212141-51-0 Usage
Description
Vatalanib Dihydrochloride, also known as PTK787, is a potent antagonist of the Vascular Endothelial Growth Factor (VEGF) receptors, specifically inhibiting the receptor tyrosine kinase activities of VEGFR1 (Flt1), VEGFR2 (KDR), and VEGFR3 (Flt4) with IC50 values of 77, 37, and 190 nM, respectively. It is a white to off-white crystalline powder that less potently inhibits PDGF and c-Kit (IC50 = 600 and 700 nM) and has no effect on a large panel of additional kinases. Vatalanib completely blocks retinal neovascularization in oxygen-induced ischemic retinopathy in mice, suggesting its use in diabetic retinopathy and other diseases featuring aberrant vascular development.
Uses
Used in Anticancer Applications:
Vatalanib Dihydrochloride is used as an antineoplastic agent for inhibiting the VEGF receptors, which play a crucial role in tumor angiogenesis and growth. By targeting VEGFR1, VEGFR2, and VEGFR3, Vatalanib Dihydrochloride disrupts the signaling pathways that promote the formation of new blood vessels, thereby limiting the supply of nutrients and oxygen to the tumor and inhibiting its growth.
Used in Vascular Disorders:
Vatalanib Dihydrochloride is used as a treatment for vascular disorders characterized by aberrant vascular development, such as diabetic retinopathy. Its ability to completely block retinal neovascularization in oxygen-induced ischemic retinopathy in mice suggests its potential use in managing and treating these conditions.
Used in Pharmaceutical Research:
Vatalanib Dihydrochloride is used as a research tool for studying the role of VEGF receptors in various diseases and conditions. Its potent inhibition of VEGFR1, VEGFR2, and VEGFR3 makes it a valuable compound for investigating the underlying mechanisms of angiogenesis and vascular development in both health and disease.
Used in Drug Development:
Vatalanib Dihydrochloride is used as a lead compound in the development of new drugs targeting VEGF receptors for the treatment of various cancers and vascular disorders. Its potent inhibitory activity and selectivity for VEGF receptors make it an attractive starting point for designing and optimizing novel therapeutic agents.
Used in Drug Delivery Systems:
Vatalanib Dihydrochloride can be used as an active pharmaceutical ingredient in the development of drug delivery systems, such as nanoparticles or liposomes, to improve its bioavailability, delivery, and therapeutic outcomes. These systems can help overcome limitations associated with the compound's solubility, stability, or pharmacokinetic properties, enhancing its overall efficacy and safety in clinical applications.
References
1) Wood?et al. (2000),?PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration;? Cancer Res.,?60?2178
2) Lin?et al. (2002),?The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in bone marrow microenvironment;? Cancer Res.,?62?5019
Check Digit Verification of cas no
The CAS Registry Mumber 212141-51-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,1,2,1,4 and 1 respectively; the second part has 2 digits, 5 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 212141-51:
(8*2)+(7*1)+(6*2)+(5*1)+(4*4)+(3*1)+(2*5)+(1*1)=70
70 % 10 = 0
So 212141-51-0 is a valid CAS Registry Number.
InChI:InChI=1/C20H15ClN4.2ClH/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14;;/h1-12H,13H2,(H,23,25);2*1H
