TL4830031 - ≥98% , CAS No.2084107-15-1

CAS: 2084107-15-1 Cat. No.: T651405 Peso molecular: 657.66

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC 50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research.

In Vitro

TL4830031 (compound 8i) binds to Axl with a K d value of 1.1 nM. TL4830031 exhibits a 25 fold less potency against Mer with a K d value of 25 nM, while it is much less potent to Tyro3 with a K d value of 750 nM. TL4830031 (0-5000 nM; 4 h; MDA-MB-231 cells) inhibits the phosphorylation of Axl (pAxl (Tyr702)) and the downstream Akt(pAkt(Thr308)) in a dose-dependent manner. TL4830031 (0-5000 nM; 4 h) reverses the expression of the EMT markers induced by TGF-β1 in MDA-MB-231 cells. TL4830031 (0-5000 nM; 24 h) suppresses migration and invasion of MDA-MB-231 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MDA-MB-231 cells Concentration: 0, 8, 40, 200, 1000 and 5000 nM Incubation Time: 4 hours Result: Inhibited the phosphorylation of Axl (pAxl (Tyr702)) and the downstream Akt (pAkt(Thr308)) at a low concentration. Western Blot AnalysisCell Line: MDA-MB-231 cells Concentration: 0, 40, 200, 1000 and 5000 nM Incubation Time: 4 hours Result: Increased the expression of epithelial marker E-cadherin and decreased the expression of mesenchymal marker N-cadherin in MDA-MB-231 cells.

In Vivo

TL4830031 (compound 8i) (0-800 mg/kg; p.o.; daily, for 7 d; ICR mice) has toxicity to liver and kidney in ICR mice . TL4830031 (2.5-50 mg/kg; p.o. and i.v.; SD rats) exhibits reasonable pharmacokinetic (PK) properties with an AUC 0-∞ value of 25944.7 μg/mL·h and a T 1/2 value of 5.68 h at an oral dose of 25 mg/kg. The C max (2386.9 µg/L=3.6 µM) occurred at 4.0 h postdose . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: ICR mice Dosage: 0, 50, 100, 200, 400, 600 and 800 mg/kg Administration: Oral administration; daily, for 7 days Result: Had toxicity to liver and kidney at 200 mg/kg, 400 mg/kg and 800 mg/kg administration. Animal Model: SD rats Dosage: 2.5 and 25 mg/kg Administration: Oral administration (2.5 mg/kg) and intravenous injection (25 mg/kg) Result: 1.19 Administration p.o. (25 mg/kg) i.v. (2.5 mg/kg) AUC 0-∞ (μg/mL·h) 25944.7 20680.6 C max (ng/mL) 2386.9 4358.2 T 1/2 (h) 5.68 4.26 T max (h) 4.0 CLz (L/h/kg) 0.12 BA (%) 12.5

Form:Solid

Specifications

Especificaciones y pureza

≥98%

Mecanismos bioquímicos y fisiológicos

TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC 50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl . TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Pureza

≥98%

Nombres e identificadores

• Sonrisas canónicas: O=C(C1=CN2C3=C(CCC2C)C(N4CCC(CC4)O)=C(F)C=C3C1=O)NC5=CC=C(C(F)=C5)OC6=NC=NC7=C6C=C(OC)C(OC)=C7
• Peso molecular: 657.66

Propiedades químicas y físicas

• Solubilidad: DMSO : 2.38 mg/mL (3.62 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)