产品
编 号：F748723
分子式：C35H33F2N5O6
分子量：657.66
分子式：C35H33F2N5O6
分子量：657.66
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2084107-15-1
产品详情
生物活性：
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.
体内研究：
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 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.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 Administrationp.o. (25 mg/kg)i.v. (2.5 mg/kg)
AUC0-∞ (μg/mL·h)25944.720680.6
Cmax (ng/mL)2386.94358.2
T1/2 (h)5.684.26
Tmax (h)4.0
CLz (L/h/kg)0.12
BA (%)12.5
体外研究：
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.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.
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.
体内研究：
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 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.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 Administrationp.o. (25 mg/kg)i.v. (2.5 mg/kg)
AUC0-∞ (μg/mL·h)25944.720680.6
Cmax (ng/mL)2386.94358.2
T1/2 (h)5.684.26
Tmax (h)4.0
CLz (L/h/kg)0.12
BA (%)12.5
体外研究：
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.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.
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