Home Protein Tyrosine Kinase Axl inhibitor - Tyro3 inhibitor - Mertk inhibitor LDC1267

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LDC1267 Axl inhibitor

Cat.No.S7638

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

Chemical Structure

Molecular Weight: 560.55

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 560.55 Formula

C30H26F2N4O5

 Storage (From the date of receipt)
CAS No. 1361030-48-9 Download SDF Storage of Stock Solutions

Synonyms N/A 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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (178.39 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Mer [1]
(Cell-free assay)
<5 nM
Tyro3 [1]
(Cell-free assay)
8 nM
Axl [1]
(Cell-free assay)
29 nM
In vitro
LDC1267 moderately affects cell proliferation in 11 of 95 different cell lines with IC50 of >5μM. In NKG2D-activated NK cells, this compound 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, this 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 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]
References

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