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. Author manuscript; available in PMC: 2012 Jul 15.
Published in final edited form as: Cancer Res. 2011 May 25;71(14):4758–4768. doi: 10.1158/0008-5472.CAN-10-2527

Table 1.

IC50 (nM) values of XL880, XL184, XL999 and sorafenib on kinase activity

Kinases VEGFR-
2 (KDR)		 c-MET
(HGFR)		 FGFR1 PDGFR-
β		 KIT FLT1 FLT4 FLT3 Tie2 AXL RON
XL880 (27, 31) 0.86 0.4 660 9.6 6.7 6.8 2.8 3.6 1.1 11 3
XL184 (29, 32) 0.035 1.3 5294 234 4.6 12 6.0 11.3 14.3 7.0 124
XL999 (33, 34) 2.6 463 8.2 1.5 13.8 29 3.0 0.8 270 4.6 124
Sorafenib (50) 90 − 580 57 68 − − 33 − − −

IC50 values (nM) for inhibition of phosphorylation of 11 receptor tyrosine kinases by XL880, XL184, and XL999 show similarities for VEGFR-2, KIT, and AXL and differences for c-MET. XL880 and XL184 differ in inhibition of PDGFR-β and RON, and neither inhibits FGFR1. IC50 values of sorafenib are shown for comparison.