4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine Property

Boiling point:

551.4±60.0 °C(Predicted)

Density 

2.12±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 125 mg/mL (317.19 mM; Need ultrasonic)

form 

Solid

pka

2.01±0.50(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine Chemical Properties,Usage,Production

Biological Activity

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].

References

[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.