676503
VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor
The VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor controls the biological activity of VEGFR/Tie-2/PDGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor, 1-(2-Fluoro-4-((5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)oxy)phenyl)-3-(3-(trifluoromethyl)phenyl)urea, PDGFR Tyrosine Kinase Inhibitor XXI, VEGFR Tyrosine Kinase Inhibitor XXXIV, VEGFR2 Kinase Inhibitor XXXII, VEGFR1 Kinase Inhibitor VII
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
light beige
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
O=C(NC1=CC(C(F)(F)F)=CC=C1)NC2=CC=C(OC3=NC=NC4=C3N(C)C=C4)C=C2F
一般描述
An orally bioavailable pyrrolopyrimidinylurea compound that simultaneously binds to both the adenine and the adjacent hydrophobic pocket of the inactive form of VEGFR2 with high-affinity (type-II inhibitor) and acts as a pseudo-irreversible inhibitor with prolonged action. Shown to potently inhibit the activities of VEGFR2, VEGFR1, Tie-2, PDGFRα, PDGFRβ and c-kit (IC50 = 6.2, 15, 20, 35, 96 and 170 nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC50 = 0.9 and 1.05 µM) and FGFR1, HER2, EGFR, IR, PKCθ (>10 µM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC50 = 4.4 µM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6 mg/kg, b.i.d.).
包装
Packaged under inert gas
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.
其他说明
Oguro, Y., et al. 2010. Bioorg. Med. Chem.18, 7150.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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