Home Protein Tyrosine Kinase Axl inhibitor - Tyro3 inhibitor - Mertk inhibitor LDC1267 For research use only.

LDC1267

LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.

LDC1267 Chemical Structure

LDC1267 Chemical Structure

CAS No. 1361030-48-9

Purity & Quality Control

Batch: S763801 DMSO]100 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.75%
99.75

LDC1267 Related Products

Biological Activity

Description LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
Targets
Mer [1]
(Cell-free assay)		 Tyro3 [1]
(Cell-free assay)		 Axl [1]
(Cell-free assay)
<5 nM 8 nM 29 nM
In vitro
In vitro LDC1267 moderately affects cell proliferation in 11 of 95 different cell lines with IC50 of >5μM. In NKG2D-activated NK cells, LDC1267 abolishes the inhibitory effects of Gas6 stimulation. [1]
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.
Cell Research Cell lines A panel of 93 cancer cell lines and two primary cells (x axis, IMR90 and human peripheral blood mononuclear cells)
Concentrations ~30 μM
Incubation Time 72 hours
Method After incubation for 72 hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control.
In Vivo
In vivo In B16F10 melanoma-bearing mice, LDC1267 (20 mg/kg, i.p.) efficiently enhances anti-metastatic NK cell activity, and rejects tumor metastases without serious cytotoxicity. [1]
Animal Research Animal Models Mouse B16F10 metastatic melanoma model
Dosages 20 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 560.55 Formula

C30H26F2N4O5
CAS No. 1361030-48-9 SDF Download LDC1267 SDF
Smiles CCOC1=CN(N=C1C(=O)NC2=CC(=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)F)C5=C(C=C(C=C5)F)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (178.39 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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