4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine
- Product Name
- 4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine
- CAS No.
- 1621375-32-3
- Chemical Name
- 4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine
- Synonyms
- 187295;4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine;4-(4-(2,4-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine;Morpholine, 4-[4-(2,4-dibromo-1H-imidazol-1-yl)-2-thiazolyl]-
- CBNumber
- CB93122173
- Molecular Formula
- C10H10Br2N4OS
- Formula Weight
- 394.09
- MOL File
- 1621375-32-3.mol
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
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.
4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine Preparation Products And Raw materials
Raw materials
Preparation Products
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