物质信息

ID:73016

名称和标识
IUPAC标准名
4-(4-{[2-(4-chlorophenyl)phenyl]methyl}piperazin-1-yl)-N-(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzenesulfonyl)benzamide
IUPAC传统名
4-(4-{[2-(4-chlorophenyl)phenyl]methyl}piperazin-1-yl)-N-(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzenesulfonyl)benzamide
别名
ABT-737
数据登录号
化合物性质
安全信息
保存条件
-20°C
产品相关信息
成盐信息
Free Base
药理学性质
作用靶点
Bcl-2
理化性质
溶解度
DMSO
描述信息
Research Area
Description
Cancer
Protocol
Kinase Assay [1]
Fluorescence polarization assays
Binding affinity of GST-Bcl-2 family proteins to the FITC-conjugated BH3 domain of Bim (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is determined. Briefly, 100 nM of GST-Bcl-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-Bim BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. Then IC50 are determined.
Cell Assay [4]
Cell Lines
SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
Concentrations
0.001-10 μM
Incubation Time
48 hours
Methods

SCLC cells are treated for 48 hours in 96-well tissue culture plates in a total volume of 100 μL tissue culture medium supplemented with 10% human serum. Viable cells are determined using the MTS assay.

Animal Study [1]
Animal Models
Scid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
Formulation
1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4?5; final concentration of DMSO ≤ 1%)
Doses
20 and 30 mg/kg
Administration
For intraperitoneal (i.p.) every day
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参考文献
• Whitecross KF, et al, Blood, 2009, 113(9), 1982-1991.
• Del Gaizo Moore V, et al. J Clin Invest, 2007, 117(1), 112-121.
• Tahir SK, et al. Cancer Res, 2007, 67(3), 1176-1183.
• Hikita H, et al. Hepatology. 2010, 52(4), 1310-21.
• Ishitsuka K, et al. Cancer Lett, 2012, 317(2), 218-225.
• van Delft MF,et al. Cancer Cell, 2006, 10(5), 389-399.
• Konopleva M, et al. Cancer Cell, 2006, 10(5), 375-388.
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