Loxiglumide (CR-1505) is an antagonist of cholecystokinin (CCK-1) receptor.

Kinase binding assays: For optimization of Axl/TAM receptor inhibitors, an Axl binding assay is established (HTRF method; Kinase tracer 236). This assay is based on the binding and displacement of the Alexa Fluor 647-labelled Kinase tracer 236 to each glutathione S-transferase (GST)-tagged kinase used in the binding assay. Binding of the tracer to the kinase was detected by using europium (Eu)-labelled anti-GST antibodies. Simultaneous binding of both the fluorescent tracer and the Eu-labelled antibodies to the GST-tagged kinase generates a fluorescence resonance energy transfer (FRET) signal. Binding of inhibitor to the kinase competes for binding with the tracer, resulting in a loss of the FRET signal. For the assay, the compound is diluted in 20?mM HEPES, pH?8.0, 1?mM DTT, 10?mM MgCl2 and 0.01% Brij35. Then, the kinase of interest (5?nM final concentration), fluorescent tracer (15?nM final concentration) and LanthaScreen Eu-anti-GST antibody (2?nM final concentration) are mixed with the respective compound dilutions (from 5?nM to 10?μM) and incubated for 1?h. The FRET signal is quantified using an EnVision Multilabellreader 2104.

DMSO: 4.62 mg/mL (10.01 mM), Sonication is recommended.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.17 mM), Sonication is recommended.