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UNBS5162

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Chemical Structure| 956590-23-1 同义名 : -
CAS号 : 956590-23-1
货号 : A893890
分子式 : C17H18N4O3
纯度 : 99%+
分子量 : 326.35
MDL号 : MFCD22380608
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 20 mg/mL(61.28 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 UNBS5162 is a pan-antagonist of CXCL chemokine expression. In vitro exposure of PC-3 cells to UNBS5162 (1 μM for 5 successive days) dramatically decreased the expression of the proangiogenic CXCL chemokines shown by Affymetrix genome-wide microarray analysis and enzyme-linked immunosorbent assay. UNBS5162 at 10μM prevented PC-3 cell population development in vitro and caused a marked enlargement in PC-3 cells by the end of the 6-day treatment period. Similar effect of UNBS5162 could also be observed on DU-145 cells. Treatment of PC-3 and DU-145 cells with 10 μM UNBS5162 for 72 hours markedly blocked PC-3 cells in their G2 cell cycle phase. The percentage of PC-3 cells in the G2/M phase markedly increased; accordingly, the percentage of cells in the G1 phase diminished. It displayed antitumor effects in experimental models of human refractory prostate cancer when administered alone and found to enhance the activity of taxol when coadministered with the taxoid. Antiangiogenic properties in vivo for UNBS5162 in the orthotopic PC-3 model could be observed[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.32mL

3.06mL

1.53mL

30.64mL

6.13mL

3.06mL

参考文献

[1]Mijatovic T, Mahieu T, et al. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86.

[2]Mahadevan D, Northfelt DW, et al. Phase I trial of UNBS5162, a novel naphthalimide in patients with advanced solid tumors or lymphoma. Int J Clin Oncol. 2013 Oct;18(5):934-41.

[3]Mijatovic T, Mahieu T, Bruyère C, De Nève N, Dewelle J, Simon G, Dehoux MJ, van der Aar E, Haibe-Kains B, Bontempi G, Decaestecker C, Van Quaquebeke E, Darro F, Kiss R. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86. doi: 10.1593/neo.08290. PMID: 18516294; PMCID: PMC2386542.