| Identification | Back Directory | [Name]
4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine | [CAS]
1621375-32-3 | [Synonyms]
187295
4-(4-(2,4-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine
4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine
Morpholine, 4-[4-(2,4-dibromo-1H-imidazol-1-yl)-2-thiazolyl]- | [Molecular Formula]
C10H10Br2N4OS | [MDL Number]
MFCD32206764 | [MOL File]
1621375-32-3.mol | [Molecular Weight]
394.086 |
| Chemical Properties | Back Directory | [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 Information | Back Directory | [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. |
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ChemShuttle, Inc.
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0510-83588313-802 18800520310; |
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https://www.jiehuapharma.com/ |
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DC Chemicals
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021-58447131 13564518121 |
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https://www.chemicalbook.com/ShowSupplierProductsList927327/0.htm |
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