LDC1267 Chemical Properties

Boiling point:

628.4±55.0 °C(Predicted)

Density 

1.32±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; insoluble in EtOH; ≥20.75 mg/mL in DMSO

form 

solid

pka

9.36±0.70(Predicted)

color 

White to off-white

InChIKey

ISPBCAXOSOLFME-UHFFFAOYSA-N

SMILES

N1(C2=CC=C(F)C=C2C)C=C(OCC)C(C(NC2=CC=C(OC3C4C(N=CC=3)=CC(OC)=C(OC)C=4)C(F)=C2)=O)=N1

LDC1267 Usage And Synthesis

Uses

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].

Biological Activity

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.

in vitro

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 vivo

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

IC 50

Axl; Tyro3; Mer

References

[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

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