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

CAS: 2084107-15-1 Cat. No.: T651405 Fórmula: C₃₅H₃₃F₂N₅O₆ Peso molecular: 657.66

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Visão geral

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

Especificações e pureza

≥98%

Mecanismos bioquímicos e 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

Condições de armazenamento de armazenamento

Store at -20°C

Enviado em

Ice chest + Ice pads

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Pureza

≥98%

Nomes e identificadores

• Sorrisos canónicos: 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

Propriedades químicas e físicas

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

Perguntas frequentes

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2084107-15-1, the molecular formula is C35H33F2N5O6, and the molecular weight is 657.66 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.