| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
T98260-1ml促销 |
10mM in DMSO | ￥720.00 ￥648.00 |
6 | - | - | - | - |
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| 产品描述： | VEGFR2 选择性抑制剂;VEGFR2 Selective Inhibitors;;InformationZD-4190 is a submicromolar inhibitor ofVEGF RTKactivity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.TargetsKDR ; Flt-1In vitroZD4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with greatest effect against KDR. Selectivity versus FGFR1 tyrosine kinase activity is demonstrated, with at least a 30-fold difference in the IC50 required to inhibit HUVEC proliferation stimulated by VEGF or bFGF, respectively. No effects on basal HUVEC growth are observed, even at the maximum ZD4190 concentration examined in these assays (10 μM).In vivoChronic once-daily oral dosing of ZD4190 to young rats produces a dose-dependent increase in the femoral epiphyseal growth plate area. Once-daily oral dosing of ZD4190 to mice bearing established (∼0.5 cm3) human tumor xenografts (breast, lung, prostate, and ovarian) elicits significant antitumor activity and at doses that would not be expected to have any direct antiproliferative effect on tumor cells. In a PC-3 xenograft model, 10 weeks of ZD4190 dosing prolongs tumor cytostasis and upon withdrawal of therapy, tumor growth resumed after a short delay. | ||||||||||||||||||||
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| 体内研究： | ZD4190 (100 mg/kg, p.o.) effectively delays MDA-MB-435 tumor growth in mice. In ZD4190-treated tumors, 18F-FPPRGD2 uptake has decreased significantly relative to baseline by 26.74±8.12% (p<0.05) on day 1 and by 41.19±6.63% (p<0.01) on day 3, then has returned to baseline on day 7. Tumor uptake of 18F-FLT has also decreased on both day 1 and day 3 after initiation of ZD4190 treatment. However, ZD4190 does not significantly change 18F-FDG uptake in tumors, compared with the control group. ZD4190 (50 mg/kg, p.o.) prevents outgrowth of residual tumour in a muscle model of minimal residual carcinoma. ZD4190 (12.5-100 mg/kg, p.o.) produces a dose-dependent reduction in K(trans) in PC-3 prostate tumors. At 100 mg/kg, ZD4190 reduces K(trans) in PC-3 tumors by 31% following 2 doses and by 53% following 8 doses. | ||||||||||||||||||||
| 参考文献： | 1. Yang M, et al. PET imaging of early response to the tyrosine kinase inhibitor ZD4190. Eur J Nucl Med Mol Imaging. 2011 Jul;38(7):1237-47. doi: 10.1007/s00259-011-1742-z. Epub 2011 Mar 1. 2. Gaballah K, et al. The antiangiogenic agent ZD4190 prevents tumour outgrowth in a model of minimal residual carcinoma in deep tissues. Br J Cancer. 2009 Aug 4;101(3):418-23. doi: 10.1038/sj.bjc.6605092. Epub 2009 Jul 21. 3. Checkley D, et al. Dynamic contrast-enhanced MRI of vascular changes induced by the VEGF-signalling inhibitor ZD4190 in human tumour xenografts. Magn Reson Imaging. 2003 Jun;21(5):475-82. |
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| 保存条件： | -80℃（运输条件：冰袋低温运输） | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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