. Author manuscript; available in PMC: 2013 Oct 31.

Published in final edited form as: Biochim Biophys Acta. 2009 Jan 31;1795(2):10.1016/j.bbcan.2009.01.003. doi: 10.1016/j.bbcan.2009.01.003

Table 1.

Biochemical and biological comparisons between selective and non-selective compounds against B-Raf^V600E used previously published in vitro and/or in vivo experimental models of human thyroid cancer.

Compound	Targeted gene	Human thyroid cancer cell line harboring B-Raf^V600E	Animal model	B-Raf^V600E inhibition (IC₅₀)	Biological effects (in vitro and in vivo studies)	Clinical trial
PLX4032 ^a	B-Raf^V600E	NPA^, ARO^	no	126 nmol/L or 205 nmol/L	Cell growth arrest; apoptosis	Phase I
BAY 43-9006 (sorafenib)^b,^c,^d	wild-type B-Raf, B- Raf^V600E, C-Raf, VEGFR-2 and 3, Flt-3, PDGFR-B, FGFR1, c-KIT, p38α, RET tyrosine kinase	NPA^, ARO^, KAT-4^, 8505c, FRO, DRO^, TPC-1 (harbors RET/PTC-1 and wild type B-Raf), TT (harbors oncogenic RET and wild type B-Raf but not B-Raf^V600E)	Xenograft by ARO^, DRO^ and TT cell lines	5 µmol/L or 1 µmol/L	Cell growth arrest and apoptosis in vitro (cytostatic effects); cell growth arrest and apoptosis in vivo	Phase II
AAL-881^e AAL-881^f	wild-type B-Raf, B-Raf^V600E, C-Raf, c-ABL, VEGFR2	NPA^, ARO^, FRO BHP-5^, BHP-14^, BHP-17^, BHP-18, BHP-19, NPA^, ARO^*, FRO	Xenograft by NPA^* and ARO^* cell lines no	0.22 µmol/L 5 µmol/L	Cell growth arrest in vitro and in vivo apoptosis	no
LBT-613^e	wild-type B-Raf, B-Raf^V600E, C-Raf, RET tyrosine kinase, c-ABL, VEGFR2	NPA^, ARO^, FRO	Xenograft by NPA^* and ARO^* cell lines	0.21 µmol/L	Cell growth arrest in vitro and in vivo	no

IC₅₀= concentration of compound that inhibits the kinase activity by 50%.

Abbreviations: FGFR-1, fibroblast growth factor receptor-1; PDGFR, platelet-derived growth factor receptor; VEGFR, vascular endothelial growth factor receptor.

= reference 73;

= reference 66;

= reference 67;

= reference 68;

= reference 70;

= reference 71.

Note that a very recent publication (reference 64) demonstrates that all these cell lines may be in fact melanoma (NPA, DRO, BHP5-16, BHP14-9, BHP-17-10 are genetically identical to each other and the MDA-MB-435S/M14 melanoma cell line) or colon cancer cell lines (ARO and KAT-4 cells are genetically identical to each other and to HT-29 human colon cancer cell line).