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GDC-0152
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GDC-0152图片
CAS NO:873652-48-3
包装:10mg, 50mg
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍

生物活性

GDC-0152是一种有效的XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3和cIAP2-BIR3拮抗剂,Ki分别为28 nM, 14 nM, 17 nM和43 nM,对cIAP1-BIR2和cIAP2-BIR2具有低的亲和力。GDC-0152可阻断IAP蛋白和促凋亡分子参与的蛋白质-蛋白质的相互作用。GDC-0152瞬时转染HEK293T细胞,表现为扰乱XIAP结合部分处理的caspase-9并扰乱ML-IAP,CIAP1,cIAP2和Smac蛋白的结合。在黑色素瘤SK-MEL28细胞中,GDC-0152有效抑制ML-IAP和Smac蛋白的内源性结合。


化学数据

分子量498.64
分子式C25H34N6O3S
CAS号873652-48-3
纯度>98%
溶解性(25°C)DMSO 79 mg/mL
Ethanol 60 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系MDA-MB-231, mormal HMECs cell lines
方法Cell Viability and Caspase Activation Assays Human breast carcinoma MDA-MB-231 were obtained from ATCC. Normal human mammary epithelial cells (HMECs) were obtained from Cambrex Corp.. Cells were dissociated from tissue culture flasks by incubation with Accutase(R) (Innovative Cell Technology Inc.) for 5–10 minutes. Detached cells were washed with phosphate-buffered saline (PBS) and were resuspended in assay media (MDA-MB-231 cells: RPMI1640 supplemented with 10% fetal bovine serum [Sigma-Aldrich] and 2 mM L-glutamine [GlutaMAX-1; Gibco/Invitrogen Corp.]) or culture media (HMECs: MEBM(R) with MEGM SingleQuots(R) provided by Cambrex Corp.). Cells were placed in tissue culture-treated, white-wall (Corning, Inc.) or black-wall (PE Biosystems), clear-bottom, 96-well plates at 1 × 104 cells/well in a volume of 50 μL. The plates were incubated at 37°C and 5% CO2 overnight, the media was removed, and 1 or it's enantiomer were added in assay media. Cells cultured in white-wall, clear-bottom plates were incubated at 37°C and 5% CO2 for 3 days before cell viability was measured using the CellTiter-Glo(R) luminescent cell viability assay kit (Promega Corp.) according to the manufacturer's instructions. Cells seeded in black-wall, clear-bottom plates were incubated at 37°C and 5% CO2 for 3–24 hours before caspase-3 and -7 homogeneous activities were assessed using the Apo-ONE(R) caspase-3/7 assay kit (Promega Corp.) according to the manufacturer's instructions.
浓度
处理时间3 days

动物实验
动物模型Human breast cancer MDA-MB-231 cells tumor xenograft mice
配制PBS
剂量4.0 ml/kg
给药处理oral gavage

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.0055 mL10.0273 mL20.0545 mL
5 mM0.4011 mL2.0055 mL4.0109 mL
10 mM0.2005 mL1.0027 mL2.0055 mL