Table 2.

Axl and Mer inhibitors in development.

Compound (other names)	Axl IC50*	Mer IC50*	Other Known Targets	Phase of Development	Disease Indication	References
Small Molecule Inhibitors
Amuvatinib (MP-470)	1 μM	Unk	c-Kit, Met, c- Ret, PDGFR, Rad51	Phase I/II	Neuroendocrine, lung, and endometrial carcinomas	[34, 86]
Bosutinib (SKI-606, PF- 5208763)	0.4 μM	Unk	Src, ABL	Phase II/III	Breast carcinoma, Ph+ CML	[79, 87, 88]
Foretinib (GSK1363089, XL880)	11 nM	Unk	Met, VEGFR2	Phase II	Renal cell, gastric, and head & neck carcinomas	[33, 83, 84]
BMS-777607	1.1 nM	14 nM	Met, Ron, Tyro3, Flt- 3, AuroraB	Phase I/II	Gastroesophageal, prostate, head & neck, and renal cell carcinomas	[89]
PF-2341066	0.3 μM	Unk	Met, ALK, Ron	Phase III	NSCLC	[65]
R428	14 nM	224 nM	Tie-2, Tyro3, Ret, ABL	Preclinical	Breast carcinoma	[38]
Receptor Monoclonal Antibodies
α-Axl mAb	Unk	Unk	None	Preclinical	Breast carcinoma and NSCLC	[70, 79]
α-Mer mAb	Unk	Unk	None	Preclinical	ALL, AML, and GBM	[30, 57, 92]
Fusion Proteins
Axl-Fc	Unk	Unk	Mer, Tyro3	Preclinical		[94]
Mer-Fc	Unk	Unk	Axl, Tyro3	Preclinical	Thrombophilia	[93, 94]

^*IC₅₀ values for various compounds may not be directly comparable as they were determined by a variety of assays including in vitro kinase assays and cell-based phosphorylation assays. Unk, unknown.