PD153035 Hydrochloride (ZM 252868)
(Synonyms: SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride) 目录号 : GC34105
A highly potent EGFR inhibitor
Cas No.:183322-45-4
Sample solution is provided at 25 µL, 10mM.
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Overactivity of the epidermal growth factor receptor-
1.Ciardiello, F., and Tortora, G.A novel approach in the treatment of cancer: Targeting the epidermal growth factor receptorClin. Cancer Res.7(10)2958-2970(2001) 2.Fry, D.W., Kraker, A.J., McMichael, A., et al.A specific inhibitor of the epidermal growth factor receptor tyrosine kinaseScience265(5175)1093-1095(1994) 3.Bos, M., Mendelsohn, J., Kim, Y.M., et al.PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent mannerClin. Cancer Res.3(11)2099-2106(1997) 4.Rae, J.M., and Lippman, M.E.Evaluation of novel epidermal growth factor receptor tyrosine kinase inhibitorsBreast Cancer Res. Treat.83(2)99-107(2004)
Cell experiment: | Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5 p.M. Growth inhibitory effect in monolayer cell culture is assessed[3]. |
Animal experiment: | Mice: Mice are injected with PD153035 (80 mg/kg) or vehicle and rumors are excised at 20 minutes and 180 minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD 153035 of the EGF-stimulation[3]. |
References: [1]. Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76. | |
| Cas No. | 183322-45-4 | SDF | |
| 别名 | SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride | ||
| Canonical SMILES | COC1=C(C=C(C2=C1)N=CN=C2NC3=CC(Br)=CC=C3)OC.Cl | ||
| 分子式 | C16H15BrClN3O2 | 分子量 | 396.67 |
| 溶解度 | DMSO : 5.125 mg/mL (12.92 mM) | 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 | 2.521 mL | 12.6049 mL | 25.2099 mL |
| 5 mM | 0.5042 mL | 2.521 mL | 5.042 mL |
| 10 mM | 0.2521 mL | 1.2605 mL | 2.521 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
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet