| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Androgen receptor antagonist 1 (compound 26) had notable cytostatic effects on LNCaP and LNAR cells, while having no effect on DU145 cells [1].
|
|---|---|
| ln Vivo |
In an animal model of castration-resistant prostate cancer (CRPC), androgen receptor antagonist 1 (Compound 26; 100 mg/kg once daily for 5 weeks) showed good in vivo tumor growth reduction following oral administration [ 1].
|
| Cell Assay |
Cell proliferation assay[1]
Cell Types: Prostate cancer (CaP) cells (LNCAP, LNAR and DU145) Tested Concentrations: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM Incubation Duration: 7 days Experimental Results: Anti-proliferation Effects on LNCAP and LNAR cells. |
| Animal Protocol |
Animal/Disease Models: Male athymic nude mouse LNCaP CRPC xenograft model [1]
Doses: 100 mg/kg Route of Administration: Orally administered one time/day for 5 weeks. Experimental Results: It has a significant effect in inhibiting tumor growth. At the given dose (100 mg/kg one time/day), tumor growth (90% inhibition) and PSA levels (78%) were almost completely inhibited after 5 weeks, and no weight loss was detected in the animals during treatment. |
| References |
|
| Molecular Formula |
C21H25CLN4O3
|
|---|---|
| Molecular Weight |
416.901203870773
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| Exact Mass |
416.161
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| CAS # |
1338812-36-4
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| PubChem CID |
56643472
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| Appearance |
White to off-white solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
646
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C#N)C=CC(=C1)OC1C(C)(C)C(C1(C)C)NC(C1C=NN(CCO)C=1)=O
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| InChi Key |
HJJNHDLYWZTKGQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25ClN4O3/c1-20(2)18(25-17(28)14-11-24-26(12-14)7-8-27)21(3,4)19(20)29-15-6-5-13(10-23)16(22)9-15/h5-6,9,11-12,18-19,27H,7-8H2,1-4H3,(H,25,28)
|
| Chemical Name |
N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-1-(2-hydroxyethyl)pyrazole-4-carboxamide
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| Synonyms |
Androgen receptor antagonist 1; Androgen receptor antagonist 1
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| 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 (~239.87 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3987 mL | 11.9933 mL | 23.9866 mL | |
| 5 mM | 0.4797 mL | 2.3987 mL | 4.7973 mL | |
| 10 mM | 0.2399 mL | 1.1993 mL | 2.3987 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.
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