572660
SU11652
A cell-permeable pyrrole-indolinone compound that acts as a potent, reversible, and ATP-competitive tyrosine kinase receptor and angiogenic inhibitor.
别名:
SU11652, 5-[(Z)-(5-Chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, PDGFR Tyrosine Kinase Inhibitor VIII, VEGFR Tyrosine Kinase Inhibitor XVII, VEGFR2 Kinase Inhibitor XIV
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关于此项目
经验公式（希尔记法）:
C22H27ClN4O2
化学文摘社编号:
分子量:
414.93
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥95% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
orange
solubility
DMSO: 4 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
Clc1cc2c(cc1)NC(=O)\C\2=C/c3[nH]c(c(c3C)C(=O)NCCN(CC)CC)C
InChI
1S/C22H27ClN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChI key
XPLJEFSRINKZLC-ATVHPVEESA-N
General description
A cell-permeable pyrrole-indolinone compound that acts as a potent, reversible, and ATP-competitive tyrosine kinase receptor and angiogenic inhibitor that exhibits greater selectivity for PDGFRβ (IC50 = 3 nM), VEGFR2 (IC50 = 27 nM), FGFR1 (IC50 = 170 nM), and Kit family members (IC50 = ~ 10-500 nM) over EGFR (IC50 >20 µM). Reported to display anti-proliferative and pro-apoptotic properties in tumor cells.
A cell-permeable, potent, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of PDGFRβ (IC50 = 3 nM), VEGFR2 (IC50 = 27 nM), FGFR1 (IC50 = 170 nM), and Kit family members (IC50 ~10-500 nM). Does not effect the activity of EGFR (IC50 >20 µM). Reported to display anti-proliferative, antiangiogenic and pro-apoptotic properties in tumor cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDGFRB
PDGFRB
Product competes with ATP.
Reversible: yes
Target IC50: 3 nM, 27 nM, 170 nM against PDGFRβ, VEGFR2, and FGFR1, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Heryanto, B., et al. 2003. Reproduction125, 334.
Sun, L., et al. 2003. J. Med. Chem.46, 1116.
Liao, A.T., et al. 2002. Blood100, 585.
Sun, L., et al. 2003. J. Med. Chem.46, 1116.
Liao, A.T., et al. 2002. Blood100, 585.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1