产品报价：询价
更新时间：2012/7/26 10:39:49
产地：美国
品牌：selleck
型号：CAS号: 1213269-23-8
厂商性质： 生产型,贸易型,
公司名称： 赛导通生物科技（广州）有限公司
潘贺华 : (13926198506) (400-168-1698)
（联系我时，请说明是在来宝网上看到的，谢谢！）| 分子量(MW): | 494.18 |  |
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| 化学式: |
C25H27ClN6O3 |
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| 溶解度: | DMSO ≥13mg/mL Water <1mg/mL Ethanol <1mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 1213269-23-8 |
WZ4002不可逆抑制表皮生长因子T790M突变，IC50<20nM。WZ4002不可逆抑制表皮生长因子T790M突变,这种突变是在50%抗gefitinib和 erlotinib的患者身上发现的。WZ4002
有着和其他EGFR抑制剂不同的基本化学结构。与体内带有喹唑啉基的EGFR抑制剂HKI-272 和CL-387,785相比，WZ4002作用于EGFR T790M突变型时效果强30-100倍，而作用于野生型EGFR时效果弱到100倍。低于最大抑制浓度的一半的WZ4002和其他还处于临床阶段的抑制剂如HKI-272联用作用于PC9GR(delE746_A750/T790M,抗gefitinib的突变) 细胞，效果达到300倍。在两周的有效研究中发现，同时作用于鼠类T790M突变，与空白对照组相比，用WZ4002处理导致肿瘤的明显退化。WZ4002目前还处在临床研究阶段。WZ4002最初是由波士顿的Dana Farber癌症研究所研究的。[1]
[1] Nature. 2009 December 24; 462(7276): 1070–1074.
[2] Cancer Cell.2007 Mar;11(3):217-27
[3] Science.2007 May 18;316(5827):1039-43. Epub 2007 Apr 26
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(a) Western blots examine the effects of WZ4002 alone or a combination of WZ4002 and ABT-263 in H1975 parental or SR cells in suspension. Cells were grown for 48 h and then treated with the indicated pharmacological agent(s) for another 24 h. The cleaved/total poly (ADP-ribose) polymerase-1 (PARP-1) ratio determined for each cell line using Image J software is also represented. The values are the means of three independent experiments. (b) Quantification of apoptotic cells assessed by PARP-1 cleavage from each cell line. |
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Caspase 3/7 activation in H1975 SR cells and HCC827 cells. Cells were seeded and left in suspension for 24 h, and then untreated or treated with the indicated drug(s) for another 24 h before being assessed. Caspase activity was evaluated by using the Caspase-Glo 3/7 assay and normalized to a 1.0 arbitrary unit for the mean of three untreated wells. |
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For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WZ4002 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. |
特定的存储和包装每个产品的信息在产品说明书上都有注明 。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20 ° C ，抗体及蛋白等产品建议-60℃。抑制剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。
