产品说明书

PD 153035 HCl

Print
Chemical Structure| 183322-45-4 同义名 : ZM 252868 Hydrochloride;AG1517 Hydrochloride;AG-1517;PD 153035 (hydrochloride);SU-5271 Hydrochloride;PD153035 Hydrochloride
CAS号 : 183322-45-4
货号 : A187704
分子式 : C16H15BrClN3O2
纯度 : 98%
分子量 : 396.666
MDL号 : MFCD01074805
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(10.08 mM)，配合低频超声，并水浴加热至45℃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
动物实验配方：
生物活性
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 . 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 .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.21mL

5.04mL

2.52mL
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.