| 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 | [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 | [InChIKey]
AZLNRGRZOLVWRX-UHFFFAOYSA-N | [SMILES]
C1COCCN1C2=NC(=CS2)N3C=C(N=C3Br)Br |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [in vivo]
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]. | Animal Model: | Nude mice (Harlan Sprague-Dawley; 25-31 g; 6-8 weeks) were subcutaneously inoculated with LNCaP cells and castrated[1] | | Dosage: | 100 mg/kg | | Administration: | I.p. twice daily for 4 weeks | | Result: | Suppressed LNCaP tumor volume and blocked serum PSA production. |
| [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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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|