|4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉|CsnPharm

CAS No.: 153436-54-5

PD153035 Catalog No. CSN12357

Synonyms: SU-5271;AG1517;ZM 252868

PD153035 is EGFR inhibitor with Ki and IC50 of 5.2 pM and 29 pM and could rapidly suppress autophosphorylation of EGFR.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:29pM IKKε

IC50:1-2μM
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 K_i 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 .
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7762 mL
- 13.8810 mL
- 27.7619 mL
- 5 mM
- 0.5552 mL
- 2.7762 mL
- 5.5524 mL
- 10 mM
- 0.2776 mL
- 1.3881 mL
- 2.7762 mL

技术信息

CAS号

153436-54-5

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14BrN3O2

运输

蓝冰

分子量

360.21

别名

SU-5271;AG1517;ZM 252868;NSC-669364;WHIP 79

溶解度

DMSO	6.0 mg/mL (16.7 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
EGFR		IC50:29pM
IKKε		IC50:1-2μM

PD153035 Catalog No. CSN12357

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