrogen in hamster ovarian slices. The IC50 value for the inhibition of progesterone production is 120 μM. To different degrees, the manufacture of additional cytochrome P-450-dependent hormones can be inhibited by high doses of fadrozole hydrochloride [1].
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ln Vivo |
Orally given benzodiazepine hydrochloride has an ED50 of 0.03 mg/kg and can suppress aromatase-mediated uterine hypertrophy in immature female rats. Oral aminoglutethimide dosing produced the same result in the same model, with an ED50 of 30 mg/kg [1]. In female Sprague-Dawley rats, fadrozole hydrochloride inhibits the growth of spontaneous mammary tumors, both benign and malignant. Additionally, it lowers the incidence of spontaneous hepatocellular tumors in both male and female rats and inhibits the spontaneous formation of distal pituitary adenomas in female rats [2]. The parasite burden in male and female mice treated with fadrozole hydrochloride was reduced by 70%. In male mice, this protection was linked to the recovery of particular cellular immune responses. Interleukin-6 (IL-6) expression in the testes of infected male mice increased tenfold, while serum levels and splenocyte synthesis of the substance increased by 80%. These levels recover to baseline amounts following treatment with fadrozole hydrochloride [3].
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References |
[1]. Browne LJ, et al. Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J Med Chem. 1991 Feb;34(2):725-36.
[2]. Gunson DE, et al. Prevention of spontaneous tumours in female rats by fadrozole hydrochloride, an aromatase inhibitor. Br J Cancer. 1995 Jul;72(1):72-5. [3]. Morales-Montor J, et al. Inhibition of p-450 aromatase prevents feminisation and induces protection during cysticercosis. Int J Parasitol. 2002 Oct;32(11):1379-87 |
Molecular Formula |
C14H14CLN3
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Molecular Weight |
259.73406
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CAS # |
102676-31-3
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Related CAS # |
Fadrozole;102676-47-1;Dexfadrostat;102676-87-9;Fadrozole hydrochloride hemihydrate;176702-70-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
N#CC1=CC=C(C2CCCC3=CN=CN23)C=C1.[H]Cl
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InChi Key |
UKCVAQGKEOJTSR-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H13N3.ClH/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14/h4-7,9-10,14H,1-3H21H
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Chemical Name |
Benzonitrile, 4-(5,6,7,8-tetrahydroimidazo(1,5-a)pyridin-5-yl)-, monohydrochloride
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Synonyms |
Fadrozole hydrochloride CGS 16949A CGS-16949A CGS16949A
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O : ~100 mg/mL (~385.02 mM)
DMSO : ~100 mg/mL (~385.02 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.01 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 20.8 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: ≥ 2.08 mg/mL (8.01 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 20.8 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: ≥ 2.08 mg/mL (8.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (385.02 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.8502 mL | 19.2508 mL | 38.5015 mL | |
5 mM | 0.7700 mL | 3.8502 mL | 7.7003 mL | |
10 mM | 0.3850 mL | 1.9251 mL | 3.8502 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.