For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I043350 |
| CAS Number | 2084107-15-1 |
| Synonyms | N-[4-(6,7-dimethoxyquinazolin-4-yl)oxy-3-fluorophenyl]-7-fluoro-8-(4-hydroxypiperidin-1-yl)-12-methyl-4-oxo-1-azatricyclo[7.3.1.05,13]trideca-2,5,7,9(13)-tetraene-3-carboxamide |
| Molecular Formula | C35H33F2N5O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C35H33F2N5O6/c1-18-4-6-21-31-23(13-26(37)32(21)41-10-8-20(43)9-11-41)33(44)24(16-42(18)31)34(45)40-19-5-7-28(25(36)12-19)48-35-22-14-29(46-2)30(47-3)15-27(22)38-17-39-35/h5,7,12-18,20,43H,4,6,8-11H2,1-3H3,(H,40,45) |
| InChIKey | SRXCPBOKWGKZRP-UHFFFAOYSA-N |
| SMILES | CC1CCC2=C3N1C=C(C(=O)C3=CC(=C2N4CCC(CC4)O)F)C(=O)NC5=CC(=C(C=C5)OC6=NC=NC7=CC(=C(C=C76)OC)OC)F |
| Reference | [1]. Tan L, et, al. Quinolone antibiotic derivatives as new selective Axl kinase inhibitors. Eur J Med Chem. 2019 Mar 15;166:318-327. |
