Axl-IN-3 

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^[1].

IC50: 41.5 nM (AXL kinase)^[1]

Axl-IN-3 (Compound 54) shows anti-proliferative activity in SKOV3 cells with a GI₅₀ of 1.02 μM^[1].
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^[1].

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

Pharmacokinetic studies of Axl-IN-3 (Compound 54) at 5 mg/kg reveal rapid oral absorption with a T_max of 0.25 hr, C_max of 460 ng/mL, T_1/2 of 2.46 hr, and area under the curve (AUC) values of 1620 (ng*hr/mL)^[1].

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

464.95

C₂₄H₂₅ClN₆O₂

2783991-34-2

COC1=CC=C(C=C1)N2C=C(C=N2)C3=NNC4=C3C=C(C(Cl)=C4)N[C@@H]5CCN(C5)C6COC6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Pearly Shuyi Ng, et al. Fragment-based lead discovery of indazole-based compounds as AXL kinase inhibitors. Bioorg Med Chem. 2021 Nov 1;49:116437.  [Content Brief]