| Name | LDC1267 |
| Description | LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM). |
| Cell Research | After incubation for 72?hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control.(Only for Reference) |
| Kinase Assay | 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. |
| In vitro | In mice bearing B16F10 melanoma, intraperitoneal injection of LDC1267 (20 mg/kg) exhibits high safety and is capable of inhibiting tumor metabolism and enhancing the activity of anti-metastatic NK cells. |
| In vivo | In various cell lines, LDC1267 exhibits inhibition of cellular proliferation with an IC50 >5 μM. Moreover, in NKG2D-activated NK cells, LDC1267 can block the inhibitory effect induced by Gas6 stimulation. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 45.4 mg/mL (80.99 mM), Sonication is recommended.
Ethanol : 2 mg/mL (3.57 mM), Heating is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.89 mM), Sonication is recommended.
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| Keywords | Tyro3 | TAMReceptor | TAM Receptor | Mer | LDC-1267 | LDC1267 | LDC 1267 | Inhibitor | inhibit | AXL |
| Inhibitors Related | UNC2025 | Cabozantinib | Bemcentinib | Gilteritinib | UNC 1025 | Dubermatinib | Sitravatinib | NCT-503 | Tepotinib | Cabozantinib S-malate | AXL-IN-13 | BMS 777607 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
