521235
PDGFR Tyrosine Kinase Inhibitor VI, SU6668 - CAS 210644-62-5 - Calbiochem
The PDGFR Tyrosine Kinase Inhibitor VI, SU6668, also referenced under CAS 210644-62-5, controls the biological activity of PDGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
PDGFR Tyrosine Kinase Inhibitor VI, SU6668 - CAS 210644-62-5 - Calbiochem, (Z)-3-(2,4-Dimethyl-5-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl)-propionic acid, mTOR Inhibitor X, VEGFR Tyrosine Kinase Inhibitor XXVII, VEGFR2 Kinase Inhibitor XXV, Aurora Kinase Inhibitor IV
InChI key
NHFDRBXTEDBWCZ-ZROIWOOFSA-N
InChI
1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9-
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
dark yellow
solubility
DMSO: 100 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable indolinone compound that acts as a potent ATP-competitive inhibitor against RTKs (receptor tyrosine kinases) Kit, PDGFRβ, VEGFR2 (Flk-1/KDR), FGFR1 activity in vitro (IC50 = 0.01, 0.1, 3.9, and 3.8 µM, respectively) and PDGF/VEGF/bFGF-mediated angiogenesis and tumor development in vivo. Although initially characterized as an RTK inhibitor, SU6668 is now also known to target ser/thr kinases Aurora A, Aurora B, TBK1 (NAK/T2K), and AMPK (IC50 = 0.85, 0.047, 1.4, and 1.8 µM, respectively), as well as non-receptor TKs Lyn and Yes (IC50 = 4.3 and 5.8 µM, 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
Godl, K., et al. 2005. Cancer Res.65, 6919.
Laird, A.D., et al. 2002. FASEB J.16, 681.
Krystal, G.W., et al. 2001. Cancer Res.61, 3660.
Smolich, B.D., et al. 2001. Blood97, 1413.
Laird, A.D., et al. 2000. Cancer Res.60, 4152.
Shaheen, R.M., et al. 1999. Cancer Res.59, 5412.
Sun, L. et al. 1999. J. Med. Chem.42, 5120.
Laird, A.D., et al. 2002. FASEB J.16, 681.
Krystal, G.W., et al. 2001. Cancer Res.61, 3660.
Smolich, B.D., et al. 2001. Blood97, 1413.
Laird, A.D., et al. 2000. Cancer Res.60, 4152.
Shaheen, R.M., et al. 1999. Cancer Res.59, 5412.
Sun, L. et al. 1999. J. Med. Chem.42, 5120.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
L Sun et al.
Journal of medicinal chemistry, 42(25), 5120-5130 (1999-12-22)
Receptor tyrosine kinases (RTKs) have been implicated as therapeutic targets for the treatment of human diseases including cancers, inflammatory diseases, cardiovascular diseases including arterial restenosis, and fibrotic diseases of the lung, liver, and kidney. Three classes of 3-substituted indolin-2-ones containing
A Douglas Laird et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 16(7), 681-690 (2002-04-30)
SU6668 is a small molecule inhibitor of the angiogenic receptor tyrosine kinases Flk-1/KDR, PDGFRbeta, and FGFR1. In mice, SU6668 treatment resulted in regression or growth arrest of all large established human tumor xenografts examined associated with loss of tumor cellularity.
R M Shaheen et al.
Cancer research, 59(21), 5412-5416 (1999-12-20)
Increased vascular endothelial growth factor (VEGF) expression is associated with colon cancer metastases. We hypothesized that inhibition of VEGF receptor activity could inhibit colon cancer liver metastases. BALB/c mice underwent splenic injection with CT-26 colon cancer cells to generate metastases.
B D Smolich et al.
Blood, 97(5), 1413-1421 (2001-02-27)
SU5416 and SU6668 are potent antiangiogenic small-molecule inhibitors of receptor tyrosine kinases, including those of the vascular endothelial growth factor and platelet-derived growth factor receptor families. The stem cell factor (SCF) receptor, c-kit, is structurally related to these receptors and
G W Krystal et al.
Cancer research, 61(9), 3660-3668 (2001-04-28)
Six indolinone tyrosine kinase inhibitors were characterized for their ability to inhibit Kit kinase and for their effects on the growth of small cell lung cancer (SCLC) cell lines. All of the six compounds were potent inhibitors of Kit kinase
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