2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. TL4830031

TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research.

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TL4830031 Chemical Structure

TL4830031 Chemical Structure

CAS No. : 2084107-15-1

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Based on 1 publication(s) in Google Scholar

TL4830031 Related Antibodies

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Axl Mer Tyro3

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Description

TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research[1].

IC50 & Target

Axl

 

In Vitro

TL4830031 (compound 8i) binds to Axl with a Kd value of 1.1 nM. TL4830031 exhibits a 25 fold less potency against Mer with a Kd value of 25 nM, while it is much less potent to Tyro3 with a Kd value of 750 nM[1].
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[1].
TL4830031 (0-5000 nM; 4 h) reverses the expression of the EMT markers induced by TGF-β1 in MDA-MB-231 cells[1].
TL4830031 (0-5000 nM; 24 h) suppresses migration and invasion of MDA-MB-231 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TL4830031 Related Antibodies

Western Blot Analysis[1]

Cell 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 Analysis[1]

Cell 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[1].
TL4830031 (2.5-50 mg/kg; p.o. and i.v.; SD rats) exhibits reasonable pharmacokinetic (PK) properties with an AUC0-∞ value of 25944.7 μg/mL·h and a T1/2 value of 5.68 h at an oral dose of 25 mg/kg. The Cmax (2386.9 µg/L=3.6 µM) occurred at 4.0 h postdose[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice[1]
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[1]
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)
AUC0-∞ (μg/mL·h) 25944.7 20680.6
Cmax (ng/mL) 2386.9 4358.2
T1/2 (h) 5.68 4.26
Tmax (h) 4.0
CLz (L/h/kg) 0.12
BA (%) 12.5
Molecular Weight

657.66

Formula

C35H33F2N5O6
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2.38 mg/mL (3.62 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5205 mL 7.6027 mL 15.2054 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5205 mL 7.6027 mL 15.2054 mL 38.0136 mL
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TL4830031 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TL48300312084107-15-1TL 4830031TL-4830031TAM ReceptorTyro3AxlMerquinolonesselective inhibitorbreast canceranticancerphosphorylationcell invasioncell migrationInhibitorinhibitorinhibit

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