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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Specifications & Purity | Moligand™, ≥98% |
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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 -20°C |
Shipped In | Ice chest + Ice pads |
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 |
ALogP | 6.213 |
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HBD Count | 1 |
Rotatable Bond | 9 |
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Pubchem Sid | 488201781 |
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Pubchem Sid Url | https://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 |
CAS Registry No. | 1361030-48-9 |
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PubChem CID | 56847486 |
RCSB PDB Ligand | R6H |
PubChem SID | 488201781 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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C2331533 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C2331534 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C2331535 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C2331539 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C2331558 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C2331619 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C2331627 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C2331632 | Certificate of Analysis | Dec 19, 2022 | L413798 |
C23081514 | Certificate of Analysis | Nov 25, 2022 | L413798 |
C23081516 | Certificate of Analysis | Nov 25, 2022 | L413798 |
C23081518 | Certificate of Analysis | Nov 25, 2022 | L413798 |
C23081528 | Certificate of Analysis | Nov 25, 2022 | L413798 |
Solubility | Solubility (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; |
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DMSO(mg / mL) Max Solubility | 100 |
DMSO(mM) Max Solubility | 178.396218 |
Water(mg / mL) Max Solubility | <1 |
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] |