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LDC1267 - 10mM in DMSO, 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

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L421370
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L421370-1ml
1ml
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$241.90
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Axl Inhibitors

View related series
Compound libraries (12325) Receptor Tyrosine Kinase (1260)

Basic Description

Synonyms N-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-3-fluoro-phenyl]-4-ethoxy-1-(4-fluoro-2-methyl-phenyl)pyrazole-3-carboxamide
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms 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.
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor 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 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Benzene and substituted derivatives
Subclass Anilides
Intermediate Tree Nodes Not available
Direct Parent Aromatic anilides
Alternative Parents Phenylpyrazoles  Diarylethers  Quinolines and derivatives  Pyrazole-5-carboxamides  Phenoxy compounds  2-heteroaryl carboxamides  Anisoles  Toluenes  Alkyl aryl ethers  Fluorobenzenes  Pyridines and derivatives  Aryl fluorides  Heteroaromatic compounds  Secondary carboxylic acid amides  Azacyclic compounds  Hydrocarbon derivatives  Organic oxides  Organofluorides  Organonitrogen compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Aromatic anilide - Diaryl ether - Phenylpyrazole - Quinoline - 2-heteroaryl carboxamide - Phenoxy compound - Phenol ether - Pyrazole-5-carboxamide - Anisole - Halobenzene - Fluorobenzene - Alkyl aryl ether - Toluene - Pyridine - Aryl halide - Aryl fluoride - Heteroaromatic compound - Pyrazole - Azole - Secondary carboxylic acid amide - Carboxamide group - Azacycle - Organoheterocyclic compound - Carboxylic acid derivative - Ether - Organooxygen compound - Organic oxygen compound - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Organonitrogen compound - Organofluoride - Organohalogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group.
External Descriptors Not available

Product Properties

ALogP 6.213
hba_count 7
HBD Count 1
Rotatable Bond 9

Associated Targets(Human)

TYRO3 Tchem Tyrosine-protein kinase receptor TYRO3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MERTK Tchem Tyrosine-protein kinase Mer (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MST1R Tchem Macrophage-stimulating protein receptor (2327 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BLK Tchem Tyrosine-protein kinase BLK (2498 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HCK Tclin Tyrosine-protein kinase HCK (2743 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSF1R Tclin Macrophage colony stimulating factor receptor (5179 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKC Tchem Serine/threonine-protein kinase Aurora-C (1780 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK10 Tchem Serine/threonine-protein kinase 10 (2119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FER Tclin Tyrosine-protein kinase FER (2362 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FRK Tchem Tyrosine-protein kinase FRK (2284 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 (1523 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AXL Tchem Tyrosine-protein kinase receptor UFO (3469 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TIE1 Tchem Tyrosine-protein kinase receptor Tie-1 (296 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TYRO3 Tchem Tyrosine-protein kinase receptor TYRO3 (2906 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DDR1 Tchem Epithelial discoidin domain-containing receptor 1 (1050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MERTK Tchem Proto-oncogene tyrosine-protein kinase MER (2687 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROS1 Tclin Proto-oncogene tyrosine-protein kinase ROS (2436 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK3 Tclin NT-3 growth factor receptor (2338 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MUSK Tchem Muscle, skeletal receptor tyrosine protein kinase (1511 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK8 Tchem Cell division protein kinase 8 (1536 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK19 Tchem Cell division cycle 2-like protein kinase 6 (553 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EPHB6 Tchem Ephrin type-B receptor 6 (487 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HIPK4 Tchem Homeodomain-interacting protein kinase 4 (1718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

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)
InChIKey ISPBCAXOSOLFME-UHFFFAOYSA-N
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
Molecular Weight 560.55
Reaxy-Rn 22371579
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22371579&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 178.396218
Water(mg / mL) Max Solubility ＜1
Molecular Weight 560.500 g/mol
XLogP3 5.700
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 9
Rotatable Bond Count 9
Exact Mass 560.187 Da
Monoisotopic Mass 560.187 Da
Topological Polar Surface Area 96.700 Ų
Heavy Atom Count 41
Formal Charge 0
Complexity 860.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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