5.33850

TAM Receptor Kinase Inhibitor, LDC1267

• Sinonimo/i: TAM Receptor Kinase Inhibitor, LDC1267, TAM Receptor Blocker
• Formula empirica (notazione di Hill): C₃₀H₂₆F₂N₄O₅
• Numero CAS: 1361030-48-9
• Peso molecolare: 560.55
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: 2-8°C
• 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); ISPBCAXOSOLFME-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

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.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

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.

Azioni biochim/fisiol

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

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable