5.33850

TAM Receptor Kinase Inhibitor, LDC1267

• Sinônimo(s): TAM Receptor Kinase Inhibitor, LDC1267, TAM Receptor Blocker
• Fórmula empírica (Notação de Hill): C₃₀H₂₆F₂N₄O₅
• Número CAS: 1361030-48-9
• Peso molecular: 560.55
• Número MDL: MFCD28385861
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: Fc1c(ccc(c1)NC(=O)c4n[n](cc4OCC)c5c(cc(cc5)F)C)Oc2c3c(ncc2)cc(c(c3)OC)OC
• 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)
• chave InChI: ISPBCAXOSOLFME-UHFFFAOYSA-N

Descrição

Descrição geral

A cell-permeable, bioactive, non-toxic quinoline based compound that acts as a highly potent, ATP-non-competitive, tight-binding type II TAM (Tyro3, Axl, and Mer) kinase inhibitor (IC₅₀ = 8, 29, and 5 nM, respectively for Tyro3, Axl, and Mer). Occupies both the ATP binding cleft and an adjacent hydrophobic pocket. Also displays inhibitory activity against Met, Aurora B, Lck, and Src, but only at relatively higher concentration (IC₅₀ = 35, 36, 51, and 338 nM, respectively). Displays modest selectivity over 39 other protein kinases (at ~1 µM). Reduces the proliferation of selected cancer lines (~ 15 µM). By inhibiting TAM receptors, it enhances anti-metastatic activity of natural killer (NK) cells via TAMR/E3 ligase (Cbl-b; casitas B-lineage lymphoma-b) pathway modulation. Reduces the number and size of 4T1 micro metastases in the liver of an orthotopic murine model of metastatic breast cancer without apparently affecting the primary mammary tumor. Also shown to reduce metastatic spreading of B16F10 melanomas, an effect that is abolished upon NK1.1 depletion.

TAM Receptor Kinase Inhibitor, LDC1267, is a cell-permeable, tight-binding "type II" TAM kinase inhibitor (IC₅₀ = 8, 29 & 5 nM for Tyro3, Axl & Mer). Enhances anti-metastatic activity of NK cells.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Tyro3, Axl, and Mer kinases

Secondary Target
Met, Aurora B, Lck and Src kinases

Target IC₅₀: 8, 29, and 5 nM for Tyro3, Axl, and Mer, respectively

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Paolino, M., et al. 2014. Nature.507, 508.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable