171179-06-9 Usage
Description
PD158780 is a potent tyrosine kinase inhibitor of the epidermal growth factor receptor (EGFR), characterized by its high specificity and affinity for the target enzyme. It is known for its ability to inhibit heregulin-stimulated autophosphorylation in breast carcinomas and to suppress the activation of MAP kinase kinase 1/2 (MKK1/2) and EGFR tyrosine phosphorylation in various cell lines. The inhibitory action of PD158780 is competitive, as it binds to the ATP site of the enzymes, thereby preventing their activation.
Uses
Used in Oncology:
PD158780 is used as an anticancer agent for delaying the substantial growth of tumors in vivo tumor models. It targets the EGFR tyrosine kinase activity, which plays a crucial role in cell proliferation and tumor growth. By inhibiting this activity, PD158780 can potentially slow down or halt the progression of cancer.
Used in Pharmaceutical Research:
In the field of pharmaceutical research, PD158780 is used as a research tool for studying the role of EGFR in various cellular processes and its potential as a therapeutic target for cancer treatment. Its high potency and specificity make it an invaluable compound for investigating the molecular mechanisms underlying EGFR-mediated signaling pathways and the development of resistance to EGFR inhibitors.
Used in Drug Development:
PD158780 serves as a lead compound in the development of novel EGFR inhibitors for cancer therapy. Its competitive inhibition of the ATP site of the enzyme makes it a promising starting point for the design and synthesis of new, more potent, and selective EGFR inhibitors with improved pharmacological properties and reduced side effects.
Used in Drug Delivery Systems:
Similar to gallotannin, PD158780 can also benefit from novel drug delivery systems to enhance its applications and efficacy against cancer cells. Various organic and metallic nanoparticles can be employed as carriers for PD158780 delivery, aiming to improve its delivery, bioavailability, and therapeutic outcomes.
Biological Activity
Potent inhibitor of ErbB receptor family tyrosine kinases (IC 50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G 1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells.
Biochem/physiol Actions
Cell permeable: yes
Check Digit Verification of cas no
The CAS Registry Mumber 171179-06-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,1,1,7 and 9 respectively; the second part has 2 digits, 0 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 171179-06:
(8*1)+(7*7)+(6*1)+(5*1)+(4*7)+(3*9)+(2*0)+(1*6)=129
129 % 10 = 9
So 171179-06-9 is a valid CAS Registry Number.
InChI:InChI=1/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20)
171179-06-9Relevant articles and documents
Process for preparing 4,6-disubstituted pyrido[3,4-d]pyrimidines
-
, (2008/06/13)
An improved process for the preparation of 4,6-disubstituted pyrido[3,4-d]pyrimidines is described where 5-amino-2-fluoropyridine is converted in seven operations to the desired products, as well as other valuable intermediates used in the process.
Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
-
, (2008/06/13)
-
