ZD-4190
目录号 : GC33171
ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
Cas No.:413599-62-9
Sample solution is provided at 25 µL, 10mM.
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ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
ZD4190 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)[1].
Chronic 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[1].
[1] Wedge SR, et al. Cancer Res. 2000, 60(4):970-5.
Cell experiment: | The cytotoxicity of ZD4190 for PDVC57B cells is established when 104 cells are exposed to 1-10 μM ZD4190 for 96 h before MTS solution is added and the optical density measured at 490 nm. Cells are also grown to 40% confluence and treated with 1-100 μM ZD4190 for 7 days and the cytopathic effect examined by staining with crystal violet. |
Animal experiment: | ZD4190 is suspended in a 1% (v/v) solution of polyoxyethylene sorbitan mono-oleate in deionized water and administered by oral gavage (0.1 mL/10 g body weight). In each experiment, mice are randomized to receive either vehicle or ZD4190, administered once daily using a 1 day (at 0 and 22 h) or 7 day (at 0, 24, 48, 72, 96, 120, 144, and 166 h) treatment regimen (i.e., daily administration of compound for 1 or 7 days with an additional dose given 2 h prior to the end of the treatment period) followed by DCEMRI under terminal anesthesia. |
References: [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. | |
| Cas No. | 413599-62-9 | SDF | |
| Canonical SMILES | COC1=CC2=C(NC3=CC=C(Br)C=C3F)N=CN=C2C=C1OCCN4N=NC=C4 | ||
| 分子式 | C19H16BrFN6O2 | 分子量 | 459.27 |
| 溶解度 | DMSO : 20.83 mg/mL (45.35 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1774 mL | 10.8868 mL | 21.7737 mL |
| 5 mM | 0.4355 mL | 2.1774 mL | 4.3547 mL |
| 10 mM | 0.2177 mL | 1.0887 mL | 2.1774 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet