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编 号:F755980
分子式:C24H25ClN6O2
分子量:464.95
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生物活性:
Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.

体内研究:
Pharmacokinetic studies of Axl-IN-3 (Compound 54) at 5 mg/kg reveal rapid oral absorption with a Tmax of 0.25 hr, Cmax of 460 ng/mL, T1/2 of 2.46 hr, and area under the curve (AUC) values of 1620 (ng*hr/mL).

体外研究:
Axl-IN-3 (Compound 54) shows anti-proliferative activity in SKOV3 cells with a GI50 of 1.02 μM.Axl-IN-3 (Compound 54; 1-10 μM; pretreated 1 h) inhibits AXL signaling in SKOV3 cells. Axl-IN-3 shows a dose dependent reduction of phosphorylated AXL (pAXL) levels compared to untreated cells. Additionally, the reduction of pAXL levels also lead to the concomitant reduction in downstream pERK1/2 levels.
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