288144-20-7 Usage
Description
VEGFR2 Kinase Inhibitor II is a cell-permeable and reversible indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor with an IC50 of 70 nM for VEGF-R2 (KDR/Flk-1), 920 nM for PDGF-Rβ, 4.92 μM for p60c-src, and 13.3 μM for FGF-R1. Its inhibition is suggested to be competitive with respect to ATP. It also inhibits VEGF-induced and PDGF-induced cell proliferation in umbilical vein endothelial cells (HUVEC) but does not exhibit any inhibitory effect on EGF-R kinase activity.
Uses
Used in Pharmaceutical Industry:
VEGFR2 Kinase Inhibitor II is used as a research tool for studying the role of VEGFR2 in angiogenesis and tumor growth. Its ability to inhibit VEGF-induced and PDGF-induced cell proliferation makes it a potential candidate for the development of anti-angiogenic therapies and cancer treatments.
Used in Drug Discovery:
VEGFR2 Kinase Inhibitor II is used as a lead compound in the development of new drugs targeting receptor tyrosine kinases, which play a crucial role in various cellular processes, including cell growth, differentiation, and migration. Its selectivity for different kinases can aid in the design of more targeted and effective therapeutic agents.
Used in Cancer Research:
VEGFR2 Kinase Inhibitor II is used as a research compound to investigate the mechanisms of angiogenesis and tumor growth in various cancer types. Its inhibitory effects on VEGF-R2 and PDGF-Rβ can provide insights into the development of novel anti-cancer strategies and the identification of potential biomarkers for cancer progression.
Used in Angiogenesis Studies:
VEGFR2 Kinase Inhibitor II is used as a research reagent to study the process of angiogenesis, which is the formation of new blood vessels from pre-existing ones. Its ability to inhibit VEGF-induced cell proliferation can help researchers understand the molecular mechanisms underlying angiogenesis and identify potential targets for therapeutic intervention in various diseases, including cancer, diabetic retinopathy, and age-related macular degeneration.
Biochem/physiol Actions
Cell permeable: yes
Check Digit Verification of cas no
The CAS Registry Mumber 288144-20-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,8,8,1,4 and 4 respectively; the second part has 2 digits, 2 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 288144-20:
(8*2)+(7*8)+(6*8)+(5*1)+(4*4)+(3*4)+(2*2)+(1*0)=157
157 % 10 = 7
So 288144-20-7 is a valid CAS Registry Number.
288144-20-7Relevant articles and documents
Identification of substituted 3-[(4,5,6,7-tetrahydro-1H- indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rβ tyrosine kinases
Sun, Li,Tran, Ngoc,Liang, Congxing,Hubbard, Steve,Tang, Flora,Lipson, Kenneth,Schreck, Randall,Zhou, Yong,McMahon, Gerald,Tang, Cho
, p. 2655 - 2663 (2007/10/03)
A series of new 3-substituted indolin-2-ones containing a tetrahydroindole moiety was developed as specific inhibitors of receptor tyrosine kinases associated with VEGF-R, FGF-R, and PDGF-R growth factor receptors. These compounds were evaluated for their
