LDC1267
- Product Name
- LDC1267
- CAS No.
- 1361030-48-9
- Chemical Name
- LDC1267
- Synonyms
- CS-1641;LDC1267;LDC 1267;LDC-1267;LDC1267 USP/EP/BP;LDC1267, 10 mM in DMSO;TAM Receptor Kinase Inhibitor, LDC1267;LDC 1267,LDC1267,Tyro3,Inhibitor,LDC-1267,inhibit,TAM Receptor,Axl,Mer;N-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-3-fluoro-phenyl]-4-ethoxy-1-(4-fluoro-2-methyl-phenyl)pyrazole-3-carboxamide;N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)-1H-pyrazole-3-carboxamide;N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluoro-2-methylphenyl)-1H-pyrazole-3-carboxamide
- CBNumber
- CB02734808
- Molecular Formula
- C30H26F2N4O5
- Formula Weight
- 560.55
- MOL File
- 1361030-48-9.mol
LDC1267 Property
- Boiling point:
- 628.4±55.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; insoluble in EtOH; ≥20.75 mg/mL in DMSO
- form
- solid
- pka
- 9.36±0.70(Predicted)
- color
- White to off-white
- InChIKey
- ISPBCAXOSOLFME-UHFFFAOYSA-N
- SMILES
- N1(C2=CC=C(F)C=C2C)C=C(OCC)C(C(NC2=CC=C(OC3C4C(N=CC=3)=CC(OC)=C(OC)C=4)C(F)=C2)=O)=N1
N-Bromosuccinimide Price
- Product number
- 29459
- Product name
- LDC-1267
- Packaging
- 1mg
- Price
- $36
- Updated
- 2024/03/01
- Product number
- 29459
- Product name
- LDC-1267
- Packaging
- 25mg
- Price
- $553
- Updated
- 2024/03/01
- Product number
- 29459
- Product name
- LDC-1267
- Packaging
- 5mg
- Price
- $145
- Updated
- 2024/03/01
- Product number
- 29459
- Product name
- LDC-1267
- Packaging
- 10mg
- Price
- $239
- Updated
- 2024/03/01
- Product number
- 1703DN
- Product name
- CID56847486
- Packaging
- 5mg
- Price
- $260
- Updated
- 2021/12/16
LDC1267 Chemical Properties,Usage,Production
Uses
LDC1267 is a highly selective TAM (Tyro3, Axl and Mer) kinase inhibitor with IC50s of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively[1].
Biological Activity
LDC1267 is a highly selective TAM kinase inhibitor with IC50s of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Low activity against Met, Aurora B, Lck, Src, and CDK8.
in vitro
LDC1267 moderately affected proliferation in 11 of 95 different cell lines with IC50 >5 μM. In NKG2D-activated NK cells, it abrogates the inhibitory effect of Gas6 stimulation.
in vivo
In B16F10 melanoma-bearing mice, LDC1267 (20 mg/kg, ip) potently enhanced anti-metastatic NK cell activity and resisted tumor metabolism without severe cytotoxicity.
target
| Target | Value |
| Mer (Cell-free assay) | <5 nM |
| Tyro3 (Cell-free assay) | 8 nM |
| Axl (Cell-free assay) | 29 nM |
IC 50
Axl; Tyro3; Mer
References
[1] Paolino M, et al. The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature. 2014 Mar 27;507(7493):508-12. DOI:10.1038/nature12998
LDC1267 Preparation Products And Raw materials
Raw materials
Preparation Products
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