PD 153035 hydrochloride
(Synonyms: ZM252868,PD153035 HCL) 目录号 : GC15983
A highly potent EGFR inhibitor
Cas No.:183322-45-4
Sample solution is provided at 25 µL, 10mM.
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PD153035 (4-(3-Bromoanilino)-6,7-dimethoxyquinazoline) is an extremely potent epidermal growth factor receptor (EGFR) inhibitor that competitively binds at the ATP site with the half maximal inhibition concentration IC50 of 0.025 nM resulting in the inhibition of the tyrosine kinase activity of the EGFR [1].
PD153035 has been found to inhibit EGF-dependent EGFR phosphorylation in a variety of human cancer cell lines over-expressing EGFRs, which include A431, Difi, DU145, MDA-MB-468, ME180 and C4i, with IC50 of 0.22 μM, 0.3 μM, 0.4 μM, 0.68 μM, 0.95 μM and 2.5 μM respectively leading to suppression of proliferation and clonogenicity in those cell lines [2].
Besides exerting potent inhibition against EGFRs, PD153035 also inhibits the closely related HER2/neu receptor but to a lesser degree [2].
References:
[1] Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ, Denny WA. 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.
[2] Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.
| Cell experiment [1]: | |
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Cell lines |
A panel of cancer cell lines overexpressing various levels of EGF receptor and HER2/neu. |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.5-2800 nM; 2 h |
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Applications |
In EGF receptor-overexpressing cell lines, PD153035 caused a dose-dependent decrease in ligand-inducedEGF receptor phosphorylation. PD153035 only inhibited HER2/neu phosphorylation at the highest concentrations tested (1400-2800 nM). PD153035 also inhibited cell proliferation in EGF receptor-positive cell lines. |
| Animal experiment [2]: | |
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Animal models |
Immunodeficient nude mice xenografted with A431 human epidermoid tumors |
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Dosage form |
i.p. dose of 80 mg/kg |
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Application |
In immunodeficient nude mice xenografted with A431 human epidermoid tumors, PD153035 rapidly suppressed the tyrosine phosphorylation of the EGF receptor by 80-90% in the tumors. Following a single i.p. dose of 80 mg/kg, the drug levels in the plasma and tumor rose to 50 and 22 μM within 15 minutes. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106. [2]. Kunkel MW1, Hook KE, Howard CT, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302. | |
| Cas No. | 183322-45-4 | SDF | |
| 别名 | ZM252868,PD153035 HCL | ||
| 化学名 | N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine | ||
| Canonical SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC | ||
| 分子式 | C16H14BrN3O2.HCl | 分子量 | 396.67 |
| 溶解度 | ≥ 3.97mg/mL in DMSO with gentle warming, <1.83 mg/mL in EtOH, <2.81 mg/mL in Water | 储存条件 | Store at RT |
| 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 | |||
 |
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