PD153035

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Chemical Structure| 153436-54-5 同义名 : AG1517; ZM 252868; NSC 669364; SU-5271
CAS号 : 153436-54-5
货号 : A100205
分子式 : C16H14BrN3O2
纯度 : 99%+
分子量 : 360.21
MDL号 : MFCD00934896
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(97.17 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • EGFR/ErbB1

    EGFR, Ki:5.2 pM
描述 Many of the tyrosine kinase enzymes which are early components of the growth signal transduction pathway in mammalian cells are encoded by proto-oncogenes, and their transformation or overexpression has been shown to occur in a large percentage of clinical cancers. The epidermal growth factor receptor (EGFR), one of the tyrosine kinase enzymes, has thus become important target for cancer therapy. PD153035 is a potent and selective inhibitor against EGFR with an IC50 value of 25 pM and Ki value of 6 pM. PD153035 inhibited EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with IC50 of 14 nM [3]. In cell lines with the highest level of EGFR overexpression, PD153035 concentrations of ≥ 75 nM resulted in complete inhibition of receptor autophosphorylation. PD153035 caused a dose-dependent growth inhibition of EGFR-positive cell lines, beginning at less than micromolar concentrations, and the IC50 was less than 1 μM in most cases [4].
作用机制 PD153035 binds at the ATP site of EGFR .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.88mL

2.78mL

1.39mL

27.76mL

5.55mL

2.78mL
参考文献

[1]Bos M, Mendelsohn J, et al. 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]Fry DW, Kraker AJ, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5.

[3]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. doi: 10.1021/jm9503613. PMID: 8568816.

[4]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. PMID: 9815602.