CAS NO: | 1361030-48-9 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 560.55 |
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Formula | C30H26F2N4O5 |
CAS No. | 1361030-48-9 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 100 mg/mL (178.4 mM) |
Water: <1 mg/mL | |
Ethanol: 2 mg/mL (3.6 mM) | |
Other ifo | Chemical Name: N-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-3-fluoro-phenyl]-4-ethoxy-1-(4-fluoro-2-methyl-phenyl)pyrazole-3-carboxamide InChi Key: ISPBCAXOSOLFME-UHFFFAOYSA-N InChi Code: 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) SMILES Code: O=C(C1=NN(C2=CC=C(F)C=C2C)C=C1OCC)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C(F)=C3 |
Synonyms | LDC-1267; LDC1267; LDC 1267. |
In Vitro | In vitro activity: 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. Kinase Assay: For optimization of Axl/TAM receptor inhibitors, an Axl binding assay is established (HTRF method; Kinase tracer 236). This assay is based on the binding and displacement of the Alexa Fluor 647-labelled Kinase tracer 236 to each glutathione S-transferase (GST)-tagged kinase used in the binding assay. Binding of the tracer to the kinase was detected by using europium (Eu)-labelled anti-GST antibodies. Simultaneous binding of both the fluorescent tracer and the Eu-labelled antibodies to the GST-tagged kinase generates a fluorescence resonance energy transfer (FRET) signal. Binding of inhibitor to the kinase competes for binding with the tracer, resulting in a loss of the FRET signal. For the assay, the compound is diluted in 20 mM HEPES, pH 8.0, 1 mM DTT, 10 mM MgCl2 and 0.01% Brij35. Then, the kinase of interest (5 nM final concentration), fluorescent tracer (15 nM final concentration) and LanthaScreen Eu-anti-GST antibody (2 nM final concentration) are mixed with the respective compound dilutions (from 5 nM to 10 μM) and incubated for 1 h. The FRET signal is quantified using an EnVision Multilabellreader 2104. Cell Assay: After incubation for 72 hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control. Cell lines: A panel of 93 cancer cell lines and two primary cells (x axis, IMR90 and human peripheral blood mononuclear cells). |
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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. |
Animal model | Mouse B16F10 metastatic melanoma model |
Formulation & Dosage | Dissolved in 90% PEG400:10% DMSO; 20 mg/kg; i.p. |
References | Nature. 2014 Mar 27;507(7493):508-12. |