Tag: M.W=400-450

Bold, Guido’s team published research in Drugs of the Future in 27 | CAS: 300842-64-2

Drugs of the Future published new progress about 300842-64-2. 300842-64-2 belongs to phthalazine, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, and the molecular formula is C21H17BrN4, Application In Synthesis of 300842-64-2.

Bold, Guido published the artcileCGP 79787D (PTK787/ZK222584), CGP 84738, NVP-AAC789, NVP-AAD777, and related 1-anilino-(4-pyridylmethyl)phthalazines as inhibitors of VEGF- and bFGF-induced angiogenesis, Application In Synthesis of 300842-64-2, the publication is Drugs of the Future (2002), 27(1), 43-55, database is CAplus.

A review. The pharmacol. profile of the class of 1-anilino-(4-pyridylmethyl)-phthalazines is presented. 1-Anilino-(4-pyridylmethyl)phthalazines are potent, selective and orally well absorbed inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinases. In vitro they block VEGF-stimulated autophosphorylation of KDR expressing cells, resulting in the inhibition of survival effects of VEGF on endothelial cells. They also block platelet derived factor-mediated effects at slightly higher concentration but do not affect other pathways such as the bFGF receptor.

Drugs of the Future published new progress about 300842-64-2. 300842-64-2 belongs to phthalazine, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, and the molecular formula is C21H17BrN4, Application In Synthesis of 300842-64-2.

Tille, J.-C.’s team published research in Journal of Pharmacology and Experimental Therapeutics in 299 | CAS: 300842-64-2

Journal of Pharmacology and Experimental Therapeutics published new progress about 300842-64-2. 300842-64-2 belongs to phthalazine, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, and the molecular formula is C8H8O3, Recommanded Product: N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine.

Tille, J.-C. published the artcileVascular endothelial growth factor (VEGF) receptor-2 antagonists inhibit VEGF- and basic fibroblast growth factor-induced angiogenesis in vivo and in vitro, Recommanded Product: N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, the publication is Journal of Pharmacology and Experimental Therapeutics (2001), 299(3), 1073-1085, database is CAplus and MEDLINE.

Exponential tumor growth is angiogenesis-dependent. Vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF) are potent angiogenic inducers that act synergistically in vivo and in vitro. We assessed the effect of specific inhibitors of VEGF receptor (VEGFR)-2 tyrosine kinase activity in in vivo and in vitro models of VEGF- and bFGF-induced angiogenesis. In an implant mouse model of angiogenesis, VEGFR-2 inhibitors completely blocked angiogenesis induced by VEGF, and, surprisingly, also inhibited the effect of bFGF to various extents. In vitro, VEGF- and bFGF-induced bovine microvascular and aortic endothelial (BME and BAE) cell collagen gel invasion could be blocked by the VEGFR-2 inhibitors by 100 and ∼90%, resp. Similar results were obtained with VEGFR-1-IgG and VEGFR-3-IgG fusion proteins and with VEGFR-2 blocking antibodies. Both BME and BAE cells produce VEGF and VEGF-C, which is not modulated by bFGF. Thus, the unexpected inhibition of bFGF-induced angiogenesis by VEGFR-2 antagonists reveals a requirement for endogenous VEGF and VEGF-C in this process. These findings broaden the spectrum of mediators of angiogenesis that can be inhibited by VEGFR-2 antagonists and highlight the importance of these compounds as agents for inhibiting tumor growth sustained by both VEGF and bFGF.

Journal of Pharmacology and Experimental Therapeutics published new progress about 300842-64-2. 300842-64-2 belongs to phthalazine, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, and the molecular formula is C8H8O3, Recommanded Product: N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine.