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TL4830031 - ≥98.0%, high purity , CAS No.2084107-15-1

COA

Grade & Purity:

≥98%

Cas Number: 2084107-15-1
Molecular Weight: 657.66

In stock

Item Number

T651405

Grouped product items
SKU	Size	Availability	Price	Qty
T651405-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$980.90
T651405-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,500.90

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Protein Tyrosine Kinase/RTK (1314) Receptor Tyrosine Kinase (1260) TAM Receptor (37)

Basic Description

Specifications & Purity	≥98%
Biochemical and Physiological Mechanisms	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
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	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

Names and Identifiers

Smiles	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
Molecular Weight	657.66

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

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

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