| Identification | Back Directory | [Name]
LDC1267 | [CAS]
1361030-48-9 | [Synonyms]
LDC1267
CS-1641
LDC 1267;LDC-1267
LDC1267 USP/EP/BP
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
1H-Pyrazole-3-carboxamide, N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)- | [Molecular Formula]
C30H26F2N4O5 | [MDL Number]
MFCD28385861 | [MOL File]
1361030-48-9.mol | [Molecular Weight]
560.55 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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 |
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| Company Name: |
Wuhan Topule Gold
|
| Telephone: |
+86-02787215551 19945035818 |
| Website: |
http://www.topule.com/ |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
|