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LDC1267 - 98%, high purity , CAS No.1361030-48-9, Inhibitor of AXL receptor tyrosine kinase;Inhibitor of MER proto-oncogene; tyrosine kinase;Inhibitor of TYRO3 protein tyrosine kinase

  • Moligand™
  • ≥98%
Item Number
L413798
Grouped product items
SKUSizeAvailabilityPrice Qty
L413798-5mg
5mg
In stock
$86.90
L413798-25mg
25mg
In stock
$391.90
L413798-100mg
100mg
In stock
$532.90
L413798-250mg
250mg
In stock
$1,199.90

Axl Inhibitors

Basic Description

Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsLDC1267 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.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of AXL receptor tyrosine kinase;Inhibitor of MER proto-oncogene; tyrosine kinase;Inhibitor of TYRO3 protein tyrosine kinase
Product Description

Information

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.


Targets

Mer (Cell-free assay); Tyro3 (Cell-free assay); Axl (Cell-free assay) <5 nM; 8 nM; 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, LDC1267 abolishes the inhibitory effects of Gas6 stimulation.


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.


Cell Research(from reference)

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 

Product Properties

ALogP6.213
HBD Count1
Rotatable Bond9

Associated Targets

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK8 Tchem Cyclin-dependent kinase 8 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK19 Tchem Cyclin-dependent kinase 19 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DDR1 Tchem Epithelial discoidin domain-containing receptor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SRC Tclin Proto-oncogene tyrosine-protein kinase Src 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MST1R Tchem Macrophage-stimulating protein receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ROS1 Tclin Proto-oncogene tyrosine-protein kinase ROS 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

STK10 Tchem Serine/threonine-protein kinase 10 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TYRO3 Tchem Tyrosine-protein kinase receptor TYRO3 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FRK Tchem Tyrosine-protein kinase FRK 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HIPK4 Tchem Homeodomain-interacting protein kinase 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FER Tclin Tyrosine-protein kinase Fer 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MERTK Tchem Tyrosine-protein kinase Mer 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDGFRB Tclin Platelet-derived growth factor receptor beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

LCK Tclin Tyrosine-protein kinase Lck 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BLK Tchem Tyrosine-protein kinase Blk 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKC Tchem Aurora kinase C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHEK2 Tchem Serine/threonine-protein kinase Chk2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AXL Tchem Tyrosine-protein kinase receptor UFO 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TIE1 Tchem Tyrosine-protein kinase receptor Tie-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HCK Tclin Tyrosine-protein kinase HCK 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NTRK3 Tclin NT-3 growth factor receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MUSK Tchem Muscle, skeletal receptor tyrosine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Pubchem Sid488201781
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488201781
IUPAC Name N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)pyrazole-3-carboxamide
INCHI InChI=1S/C30H26F2N4O5/c1-5-40-28-16-36(23-8-6-18(31)12-17(23)2)35-29(28)30(37)34-19-7-9-25(21(32)13-19)41-24-10-11-33-22-15-27(39-4)26(38-3)14-20(22)24/h6-16H,5H2,1-4H3,(H,34,37)
InChi Key ISPBCAXOSOLFME-UHFFFAOYSA-N
Canonical 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
Isomeric 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
PubChem CID 56847486
Molecular Weight 560.55

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12 results found

Lot NumberCertificate TypeDateItem
C2331533Certificate of AnalysisDec 19, 2022 L413798
C2331534Certificate of AnalysisDec 19, 2022 L413798
C2331535Certificate of AnalysisDec 19, 2022 L413798
C2331539Certificate of AnalysisDec 19, 2022 L413798
C2331558Certificate of AnalysisDec 19, 2022 L413798
C2331619Certificate of AnalysisDec 19, 2022 L413798
C2331627Certificate of AnalysisDec 19, 2022 L413798
C2331632Certificate of AnalysisDec 19, 2022 L413798
C23081514Certificate of AnalysisNov 25, 2022 L413798
C23081516Certificate of AnalysisNov 25, 2022 L413798
C23081518Certificate of AnalysisNov 25, 2022 L413798
C23081528Certificate of AnalysisNov 25, 2022 L413798

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 100 mg/mL warmed with 50ºC Water: bath (178.39 mM); Ethanol: 2 mg/mL warmed with 50ºC Water: bath (3.56 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility100
DMSO(mM) Max Solubility178.396218
Water(mg / mL) Max Solubility<1

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References

1. Paolino M, Choidas A, Wallner S, Pranjic B, Uribesalgo I, Loeser S, Jamieson AM, Langdon WY, Ikeda F, Fededa JP et al..  (2014)  The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells..  Nature,  507  (7493): (508-12).  [PMID:24553136]

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