1361030-48-9

LDC1267 is a highly selective TAM (Tyro3, Axl and Mer) kinase inhibitor with IC50s of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively[1].

LDC1267 is a highly selective TAM kinase inhibitor with IC50s of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Low activity against Met, Aurora B, Lck, Src, and CDK8.

LDC1267 moderately affected proliferation in 11 of 95 different cell lines with IC50 >5 μM. In NKG2D-activated NK cells, it abrogates the inhibitory effect of Gas6 stimulation.

In B16F10 melanoma-bearing mice, LDC1267 (20 mg/kg, ip) potently enhanced anti-metastatic NK cell activity and resisted tumor metabolism without severe cytotoxicity.

Target	Value
Mer (Cell-free assay)	<5 nM
Tyro3 (Cell-free assay)	8 nM
Axl (Cell-free assay)	29 nM

Axl; Tyro3; Mer

Store at -20°C

[1] Paolino M, et al. The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature. 2014 Mar 27;507(7493):508-12. DOI:10.1038/nature12998