| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
In LNCaP, C4-2, MR49F, and 22Rv1 cells, VPC-14449 (0.01-100 μM; 24 hours) suppresses AR transcriptional activity and cell viability [2]. Without altering the expression of AR protein, VPC-14449 (0.01-100 μM; 24 h) dose-modeled suppression of transiently produced full-length human AR in PC3 cells (IC50=0.34 μM) [1].
|
|---|---|
| ln Vivo |
VPC-14449 (100 mg/kg; intraperitoneally injected twice daily for 4 weeks) decreased tumor volume and stopped PSA production in the LNCaP xenograft model [1]. The animals were weighed at the end of the 4 week treatment.
|
| Cell Assay |
Cell Viability Assay [2]
Cell Types: LNCaP, C4-2, MR49F and 22Rv1 Cell Tested Concentrations: 0.01, 0.1, 10, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of growth of each cell line tested. Western Blot Analysis[2] Cell Types: LNCaP, C4-2, MR49F and 22Rv1 Cell Tested Concentrations: 0.01, 0.1, 10, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of endogenous in LNCaP, C4-2 and MR49F cells AR transactivation is stimulated by the synthetic androgen R1881. |
| Animal Protocol |
Animal/Disease Models: Nude mice (Harlan SD (SD (Sprague-Dawley)); 25-31 g; 6-8 weeks) were inoculated subcutaneously (sc) (sc) with LNCaP cells and castrated [1]
Doses: 100 mg/kg Route of Administration: intraperitoneally (ip) (ip) twice (two times) daily for 4 weeks Experimental Results: Inhibits LNCaP tumor volume and prevents serum PSA production. |
| References |
|
| Molecular Formula |
C10H10BR2N4OS
|
|---|---|
| Molecular Weight |
394.08
|
| Exact Mass |
391.894
|
| CAS # |
1621375-32-3
|
| Related CAS # |
1621375-32-3;2230880-25-6 (45-dibromo-isomer);
|
| PubChem CID |
135150480
|
| Appearance |
White to off-white solid powder
|
| Density |
2.1±0.1 g/cm3
|
| Boiling Point |
542.8±60.0 °C at 760 mmHg
|
| Flash Point |
282.1±32.9 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.802
|
| LogP |
0.93
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
295
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
AZLNRGRZOLVWRX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C10H10Br2N4OS/c11-7-5-16(9(12)13-7)8-6-18-10(14-8)15-1-3-17-4-2-15/h5-6H,1-4H2
|
| Chemical Name |
4-[4-(2,4-dibromoimidazol-1-yl)-1,3-thiazol-2-yl]morpholine
|
| Synonyms |
VPC14449; VPC 14449; VPC-14449
|
| 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 : ~125 mg/mL (~317.19 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.28 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 (5.28 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 (5.28 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 | 2.5376 mL | 12.6878 mL | 25.3756 mL | |
| 5 mM | 0.5075 mL | 2.5376 mL | 5.0751 mL | |
| 10 mM | 0.2538 mL | 1.2688 mL | 2.5376 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
