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| Cas No.: | 1361030-48-9 |
| Chemical Name: | N-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-3-fluoro-phenyl]-4-ethoxy-1-(4-fluoro-2-methyl-phenyl)pyrazole-3-carboxamide |
| Synonyms: | LDC 1267,LDC-1267 |
| SMILES: | FC1=CC(NC(C2=NN(C3=CC=C(F)C=C3C)C=C2OCC)=O)=CC=C1OC4=CC=NC5=CC(OC)=C(OC)C=C54 |
| Formula: | C30H26F2N4O5 |
| M.Wt: | 560.55 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | LDC1267 is a highly selective TAM(Tyro3, Axl and Mer) kinase inhibitor with IC50 of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively. |
| Target: | IC50 value: <5 nM/8 nM/29 nM(Tyro3/Axl/Mer) [1]: TAM kinase inhibitor |
| In Vivo: | wild-type mice treated with LDC1267 showed enhanced cytotoxicity towardsRMAcells overexpressing the NKG2D ligand Rae-1 (RMA-Rae1) to the same extent as C373AKI/KI mice, but had no effect on the already enhanced NK cytotoxicity in Cbl-b-mutant mice. Challenged mice with B16F10 melanoma followedby intraperitoneal LDC1267 treatment. LDC1267 markedly reduced metastatic spreading ofmelanomas; NK1.1 depletion abolished the therapeutic benefits of LDC1267. |
| In Vitro: | LDC1267 preferentially inhibits Tyro3,Axl andMer at lownanomolarity, as determined by tracer-based binding assays. Treatment of NKG2D activated NK cells with LDC1267 indeed abolished the inhibitory effects of Gas6 stimulation;LDC1267 had no apparent additional effect in Cbl-b-deficient NK cells. |
| 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. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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