153436-54-5 Usage
Description
PD 153035 HYDROCHLORIDE, also known as AG-1517 HCl, is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR). It is a member of the class of quinazolines with a 3-bromophenylamino substituent at position 4 and two methoxy substituents at positions 6 and 7. PD 153035 HYDROCHLORIDE selectively blocks EGF-mediated cellular processes, including mitogenesis, early gene expression, and oncogenic transformation. It is an extremely useful tool for exploring EGF-mediated cellular signaling and is characterized as a yellowish solid.
Uses
Used in Pharmaceutical Industry:
PD 153035 HYDROCHLORIDE is used as an inhibitor for EGFR, competitive with ATP, due to its extremely potent and specific inhibitory effect on EGFR tyrosine kinase activity. This makes it a valuable compound for the development of targeted cancer therapies.
Used in Cancer Research:
PD 153035 HYDROCHLORIDE is used as a research tool for studying the role of EGFR in various cellular processes and its involvement in cancer cell growth. It helps researchers understand the mechanisms of EGF-mediated signaling and the potential of EGFR inhibition in cancer treatment.
Used in Drug Development:
PD 153035 HYDROCHLORIDE is used as a lead compound in the development of new drugs targeting EGFR-related pathways. Its potent and selective inhibition of EGFR tyrosine kinase activity makes it a promising starting point for designing more effective and targeted cancer therapies.
Used in Oncology:
PD 153035 HYDROCHLORIDE is used as an anticancer agent, particularly for inhibiting the growth of various cancer cell lines. Its ability to selectively block EGF-mediated cellular processes makes it a potential therapeutic option for patients with EGFR-driven cancers.
Biological Activity
An extremely potent inhibitor of epidermal growth factor (EGF) receptor tyrosine kinase, with an IC 50 of 25 pM. Inhibits other purified tyrosine kinases only at micromolar or higher concentrations.
References
1) Fry et al. (1994), A specific inhibitor of the epidermal growth factor receptor tyrosine kinase; Science, 265 1093
2) Bos et al. (1997), 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., 3 2099
3) Tetreault et al. (2008), Specific signaling cascades involved in cell spreading during healing of micro-wounded gastric epithelial monolayers; J. Cell. Biochem., 105 1240
Check Digit Verification of cas no
The CAS Registry Mumber 153436-54-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,3,4,3 and 6 respectively; the second part has 2 digits, 5 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 153436-54:
(8*1)+(7*5)+(6*3)+(5*4)+(4*3)+(3*6)+(2*5)+(1*4)=125
125 % 10 = 5
So 153436-54-5 is a valid CAS Registry Number.
InChI:InChI=1/C16H14BrN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)
153436-54-5Relevant articles and documents
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma
Asquith, Christopher R. M.,Naegeli, Kaleb M.,East, Michael P.,Laitinen, Tuomo,Havener, Tammy M.,Wells, Carrow I.,Johnson, Gary L.,Drewry, David H.,Zuercher, William J.,Morris, David C.
supporting information, p. 4772 - 4778 (2019/05/08)
We describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were characterized both in vitro and using in cell
A novel strategy to the synthesis of 4-anilinoquinazoline derivatives
Wang, Zheng,Wang, Cuiling,Sun, Yanni,Zhang, Ning,Liu, Zhulan,Liu, Jianli
, p. 906 - 913 (2014/01/23)
A novel approach to prepare 4-anilinoquinazoline derivatives based on the transformation of indoline-2,3-dione to formamidine was developed. The processes with this approach are simple, efficient, and environmentally friendly. The efficiency of this approach was evaluated by synthesizing 17 4-anilinoquinazolines and comparing the obtained yields with those achievable through conventional synthetic methods. It was the first time that compounds 8d, 8e, 8h, and 13b-f were synthesized. The characteristics of the IR and the UV spectra of these compounds and the effects of their substituents on the spectra were observed.
Impact of aryloxy-linked quinazolines: A novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors
Garofalo, Antonio,Goossens, Laurence,Six, Perrine,Lemoine, Amélie,Ravez, Séverine,Farce, Amaury,Depreux, Patrick
scheme or table, p. 2106 - 2112 (2011/04/24)
Three series of 6,7-dimethoxyquinazoline derivatives substituted in the 4-position by aniline, N-methylaniline and aryloxy entities, targeting EGFR and VEGFR-2 tyrosine kinases, were designed and synthesized. Pharmacological activities of these compounds
