VPC-14449 |
Catalog No.GC62329
One-Click Copy Product Info
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VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1621375-32-3
Sample solution is provided at 25 µL, 10mM.
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VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer[1][2].
VPC-14449 (0.01-100 μM; 24 h) inhibits AR-transcriptional activity and cell viability in LNCaP, C4-2, MR49F, and 22Rv1 cells[2].VPC-14449 (0.01-100 μM; 24 h) dose-dependently inhibits the transiently expressed full-length human AR in PC3 cells (IC50=0.34 μM) without affecting AR protein expression[1].
VPC-14449 (100 mg/kg; i.p. twice daily for 4 weeks) reduces tumor volume and abolishes PSA production with no decrease in body weight over a total duration 4 weeks in LNCaP xenograft model[1].
[1]. Dalal K, et, al. Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer. J Biol Chem. 2014 Sep 19;289(38):26417-26429.
[2]. Dalal K, et, al. Bypassing Drug Resistance Mechanisms of Prostate Cancer with Small Molecules that Target Androgen Receptor-Chromatin Interactions. Mol Cancer Ther. 2017 Oct;16(10):2281-2291.
| Cas No. | 1621375-32-3 | SDF | |
| Formula | C10H10Br2N4OS | M.Wt | 394.09 |
| Solubility | DMSO : 125 mg/mL (317.19 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5375 mL | 12.6875 mL | 25.3749 mL |
| 5 mM | 507.5 μL | 2.5375 mL | 5.075 mL |
| 10 mM | 253.7 μL | 1.2687 mL | 2.5375 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)