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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500mg |
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2g |
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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 |
The rat ovary and human placenta both exhibit strong aromatase inhibition when exposed to fadrozole hydrochloride. With an IC50 of 0.03 μM, fadrozole salty suppresses the synthesis of estrogen in hamster ovarian slices. The IC50 value for the inhibition of progesterone production is 120 μM. To varied 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 |
In immature female rats, fadrozole administered orally suppresses the uterine hypertrophy generated by androstenedione-mediated aromatase, with an ED50 of 0.03 mg/kg. Aminoglutethimide administered orally in the same mouse produced the same result, with an ED50 of 30 mg/kg [1]. In female Sprague-Dawley rats, fadrozole hydrochloride inhibits the growth of spontaneous mammary tumors, both malignant and benign. Additionally, it can lessen the frequency of spontaneous hepatic tumors in both male and female rats as well as slow down the spontaneous development of pituitary dtamas in female rats [2]. Fadrozole was given to male and female mice, and it reduced the parasite burden by 70% while inhibiting the generation of 17b-estradiol. In male mice, this defense was linked to the recovery of particular cellular immunological responses. Interleukin-6 (IL-6) production in the spleenocytes and serum levels rose by 80%, while the expression of interleukin-6 (IL-6) in the testes of male infected mice increased tenfold. Fadrozole therapy brings these levels back to initial levels [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 |
C14H13N3
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Molecular Weight |
223.27312
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CAS # |
102676-47-1
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Related CAS # |
Fadrozole hydrochloride;102676-31-3;Dexfadrostat;102676-87-9;Fadrozole hydrochloride hemihydrate;176702-70-8
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SMILES |
N#CC1=CC=C(C2CCCC3=CN=CN23)C=C1
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InChi Key |
CLPFFLWZZBQMAO-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H13N3/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,1-3H2
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Chemical Name |
4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile
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Synonyms |
Fadrozole CGS 16949A CGS-16949A CGS16949A Fadrozole free base
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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)
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Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~447.89 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (9.72 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 21.7 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: ≥ 2.17 mg/mL (9.72 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 21.7 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: ≥ 2.17 mg/mL (9.72 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 | 4.4789 mL | 22.3944 mL | 44.7888 mL | |
5 mM | 0.8958 mL | 4.4789 mL | 8.9578 mL | |
10 mM | 0.4479 mL | 2.2394 mL | 4.4789 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.